Scientific Publications

June, 2025
Zhu K, Zhang T, Wang Z, Liu Q, Zhou H. P394: Frontline combination of olverembatinib and PDT-ALL-2016 pediatric inspired protocol in Philadelphia chromosome-positive acute lymphoblastic leukemia. HemaSphere 2023. 7(suppl 3): e68180f9. [2023 EHA poster presentation].
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June, 2025
Zhao Y, Zhai W, Pang A, Yang D, He Y, Wei J, Ma Q, Chen X, Han M, Feng S, Zhang R, Jiang E. Efficacy and safety of olverembatinib-based therapies in patients with Ph/BCR-ABL1-positive acute lymphoblastic leukemia. Blood 2023. 142(suppl 1): 5893.
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June, 2025
Zhang Y, Chen W, Xu Y, Pathak A, Yang Y, Yang D, Zhai Y. HPR61 Impact of an imatinib volume-based purchase policy (VBP) on the use of tyrosine kinase inhibitors (TKI) for chronic myeloid leukemia (CML) in Chinese tertiary care hospitals: a retrospective analysis. Value in Health 2022. 25(suppl 7): S477. [2022 ISPOR poster presentation].
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June, 2025
Zhang Y, Chen W, Xu Y, Pathak A, Lu Y, Yang D, Zhai Y. HPR45 Impact of nilotinib reimbursement coverage on the use of tyrosine kinase inhibitors (TKI) for chronic myeloid leukemia (CML) in Chinese tertiary care hospitals: a retrospective analysis. Value in Health 2022. 25(suppl 7): S474 [2022 ISPOR poster presentation].
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June, 2025
Zhang Y, Chen W, Pathak A, Yang Y, Yang D, Zhai Y. POSB36 Disease burden of chronic myeloid leukemia (CML) treatment failure in mainland China: a systematic literature review. Value in Health 2022. 25(suppl 1): S32. [2022 ISPOR Europe poster presentation].
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June, 2025
Zhang X, Zhao Y, Zhang R, Zhai W, He Y, Wei J, Yang D, Pang A, Ma Q, Chen X, Han M, Feng S, Jiang E. The efficacy and safety of the third generation TKI olverembatinib in adult Ph+ acute lymphoblastic leukemia with relapsed disease or persistent MRD bridging to Allo-HSCT: a case series from a single center. Blood 2023. 142(suppl 1): 5892.
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June, 2025
Zhang T, Zhu K, Zihong C, Lin R, Liu Q, Zhou H. Frontline combination of 3rd generation TKI olverembatinib and blinatumomab for Ph+/Ph-like ALL patients. Blood 2023. 142(suppl 1): 1504. [2023 ASH poster presentation].
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June, 2025
Zhang J, Wang J, Guo H, Liu T, Zhang X, Zhang R, Ruan M, Chang L, Liu X, Ren Y, Chen X, Wang H, Chen Z, Zhang Y, Chen Y, Zhang L, Guo Y, Liu F, Chen X, Zou Y, Yang W, Zhai Y, Zhu X. Safety and efficacy of olverembatinib (HQP1351) combined with lisaftoclax (APG-2575) in children and adolescents with relapsed/refractory Philadelphia chromosome–positive acute lymphoblastic leukemia (R/R Ph+ ALL): first report from a phase 1 study. Blood 2024. 144(suppl 1): 1443. [2024 ASH poster presentation].
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June, 2025
Yu L, Men L, Li Z, Huang X-J, Jiang Q. Health-related quality of life (HRQOL) in patients (pts) with tyrosine kinase inhibitor- (TKI)-resistant chronic myeloid leukemia (CML) receiving olverembatinib (HQP1351) therapy. Blood 2023. 142(suppl 1): 6358.
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June, 2025
Yu L, Men L, Huang X, Hu Y, Li W, Liu X, Xu N, Liu B, Song Y, Zhang G, Meng L, Zhu H, Du X, Chen S, Jiang Q. P1862: Patient reported outcomes in adults with TKI-resistant chronic myeloid leukemia receiving olverembatinib-therapy. HemaSphere 2024. 8(suppl 1): 3467-3468. [2024 EHA poster presentation].
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June, 2025
Xu G, Lou Y, Wang H, Yu W, Mao L, Huang J, Li C, Suo S, Tong H, Jin J. Combination of olverembatinib and VP regimen as first-line therapy for adult patients with Philadelphia chromosome-positive acute lymphoblastic leukemia. Blood 2023. 142(suppl 1): 4205. [2023 ASH poster presentation].
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June, 2025
Xiong Y, Liang Z, Min P, Wu B, Yu H, Yang D, Zhai Y. Olverembatinib (HQP1351) in combination with lisaftoclax overcomes venetoclax resistance in preclinical model of acute myeloid leukemia (AML). Blood 2024. 144(suppl 1): 5777.
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June, 2025
Wu X, Yang Z, Lu S, Zhang X, Wu D, Sun A, Miao M, Zhou H. Treatment with blinatumomab in combination with venetoclax for mixed phenotype acute leukemia. Blood 2023. 142(suppl 1): 5890.
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June, 2025
Wen Z, Zhou X, Fan Z, Liu Q, Sun J, Liu X, Xu N. Outcomes of olverembatinib based regimen in patients with Philadelphia chromosome-positive advanced leukemias: a real-world, single-center experience. Blood 2022. 140(suppl 1): 12217.
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June, 2025
Wen Z, Fan Z, Wang Q, Zhou X, He Z, Gao Z, Chen H, Liang H, Luo D, Liu X, Zhou H, Liu Q, Xu N. Olverembatinib (HQP1351)-based therapy in adults with relapsed or refractory Philadelphia chromosome-positive acute lymphoblastic leukemia or advanced chronic myeloid leukemia: results of the real-life study. Blood 2023. 142(suppl 1): 4538. [2023 ASH poster presentation].
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June, 2025
Wang G, Lv J, Tang C, Min P, Rui L, Zhang F, Wang L, Ge Y, Lian K, Liang E, Yang D, Zhai Y. Abstract 1463: ATP-site inhibitor olverembatinib, HQP1351, enhanced the effect of allosteric inhibitor on the resistance conferred by the compound mutations of BCR-ABL. Cancer Res 2021. 81(suppl 13): 1463. [2021 AACR poster presentation].
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June, 2025
Wang G, Liang E, Min P, Yu H, Wu B, Yang D, Zhai Y. Abstract 5071: Olverembatinib (HQP1351) enhances antitumor effects of immunotherapy in renal cell carcinoma (RCC). Cancer Res 2023. 83(suppl 7): 5071. [2023 AACR poster presentation].
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June, 2025
Tu S, Wang K, Song C, Zhou X, Xiong D, Huang G, Feng J, Yang J, Jin B, Wang B, Wang L, Zhuo Y, Chen H, Li Y. Safety and efficacy of single cycle blinatumomab plus VP chemotherapy for high tumor burden acute lymphoblastic leukemia in adults. Blood 2023. 142(suppl 1): 5818.
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June, 2025
Qiuxia Lv, Qiuxia Yu, Yang Cao, Wang J, Zhang Y, Wang G, Hong Z, Meng L. Olverembatinib-based therapy in recurrent Philadelphia chromosome-positive acute lymphoblastic leukemia with BCR/ABL mutation. Blood 2022. 140(suppl 1): 11688-11689.
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June, 2025
Qiu H, Zhou Z, Zhou Y, Wan X, Li N, Tao K, Li Y, Wu X, Chen Z, Liu L, Men L, Wang H, Liang E, Min P, Wang C, Jiang L, Yang D, Zhai Y, Xu R. 1973P Antitumor activity of olverembatinib (HQP1351) in patients (pts) with TKI-resistant succinate dehydrogenase- (SDH-) deficient gastrointestinal stromal tumor (GIST). Ann Oncol 2023. 34(suppl 2): S1053-S1054.
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June, 2025
Qiu H, Zhou Z, Zhou Y, Wan X, Li N, Tao K, Li Y, Wu X, Chen Z, Lihui Liu L, Men L, Wang H, Liang E, Cunlin W, Jiang L, Yang D, Xu R, and Zhai Y. Antitumor activity of olverembatinib (HQP1351) in patients (pts) with tyrosine kinase inhibitor- (TKI-) resistant succinate dehydrogenase- (SDH-) deficient gastrointestinal stromal tumor (GIST). J Clin Oncol 2023. 41(suppl 16): 11540. [2023 ASCO poster presentation].
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June, 2025
Qiu H, Zhou Z, Zhou Y, Wan X, Tao K, Li Y, Wu X, Liu L,Chen Z, Men L, Liang Z, Lu M, Jiang L, Yang D, Xu R, Zhai Y. Promising antitumor activity of olverembatinib (HQP1351) in patients (pts) with tyrosine kinase inhibitor- (TKI-) resistant succinate dehydrogenase- (SDH-) deficient gastrointestinal stromal tumor (GIST). J Clin Oncol 2022. 40(suppl 16): 11513. [2022 ASCO poster discussion].
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June, 2025
Min P, Wang G, Liang E, Wu B, Yu H, Yang D, Zhai Y. Abstract 1631: Combination of olverembatinib (HQP1351) with BCL-2 inhibitor lisaftoclax (APG-2575) overcomes resistance in gastrointestinal stromal tumors (GISTs). Cancer Res 2023. 83(suppl 7): 1631. [2023 AACR poster presentation].
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June, 2025
Lou Y, Xu G, Wang H, Mao L, Tong H, Jin J. Olverembatinib plus low-intensive regimen in frontline therapy for newly diagnosed Philadelphia chromosome-positive acute lymphoblastic leukemia: a case series from a single center. Blood 2022. 140(suppl 1): 11683-11684.
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June, 2025
Liu W, Liu Y, Zhu Y, Weng X, Wang C, Ouyang W, Xu J, Wang J, Mi J-Q. The first report of third-generation TKI olverembatinib in adult Ph/BCR-ABL1-positive acute lymphoblastic leukemia with T315I mutation and relapsed disease. Blood 2022. 140(suppl 1): 3266-3267.
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June, 2025
Liu Y, Zhu Y, Weng X, Wang C, Ouyang W, Xu J, Wang J, Mi J-Q. P370: Efficacy and safety of the third-generation TKI olverembatinib in adults Ph/BCR-ABL1-positive acute lymphoblastic leukemia with T315I mutation and relapsed/refractory disease. HemaShpere 2023. 7(suppl 3): e21249a8. [2023 EHA poster presentation].
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June, 2025
Liu W, Wang C, Tang S, Ren J, Peng L, Zhu Y, Weng X, Ouyang W, Xu J, Liu Y, Zhang W, Wang J, Mi JQ. The promising third-generation TKI olverembatinib in adult BCR::ABL1-positive acute lymphoblastic leukemia with T315I mutation and relapsed/refractory disease. Blood 2023. 142(suppl 1): 5902.
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June, 2025
Lin Y, Wu T, Liu D, Tong C. The efficacy and safety of olverembatinib combined with monoclonal antibodies as salvage therapy for RR B ALL with ABL1 fusion gene positive. Blood 2023. 142(suppl 1): 5896.
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June, 2025
Liang E, Min P, Xiong Y, Wu B, Yu H, Yang D, Zhai Y. Olverembatinib (HQP1351) enhances antitumor effects of chemotherapy in Philadelphia chromosome-positive (Ph⁺) Acute lymphoblastic leukemia (ALL). Blood 2023. 142(suppl 1): 5882.
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June, 2025
Jiang Q, Shi D, Li Z, Qin Y, Zhao T, Liu B, Chen Z, Niu Q, Men L, Wang H, Yang D, Zhai Y. Updated safety and efficacy results of phase 1 study of olverembatinib (HQP1351), a novel third-generation BCR-ABL tyrosine kinase inhibitor (TKI), in patients with TKI-resistant chronic myeloid leukemia (CML). Blood 2021. 138(suppl 1): 311. [2021 ASH oral presentation].
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June, 2025
Jiang Q, Shi D, Li Z, Hou Y, Hu Y, Li W, Liu X, Xu N, Song Y, Zhang G, Meng L, Hong Z, Liu B, Li Y, Chen S, Xue M, Zhu H, Li H, Du X, Lou J, Zhang X, Liang Y, Dai Y, Zi Chen, Qian Niu, Lichuang Men, Yang D, Zhai Y, Huang X. Updated results of pivotal phase 2 trials of olverembatinib (HQP1351) in patients (Pts) with tyrosine kinase inhibitor (TKI)-resistant BCR-ABL1 T315I-mutated chronic- and accelerated-phase chronic myeloid leukemia (CML-CP and CML-AP). Blood 2021. 138(suppl 1): 3598. [2021 ASH poster presentation].
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June, 2025
Xiong Y, Liang Z, Min P, Wu B, Yu H, Zhai G, Yu Z, Yang D, Zhai Y. Abstract 5652: Olverembatinib (HQP1351) in combination with lisaftoclax (APG-2575) overcomes venetoclax resistance in preclinical models of acute myeloid leukemia (AML). Cancer Res 2025. 85(suppl 1): 5652. [2025 AACR poster presentation].
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June, 2025
Peng B, Xiong Y, Liang Z, Min P, Yu H, Wu B, Zhai G, Yu Z, Yang D, Zhai Y. Abstract 5648: Effects of olverembatinib (HQP1351) in combination with BCL-2 inhibitor lisaftoclax (APG-2575) in T-cell acute lymphoblastic leukemia (T-ALL). Cancer Res 2025. 85(suppl 1): 5648. [2025 AACR poster presentation].
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June, 2025
Li Z, Ting Z, Hu L, Duan W, Jiang Q. Olverembatinib (HQP1351) combined with chemotherapy is an effective and safe treatment in patients with Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL) and chronic myeloid leukemia in lymphoid blast phase (CML-LBP) that failed TKI-based regimens. Blood 2023. 142(suppl 1): 5895.
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June, 2025
Jiang Q, Li Z, Qin Y, Hu Y, Li W, Liu X, Xu N, Zhang Y, Song Y, Meng L, Hong Z, Liu B, Li Y, Chen S, Xue M, Zhu H, Li H, Du X, Lou J, Zhang X, Liang Y, Dai YJ, Chen Z, Niu Q, Men L, Yang D, Zhai Y, Huang XJ. A five-year follow-up on safety and efficacy of olverembatinib (HQP1351), a novel third-generation BCR-ABL tyrosine kinase inhibitor (TKI), in patients with TKI-resistant chronic myeloid leukemia (CML) in China. Blood 2022. 140(suppl 1): 198-199. [2022 ASH oral presentation].
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June, 2025
Jiang Q, Li Z, Hou Y, Hu Y, Li W, Liu X, Xu N, Zhang Y, Song Y, Meng L, Hong Z, Liu B, Li Y, Chen S, Xue M, Zhu H, Li H, Du X, Lou J, Zhang X, Liang Y, Dai YJ, Chen Z, Niu Q, Men L, Yang D, Zhai Y, Huang XJ. Updated results of pivotal phase 2 trials of olverembatinib (HQP1351) in patients (Pts) with tyrosine kinase inhibitor (TKI)-resistant chronic- and accelerated-phase chronic myeloid leukemia (CML-CP and CML-AP) with T315I mutation. Blood 2022. 140(suppl 1): 203-204. [2022 ASH oral presentation].
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June, 2025
Li Z, Peng D, Deng J, Xiong L, Yin P, Hu J, Qian C, Yao L, Yin H, Hong M, Wu Q. Dynamic changes in ABL1 kinase domain mutations and comparative efficacy of third-generation tyrosine kinase inhibitors across different stages in acute lymphoblastic leukemia and chronic myeloid leukemia blast crisis patients. Blood 2023. 142(suppl 1): 4207. [2023 ASH poster presentation].
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June, 2025
Jabbour EJ, Kantarjian H, Issa GC, Beck JT, Klisovic RB, Mukherjee S, Oehler VG, Chen Z, Lu M, Fu T, Jiang L, Zhai Y, Yang D. Trial in progress: Phase 1b bridging study of the pharmacokinetics (PK), safety, and efficacy of orally administered olverembatinib (HQP1351) in patients with refractory chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph⁺ ALL). Blood 2021. 138(suppl 1): 2551. [2021 ASH poster presentation].
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June, 2025
Li W, Zhang Y, Zhu H, Yang Y, Xu N, Liu B, Chen Z, Chu W, Zhai Y, Hu Y. Olverembatinib as second-line (2L) therapy in patients (pts) with chronic phase-chronic myeloid leukemia (CP-CML). Blood 2024. 144(suppl 1): 480. [2024 ASH oral presentation].
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June, 2025
Jabbour E, Koller PB, Oehler VG, Jamy OH, Mukherjee S, Hunter AM, Baer MR, Beck JT, Chen Z, Guo H, Fu L, Men L, Wang H, Yang D, Zhai Y, Kantarjian H, Jiang L, Wang C. Olverembatinib (HQP1351) overcomes ponatinib resistance in patients with heavily pretreated/refractory chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Blood 2022. 140(suppl 1): 200-202. [2022 ASH oral presentation].
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June, 2025
Jiang Q, Li Z, Zhang G, Hu Y, Li W, Song Y, Li J, Zhou L, Liu B, Liu X, Xu N, Chen S, Liu Z, Zhu H, Jin J, Huang H, Qian S, Meng L, Du X, Zhao X, Gao S, Liang Y, Hou M, Wang W, Chen Z, Niu Q, Men L, Yang D, Zhai Y, Huang X. Olverembatinib (HQP1351) demonstrates efficacy vs. best available therapy (BAT) in patients (Pts) with tyrosine kinase inhibitor (TKI)-resistant chronic myeloid leukemia chronic-phase (CML-CP) in a registrational randomized phase 2 study. Blood 2023. 142(suppl 1): 869. [2023 ASH oral presentation].
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June, 2025
Jabbour EJ, Kantarjian HM, Koller PB, Jamy O, Oehler VG, Lomaia E, Hunter AM, Uspenskaya O, Samarina S, Mukherjee S, Baer MR, Zherebtsova V, Shuvaev, Turkina A, Davydkin I, Cortes JE, Guo H, Chen Z, Fu L, Wang H, Jiang L, Wang C, Yang D, Zhai Y. Update of olverembatinib (HQP1351) overcoming ponatinib and/or asciminib resistance in patients (pts) with heavily pretreated/refractory chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Blood 2023. 142(suppl 1): 1798. [2023 ASH poster presentation].
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June, 2025
Hu W, Wang Z, Chen C, Shen S. Combination of liposomal mitoxantrone, venetoclax, homoharringtonine, and olverembatinib (HQP1351) (MVHO) in pediatric patients with refractory or relapsed acute myeloid leukemia (AML): case series. Blood 2023. 142(suppl 1): 2840. [2023 ASH poster presentation].
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June, 2025
Fang DD, Zhu H, Tang Q, Wang Q, Li N, Fang X, Min P, Wang G, Yang D, Zhai Y. Abstract 1096: FMS-like tyrosine kinase 3 (FLT3) inhibition by olverembatinib (HQP1351) downregulates MCL-1 and synergizes with BCL-2 inhibitor APG-2575 in preclinical models of FLT3-mutant acute myeloid leukemia (AML). Cancer Res 2021. 81(suppl 13): 1096. [2021 AACR poster presentation].
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June, 2025
Gong X, Fang Q, Gu R, Qiu S, Liu K, Lin D, Zhou C, Zhang G, Gong B, Liu Y, Wei S, Li Y, Li S, Liu B, Hu T, Li J, Wang Y, Wei H, Mi Y, Wang J. Olverembatinib combined with venetoclax and reduced-intensity chemotherapy for patients with newly diagnosed Philadelphia chromosome-positive acute lymphoblastic leukemia: early results from a phase II study. Blood 2023. 142(suppl 1): 827. [2023 ASH oral presentation].
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June, 2025
Jabbour E, Jamy O, Koller PB, Oehler VG, Baer MR, Lomaia E, Hunter AM, Uspenskaya O, Samarina S, Cortes JE, Mukherjee S, Kim DDH, Zherebtsova V, Shuvaev V, Turkina A, Davydkin I, Guo H, Chen Z, Wang H, Fu T, Jiang L, Yang Z, Wang C, Yang D, Zhai Y, Kantarjian H. Olverembatinib (HQP1351) overcomes resistance/intolerance to asciminib and ponatinib in patients (pts) with heavily pretreated chronic-phase chronic myeloid leukemia (CP CML): a 1.5-year follow-up update with comprehensive exposure-response (E-R) analyses. Blood 2024. 144(suppl 1): 3151. [2024 ASH poster presentation].
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June, 2025
Bao M, Wang X, Zhang X, Li Z, Gale RP, Huang X, Jiang Q. 3rd-generation tyrosine kinase-inhibitors and azacitidine are safe and effective in myeloid blast-phase chronic myeloid leukaemia and result in a high proportion of subjects in 2nd chronic phase able to receive a transplant. Blood 2023. 142(suppl 1): 4550. [2023 ASH poster presentation].
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June, 2025
Chen S, Wu D, Cai W, Dou X, Liu Z, Zhu Y, Wang Y, Yang C, Hu J, Miao M, Deng X, Chen C. A phase 2 study of olverembatinib for the treatment of myeloid/lymphoid neoplasms with FGFR1 rearrangement. Blood 2024. 144(suppl 1): 1781. [2024 ASH poster presentation].
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June, 2025
Chen J, Zhu K, Cai Z, Wang Z, Lin R, Liu Q, Zhou H. P427: Combination of third generation TKI olverembatinib and chemotherapy or blinatumomab for new diagnosed adult Ph+ ALL patients. HemaSphere 2024. 8(suppl 1): 672-673. [2024 EHA poster presentation].
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June, 2025
Deng J, Zhang K, Tang Q, Huang X, Wang Q, Li N, Fang DD, Yang DD, Zhai Y. Abstract 3964: Co-targeting MDM2-p53 and BCL-2 apoptosis pathways overcomes resistance conferred by acquired BCL-2 gene mutations in preclinical models. Cancer Res 2022. 82(suppl 12): 3964. [2022 AACR poster presentation].
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June, 2025
Deng J, Tao R, Fang DD, Tang Q, Yin Y, Zhang K, Li Y, Zhai, Wang Q, Yang D, Zhai Y. Abstract 976: Inhibition of BCL-2 (by APG-2575) and CDK4/6 synergistically induces cell cycle arrest and apoptosis in ER+ breast cancer. Cancer Res 2021. 81(suppl 13): 976. [2021 AACR poster presentation].
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June, 2025
Fang DD, Tang Q, Kong Y, Rong T, Wang Q, Deng J, Yang D, Zhai Y. Abstract 981: BCL-2 inhibitor APG-2575 and homoharringtonine (HHT) synergistically induces apoptosis and inhibits tumor growth in preclinical models of acute myeloid leukemia and myelodysplastic syndromes (AML/MDS). Cancer Res 2021. 81(suppl 13): 981. [2021 AACR poster presentation].
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June, 2025
Zhou K, Sun M, Xu W, Yi S, Qi J, Nian W, Cui G, Wang J, Zhang X, Cen H, Zhou F, Huang J, Liu H, Shen A, Geng L, Feng R, Xu C, Qian W, Li F, Liu L, Li C, Zhao X, Jin J, Jing H, Ji D, Lv F, Chen Z, Men L, Wang H, Zhang K, Xu L, Zhang Z, Yang D, Wang J, Li J, Zhai Y. Updated efficacy and safety results of lisaftoclax (APG-2575) in patients (pts) with heavily pretreated chronic lymphocytic leukemia (CLL): pooled analyses of two clinical trials. Blood 2023. 142(suppl 1): 1900. [2023 ASH poster presentation].
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June, 2025
Yu Z, Liang Z, Yao X, Ji Y, Yang D, Zhai Y. APG-2449, a novel focal adhesion kinase (FAK) inhibitor, exhibits antileukemic activity and enhances lisaftoclax (APG-2575)-induced apoptosis in acute myeloid leukemia (AML). Blood 2024. 144(suppl 1): 4150. [2024 ASH poster presentation].
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June, 2025
Wang H, Wei X, Jiang Q, He W, Li Q, Liang Y, Weng J, Chen S, Ma H, Chang C, Xu Y, He Q, Chen Z, Liu L, Men L, Cong D, Zhang Z, Yang D, Zhai Y, Jin J. Safety and efficacy of lisaftoclax (APG-2575), a novel BCL-2 inhibitor (BCL-2i), in relapsed or refractory (R/R) or treatment-naïve (TN) patients (Pts) with acute myeloid leukemia (AML), myelodysplastic syndrome (MDS), or other myeloid neoplasms. Blood 2023. 142(suppl 1): 2925. [2023 ASH poster presentation].
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June, 2025
Sun M, Qi J, Song Y, Zhou K, Liu H, Shen A, Geng L, Zhou F, Huang J, Chen Z, Zhang H, Lu M, Ahmad M, Men L, Yang D, Zhai Y, Wang J. P1106: Preliminary results of a phase 1 study of novel BCL-2 inhibitor lisaftoclax (APG-2575) in Chinese patients (pts) with relapsed or refractory (R/R) non-Hodgkin lymphomas (NHLs). HemaSphere 2022. 6: 996-997. [2022 EHA poster presentation].
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June, 2025
Sun M, Qi J, Chen Z, Zhang H, Song Y, Shen A, Liu H, Huang J, Zhou F, Jin J, Lu M, Ahmad M, Men L, Cen W, Yang D, Wang J, Zhai Y. A phase 1 study to evaluate the safety, pharmacokinetics (PK) and pharmacodynamics (PD) of lisaftoclax (APG-2575), a novel BCL-2 inhibitor (BCL-2i), in patients (pts) with certain relapsed or refractory (R/R) hematologic malignancies (HMs). Blood 2021. 138(suppl 1): 3730. [2021 ASH poster presentation].
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June, 2025
Li J, Zhou K, Nian W, Cui G, Wang J, Zhang X, Cen H, Li F, Yi S, Feng R, Xu C, Qian W, Liu L, Li C, Zhao X, Chen Z, Qiao J, Zhang H, Ahmad M, Zhai Y. A phase Ib/II study of lisaftoclax (APG-2575), a novel BCL-2 inhibitor (BCL-2i), in patients (pts) with relapsed/refractory chronic lymphocytic leukemia or small lymphocytic lymphoma (R/R CLL/SLL). J Clin Oncol 2022. 40(suppl 16): 7543. [2022 ASCO poster presentation].
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June, 2025
Wang H, Wei X, Yang L, Weng J, He W, Chang C, Chen S, Ma H, Chen Z, Men L, Liu L, Tian X, Zhang Z, Cong D, Yang D, Zhai Y, Jin J. Lisaftoclax (APG-2575), a novel BCL-2 inhibitor, in combination with azacitidine in treatment of patients with myelodysplastic syndrome (MDS). Blood 2024. 144(suppl 1): 3202. [2024 ASH poster presentation].
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June, 2025
Kalinsky K, Tolcher AW, Wang S, Meric-Bernstam F, Winkler R, Li M, Sun X, Pan W, Paudyal B, Liang Z, Lu M, Yang D, Zhai Y. Phase 1b/2 study of BCL-2 inhibitor lisaftoclax (APG-2575) safety and tolerability when administered alone or combined with a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor in patients with estrogen receptor-positive (ER⁺) breast cancer or advanced solid tumors. J Clin Oncol 2022. 40(suppl 16): TPS1122. [2022 ASCO poster presentation].
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June, 2025
Fu C, Chen Z, Li W, Men L, Wu D, Yang D, Zhai Y. Trial in progress: Phase 1b/2 open-label study of lisaftoclax (APG-2575) monotherapy or in combination with lenalidomide/dexamethasone in patients with relapsed or refractory multiple myeloma (R/R MM). Blood 2021. 138(suppl 1): 4764.
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June, 2025
Paulus A, Manna A, Wang H, Chen J, Min P, Yin Y, Dutta N, Halder N, Ciccio G, Copland JA III, Han B, Bai L, Liu L, Wang M, McEachern D, Przybranowski S, Yang C-Y, Stuckey JA, Depei Wu D, Li C, Ryan J, Letai A, Ailawadhi S, Yang D, Wang S, Chanan-Khan A, Zhai Y. Abstract ID: 1549996. Lisaftoclax (APG-2575) is a novel BCL-2 inhibitor with robust antitumor activity in preclinical models of hematologic malignancy. Leuk Lymphoma 2023. 64(suppl 1): S79. [2023 iwCLL poster presentation].
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June, 2025
Ailawadhi S, Lasica M, Fu C, Thomas SK, Wu D, Yi S, Siddiqi T, Yin Q, Allan JN, Chen W, Matous JV. Preliminary data of a phase 1b/2 study of BCL-2 inhibitor lisaftoclax (APG-2575) alone or combined with ibrutinib or rituximab in patients (pts) with Waldenström macroglobulinemia (WM). J Clin Oncol 2023. 41(suppl 16): 7569. [2023 ASCO poster presentation].
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June, 2025
Fang DD, Tang Q, Wang Q, Li N, Zhou F, Zhai G, Yin Y, Yang D, Zhai Y. Abstract P208: Synergistic antitumor activity of lisaftoclax (APG-2575) and alrizomadlin (APG-115) through dual targeting of BCL-2/MDM2-P53 apoptotic pathways in preclinical models of acute myeloid leukemia. Mol Cancer Ther 2021. 20(suppl 12): P208. [2021 EORTC-NCI-AACR oral presentation].
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June, 2025
Fang DD, Tang Q, Wang Q, Kong Y, Li N, Zhou F, Tao R, Yang D, Zhai Y. Abstract P209: Collaborative crosstalk between two apoptosis pathways drives synergy of dual inhibition of BCL-2/MDM2 in preclinical models of neuroblastoma. Mol Cancer Ther 2021. 20(suppl 12): P209. [2021 EORTC-NCI-AACR oral presentation].
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June, 2025
Leahy MF, Fleming S, Kropf P, Chua C, Kadia TM, Oliai C, Kwan J, Fong CY, Richmond J, Cannell P, Dugan J, Baer MR, Ting S, Egan D, Chen Z, Niu Q, Li M, Ahmad M, Wang H, Zhai Y. Phase 1b/2 study of lisaftoclax (APG-2575) combined with azacitidine (AZA) in patients (pts) with treatment-naïve (TN) or prior venetoclax (VEN)-exposed myeloid malignancies. J Clin Oncol 2025. 43(suppl 16): 6505. [2025 ASCO oral presentation].
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June, 2025
Davids MS, Siddiqi T, Chanan-Khan A, Skarbnik A, Winter AM, Pagel JM, Smith C, Gabrail N, Perekhrestenko T, Pylypenko H, Kyselova O, Karpenko O, Popovska T, Kriachok I, Usenko H, Proidakov A, Ivanov V, Lysa T, Borisenkova E, Bakirov B, Lukavetsky L, Uspenskaya O, Konstantinova TS, Samoylova OS, Chen Z, Huang B, Li M, Ahmad M, Mudenda B, Yang D, Zhai Y. Trial in progress: Phase 1b Study of lisaftoclax (APG-2575) as a Single Agent or Combined with Other Therapeutic Agents in Patients with Relapsed and/or Refractory Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (R/R CLL/SLL). Blood 2021. 138(suppl 1): 1554. [2021 ASH poster presentation].
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June, 2025
Davids MS, Chanan-Khan A, Mudenda B, Nogaieva L, Kriachok I, Usenko H, Ivanov V, Kyselova O, Perekhrestenko T, Muzhychuk I, Myasnikov A, Maslyak Z, Proidakov A, Uspenskaya O, Borisenkova E, Marlton P, Siddiqi T, Winter A, Lysa T, Bakirov B, Fu L, Chen Z, Yu M, Li M, Glass L, Ahmad M, Karpenko O, Osipov I, De A, Paudyal B, Wang H, Winkler R, Gabrail N, Ganju V, Konstantinova TS, Samoylova OS, Yang D, Zhai Y. Lisaftoclax (APG-2575) safety and activity as monotherapy or combined with acalabrutinib or rituximab in patients (pts) with treatment-naïve, relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (R/R CLL/SLL): initial data from a phase 2 global study. Blood 2022. 140(suppl 1): 2326-2328. [2022 ASH oral presentation].
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June, 2025
Ailawadhi S, Chanan-Khan A, Paulus A, Chen Z, Huang B, Konopleva M, Brander DM, Rizzieri D, Lasica M, Tam C, Yannakou CK, Prince HM, Davids MS, He Z, Lu M, Ahmad M, Li M, Liang E, Mudenda B, Yang D, Zhai Y. First-in-human study of lisaftoclax (APG-2575), a novel BCL-2 inhibitor, in patients with relapsed/refractory (R/R) chronic lymphocytic leukemia (CLL) and other hematologic malignancies (HMs). Leuk Lymph 2021. 62(suppl 1): S1-S191. [2021 iwCLL poster presentation].
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June, 2025
Davids MS, Ailawadhi S, Chanan-Khan A, Mudenda B, Nogaieva L, Kryachock I, Usenko G, Ivanov V, Kyselova O, Perekhrestenko T, Muzhychuk I, Myasnikov A, Lukavetskyy L, Proydakov A, Uspenskaya O, Borisenkova E, Marlton P, Siddiqi T, Winter A, Lysa T, Bakirov B, Fu T, Li M, Ahmad M, Chen Z, Liang Z, Mekala DJ, Karpenko O, Osipov I, De A, Wang H, Gabrail N, Ganju V, Konstantinova T, Samoilova O, Yang D, Zhai Y. Lisaftoclax (APG-2575) demonstrates activity and safety when given with accelerated ramp-up and then combined with acalabrutinib or rituximab in patients (pts) with chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), including those with prior exposure to venetoclax. Blood 2024. 144(suppl 1): 4614. [2024 ASH poster presentation].
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June, 2025
Ailawadhi S, Chanan-Khan A, Chen Z, Huang B, Konopleva M, Brander DM, Rizzieri D, Lasica M, Tam C, Yannakou CK, Prince HM, Davids MS, He Z, Lu M, Ahmad M, Li M, Liang E, Mudenda B, Yang D, and Zhai Y. First-in-human study of lisaftoclax (APG-2575), a novel BCL-2 inhibitor (BCL-2i), in patients (pts) with relapsed/refractory (R/R) CLL and other hematologic malignancies (HMs). J Clin Oncol 2021. 39(suppl 15): 7502. [2021 ASCO poster presentation].
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June, 2025
Ailawadhi S, Chanan-Khan A, Khouri J, Yannakou CK, Chen Z, Wang Y, Guo H, Wang H, Li M, Ahmad M, Yang D, Zhai Y. Lisaftoclax (APG-2575) combined with novel therapeutic regimens in patients (pts) with relapsed or refractory multiple myeloma (R/RMM) or immunoglobulin light chain (AL) amyloidosis. Blood 2024. 144 (suppl 1): 1022. [2024 ASH oral presentation].
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June, 2025
Ailawadhi S, Chen Z, Huang B, Paulus A, Collins MC, Fu L, Li M, Ahmad M, Men L, Wang H, Davids MS, Liang E, Mekala DJ, He Z, Lasica M, Yannakou CK, Parrondo R, Glass L, Yang D, Chanan-Khan A, Zhai Y. Abstract ID: 1549882. First-in-human open-label study of lisaftoclax (APG-2575), a novel BCL-2 inhibitor, in patients with relapsed/refractory chronic lymphocytic leukemia and other hematologic malignancies. Leuk Lymphoma 2023. 64(suppl 1): S76-S77. [2023 iwCLL poster presentation].
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June, 2025
Zhai Y, Wang J. 450 Trial in progress: A phase 1b study of alrizomadlin, alone or plus 5-azacitidine or cytarabine, in pts with relapsed/refractory acute myeloid leukemia and relapsed higher-risk myelodysplastic syndrome. J Immunother Cancer 2021. 9(suppl 2). [2021 SITC poster presentation].
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June, 2025
Zhai Y, Kadia T. 445 Trial in progress: A phase 1b/2 study of alrizomadlin (APG-115), alone or combined with 5-azacitidine, in patients with relapsed/refractory acute myeloid leukemia (R/R AML). J ImmunoTher Cancer 2021. 9(suppl 2). [2021 SITC poster presentation].
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June, 2025
Wang G, Liang E, Tang C, Rui L, Min P, Lv J, Ge Y, Zhang F, Wang L, Shang J, Yang D, Zhai Y. Abstract 5439: MDM2 inhibitor alrizomadlin (APG-115) stabilizes p53 and synergizes with proteasome inhibitors in multiple myeloma. Cancer Res 2022. 82(suppl 12): 5439. [2022 AACR poster presentation].
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June, 2025
Wang G, Liang E, Min P, Yang D, Zhai Y. Abstract 1632: MDM2 inhibitor alrizomadlin (APG-115) promotes antitumor activity of mitogen-activated protein kinase (MAPK) inhibitors in uveal melanoma. Cancer Res 2023. 83(suppl 7): 1632. [2023 AACR poster presentation].
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June, 2025
Wang G, Liang E, Min P, Ge Y, Wu B, Yu H, Yang D, Zhai Y. MDM2-p53 inhibitor alrizomadlin (APG-115) enhances antitumor activity of pomalidomide in multiple myeloma (MM). Blood 2022. 140(suppl 1): 9953-9954. [2022 ASH poster presentartion].
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June, 2025
Tolcher AW, Reeves JA, McKean M, Chmielowski B, Beck JT, Shaheen MF, Somaiah N, Wilson M, Spira AI, Drabick JJ, Tang Y, Winkler R, Li M, Ahmad M, Lu M, Liang Z, Yang D, Zhai Y. Preliminary results of a phase 2 study of alrizomadlin (APG-115), a novel, small-molecule MDM2 inhibitor, in combination with pembrolizumab in patients with unresectable or metastatic melanoma or advanced solid tumors that have been resistant to immuno-oncologic (IO) drugs. J Clin Oncol 2021. 39(suppl 15): 2506. [2021 ASCO oral presentation].
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June, 2025
Tang Q, Fang DD, Yu H, Wu B, Yin Y, Yang D, Zhai Y. Abstract 2998:Inhibition of MDM2-p53 interaction by alrizomadlin (APG-115) induces pyroptotic cell death in gasdermin E (GSDME)-expressing cancer cells. Cancer Res 2022. 83(suppl 12): 2998. [2022 AACR poster presentation].
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June, 2025
Swiecicki P, Tang Y, Pearson AT, Muzaffar J, Fidler MJ, Winkler R, Fu T, Li M, Ahmad M, Yang D, Zhai Y. Trial in progress: A phase I/II trial of novel MDM2 inhibitor alrizomadlin (APG-115), with or without platinum chemotherapy, in patients with p53 wild-type salivary gland carcinoma. J Clin Oncol 2021. 39(suppl 15): TPS6094. [2021 ASCO poster presentation].
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June, 2025
Somaiah N, Van Tine BA, Chmielowski B, Drabick JJ, Chawla SP, McKean M, Spira A, O’Byrne KJ, Foresto SA, Movva S, Kim A, Gastman B, Pressey JG, Paudyal B, De A, Winkler RE, Li M, Ahmad M, Yang D, and Zhai Y. A phase 2 study of alrizomadlin, a novel MDM2/p53 inhibitor, in combination with pembrolizumab for treatment of patients with malignant peripheral nerve sheath tumor (MPNST). J Clin Oncol 2023. 41(suppl 16): 14627.
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June, 2025
Shaheen MF, Segar J, Chmielowski B, Drabick JJ, McKean M, Reeves Jr JA, Karapetis C, Orloff MM, Tolcher AW, Beck JT, Gastman B, De A, Paudyal B, Winkler RE, Li M, Ahmad M, Yang D, and Zhai Y. A phase 2 study of alrizomadlin (APG-115) in combination with pembrolizumab in patients with unresectable or metastatic cutaneous melanoma that has failed immuno-oncologic (IO) drugs.. J Clin Oncol 2023. 41(suppl 16): 9559. [2023 ASCO poster presentation].
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June, 2025
Qi J, Wei X, Li Q, Chang C, Zhou F, Huang J, Zhang Y, Xu C, Tang X, Jiang Q, Li J, Qin Q, He Q, Gao S, Liu L, Chen Z, Yu M, Wang J, Men L, Wang H, Ahmad M, Yang D, Zhai Y, Wang J. Alrizomadlin (APG-115) alone or combined with azacitidine (AZA) in patients (pts) with relapsed or refractory (R/R) acute myeloid leukemia (AML) or relapsed or progressive higher-risk myelodysplastic syndrome (HR-MDS): phase 1b trial results. Blood 2023. 142(suppl 1): 5954.
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June, 2025
Pearson AT, Muzaffar J, Bellile E, Worden FP, Chung CH, Rosenberg A, Vokes E, Fidler MJ, Brenner JC, Zhai Y, Fu T, Winkler R, Swiecicki P. 221 (PB101) – Phase I/II study of a novel MDM-2 inhibitor (APG-115) in TP53 wild type salivary gland cancers. Eur J Cancer 2022. 174(suppl 1): S79-S80. [2022 EORTC-NCI-AACR poster presentation].
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June, 2025
Pearson A, Muzaffar J, Kirtane K, Bellile E, Suresh K, Rosenberg AJ, Worden F, Chung CH, Vokes EE, Brenner C, McHugh JB, Zhai Y, Fu T, Winkler R, Swiecicki PL. Phase I/II study of a novel MDM-2 inhibitor (APG-115-alrizomadlin) in p53 wild type salivary gland cancers. Int J Radiat Oncol Biol Phys 2024. 18: e6-e7. [2024 MHNCS oral presentation].
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June, 2025
McKean M, Tolcher AW, Reeves JA, Chmielowski B, Shaheen MF, Beck JT, Orloff MM, Somaiah N, Van Tine BA, Drabick JJ, Spira AI, O'Byrne K, Karapetis CS, Foresto SA, Movva S, Martinez J, Li M, Winkler R, Yang D, Zhai Y. Newly updated activity results of alrizomadlin (APG-115), a novel MDM2/p53 inhibitor, plus pembrolizumab: Phase 2 study in adults and children with various solid tumors. J Clin Oncol 2022. 40(suppl 16): 9517. [2022 ASCO poster presentation].
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June, 2025
Kadia TM, Benton C, Erba HP, Gandhi M, Levy MY, Percival ME M, Ulrickson M, Yimer H, Yu M, Chen Z, Wang J, Li M, Ahmad M, Yang D, Zhai Y. Trial in progress: Phase 1b/2 study of alrizomadlin (APG-115), alone or combined with 5-azacitidine (AZA), in patients with relapsed/refractory acute myeloid leukemia (AML), chronic myelomonocytic leukemia (CMML), or myelodysplastic syndrome (MDS). Blood 2022. 140(suppl 1): 11659-11660.
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June, 2025
Guo Y, Li N, Zhang X, Fang M, Wang S, Yu Y, Men L, Wang H, Zhai Y. A phase 2 study of novel MDM2 inhibitor alrizomadlin (APG-115) with or without toripalimab in patients (pts) with advanced adenoid cystic carcinoma (ACC) or other solid tumors. J Clin Oncol 2025. 43(suppl 16): 6102. [2025 ASCO poster presentation].
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June, 2025
Fang DD, Tang Q, Wang Q, Li N, Zhou F, Zhai G, Yin Y, Yang D, Zhai Y. Abstract P208: Collaborative crosstalk between two apoptosis pathways drives synergy of dual inhibition of BCL-2/MDM2 in preclinical models of neuroblastoma. Mol Cancer Ther 2021. 20(suppl 12): P208. [2021 AACR-NCI-EORTC oral presentation].
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June, 2025
Zhang L, Zhao H, Zhao Y, Cheng Y, Cui J, Ma Y, Yang C, Zhang J, Xu L, Yu J, Men L, Liang Z, Yang D, Zhai Y. Updated study results of pelcitoclax (APG-1252) in combination with osimertinib in patients (pts) with EGFR-mutant non–small cell lung cancer (NSCLC). J Clin Oncol 2022. 40(suppl 16): 9116. [2022 ASCO poster presentation].
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June, 2025
Zhang L, Zhao H, Ma Y, Cheng Y, Zhao Y, Cui J, Yang C, Zhang J, Wang P, Xu L, Yu J, Men L, Liang E, Yang D, Zhai Y. MA02.06 Phase 1b study of pelcitoclax (APG-1252) in combination with osimertinib in patients with EGFR TKI-resistant NSCLC. J Thorac Oncol 2021. 16(suppl 10): S891. [2021 IASLC-WCLC oral presentation].
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June, 2025
Wu Y, Lakhani NJ, Boyer M, Zhou Q, Rasco DW, Huang Y, Men L, Li Y, Xia Z, Wang H, Ji J, Lu B, He Z, Dong Q, Yang D, Zhai Y. OA12 A phase I study of novel Bcl-2/Bcl-xL inhibitor APG-1252 in patients with advanced SCLC or other solid tumor. J Thorac Oncol 2018. 13(suppl 12): S1048-S1049. [2018 IASLC oral presentation].
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June, 2025
Wang G, Liang E, Ming P, Rui L, Tang C, LV J, Ge Y, Zhang F, Wang L, Shang J, Yang D, Zhai Y. Antitumor activity of dual BCL-2/BCL-xL inhibitor pelcitoclax (APG-1252) in natural killer/T-cell lymphoma (NK/TCL). Blood 2021. 138(suppl 1): 2062. [2021 ASH poster presentation].
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June, 2025
Qin A, Kalemkerian GP, Patel JD, Mohindra NA, Carlisle JW, Sands J, He Z, Winkler R, Liang Z, Hammock V, Bombelli R, Lu M, Xu Y, Fu T, Wang C, Yang D, Zhai Y. Trial in progress: A multicenter, phase Ib/II study of pelcitoclax (APG-1252) in combination with paclitaxel in patients with relapsed/refractory small-cell lung cancer (R/R SCLC). J Clin Oncol 2021. 39(suppl 15): TPS8589. [2021 ASCO poster presentation].
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June, 2025
Qin A, Kalemkerian GP, Mohindra NA, Patel JD, Karapetis CS, Carlisle JW, Sands J, Spira AI, Gao B, Amin H, Paudyal B, Frank G, Sun X, Xu Y, Wang C, Fu T, Winkler R, Liang Z, Yang D, Zhai Y. First-in-human study of pelcitoclax (APG-1252) in combination with paclitaxel in patients (pts) with relapsed/refractory small-cell lung cancer (R/R SCLC). J Clin Oncol 2022. 40(suppl 16): e20612.
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June, 2025
Ma Y, Zhao H, Zhao Y, Cheng Y, Cui J, Liu G, Xiong D, Zhang J, Xu L, Yu J, Men L, Liang E, Yang D, Zhai Y, Zhang L. 1317MO Updated study results of pelcitoclax (APG-1252) combined with osimertinib in patients (pts) with EGFR-mutant non-small cell lung cancer (NSCLC). Ann Oncol 2023. 34(suppl 2): S758. [2023 ESMO oral presentation].
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June, 2025
Lakhani NJ, Rasco DW, Zeng Q, Tang Y, Liang Z, Wang H, Lu M, Chen J, Fu L, Wang C, Yang D, Zhai Y. First-in-human study of palcitoclax (APG-1252), a novel dual Bcl-2/Bcl-xL inhibitor, demonstrated advantages in platelet safety while maintaining anticancer effect in U.S. patients with metastatic solid tumors. J Clin Oncol 2020. 38(suppl 15): 3509. [2020 ASCO poster discussion].
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June, 2025
Lakhani NJ, Rasco DW, Tolcher AW, Huang Y, Ji J, Wang H, Dong Q, Men L, O'Rourke TJ, Chandana SR, Amaya A, Cole Y, Kaiser B, Mays TA, Patnaik A, Papadopoulos KP, Yang D, Zhai Y. A phase I study of novel dual Bcl-2/Bcl-xL inhibitor APG-1252 in patients with advanced small cell lung cancer (SCLC) or other solid tumor. J Clin Oncol 2018. 36(suppl 15): 2594. [2018 ASCO poster presentation].
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June, 2025
Guo Y, Deng J, Zhang L, Huang X, Zhang K, Zhou F, Li Y, Luo F, Fang DD, Yang D, Chen J, Zhai Y. Abstract 984: Targeting BCL-xL addiction with pelcitoclax (APG-1252) to overcome apoptotic blockade in neuroendocrine neoplasm (NEN). Cancer Res 2021. 81(suppl 13): 984. [2021 AACR poster presentation].
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June, 2025
Zhu S, Fang DD, Li Q, Yang D, Gu S, Wang S, Yang D, Zhai Y. Abstract 3939: Preclinical development of embryonic ectoderm development (EED) inhibitor APG-5918/EEDi-5273 for cancer therapy. Cancer Res 2022. 82(suppl 12): 3939. [2022 AACR poster presentation].
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June, 2025
Zhai Y, Yin Y, Liang E, Wang H, Min P, Yang D. Embryonic ectoderm development (EED) inhibitor APG-5918 improves chronic kidney disease- (CKD)-induced hemoglobin insufficiency in preclinical models of anemia. Blood 2023. 142(suppl 1): 5268.
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June, 2025
Yin Y, Liang Z, Li B, Yang Y, Yang D, Zhai Y. Abstract 446: Embryonic ectoderm development protein (EED) inhibitor APG-5918 exhibits potent antitumor activity and synergizes with androgen receptor (AR) inhibitor enzalutamide in preclinical prostate cancer (PCa) models. Cancer Res 2025. 85(suppl 1): 446. [2025 AACR poster presentation].
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June, 2025
Liang Z, Yin Y, Guo H, Li B, Yang D, Zhai Y. Embryonic ectoderm development (EED) inhibitor APG-5918 demonstrates robust antitumor activity in preclinical models of T-cell lymphomas (TCLs). Blood 2024. 144(suppl 1): 1415. [2024 ASH poster presentation].
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June, 2025
Chen F, Yang J, Luo Q, Qiu M, Yang D. 14P EED inhibition renders vulnerability to immunotherapy by rewiring ceramide metabolism in pancreatic cancer. Ann Oncol 2024. 35(suppl 2): S219. [2024 ESMO poster presentation].
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June, 2025
Tao R, Fang DD, Li Y, Zhang K, Xu C, Fang X, Wang Q, Yang D, Zhai Y. Abstract 968: Focal adhesion kinase (FAK) inhibitor APG-2449 sensitizes ovarian tumors to chemotherapy via CD44 downregulation. Cancer Res 2021. 81(suppl 13): 968. [2021 AACR poster presentation].
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June, 2025
Tao R, Fang DD, Li Y, Zhai G, Zhou F, Wang Q, Deng J, Yang D, Zhai Y. Abstract 2563: FAK inhibitor APG-2449 and CDK4/6 inhibitor palbociclib synergistically suppress mesothelioma tumor growth via autophagy induction. Cancer Res 2022. 82(suppl 12): 2563. [2022 AACR poster presentation].
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June, 2025
Zhao H, Chen J, Song Z, Zhao Y, Guo Y, Wu G, Ma Y, Zhou W, Yu X, Gao F, Dong Y, Zhang R, Yang C, Tian X, Wang H, Tu Y, Yu J, Sun X, Zhang L, Zhai Y. First-in-human phase I results of APG-2449, a novel FAK and third-generation ALK/ ROS1 tyrosine kinase inhibitor (TKI), in patients (pts) with second-generation TKI-resistant ALK/ROS1+ non–small cell lung cancer (NSCLC) or mesothelioma. J Clin Oncol 2022. 40(suppl 16): 9071. [2022 ASCO poster presentation].
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June, 2025
Ma Y, Zhao H, Chen J, Song Z, Zhao Y, Guo Y, Wu G, Zhou W, Yu X, Gao F, Zhang R, Fang J, Lin X, Zhuang W, Tian X, Tu Y, Yu J, Liu G, Zhai Y, and Zhang L. FAK inhibition with novel FAK/ALK inhibitor APG-2449 could overcome resistance in NSCLC patients who are resistant to second-generation ALK inhibitors. J Clin Oncol 2023. 41(suppl 16): 9015. [2023 ASCO poster discussion].
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June, 2025
Yu Z, Liang Z, Yao X, Liu D, Yang D, Zhai Y. Abstract 1679: APG-2449, a novel focal adhesion kinase (FAK) inhibitor, enhances the antitumor activity of chemotherapy in preclinical models of small-cell lung cancer (SCLC) with activated FAK. Cancer Res 2025. 85(suppl 1): 1679. [2025 AACR poster presentation].
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June, 2025
Zhang X, Xu X, Guan Y, Liang X, Liu H, Liu Z, Huang X, Xu Z, Sun J, Han X, Lu F, Wang P, Wang H, Xu L, Men L, Wang C, Yang D, Zhai Y, Hou J. First-in-human study of APG-1387, targeting inhibitor of apoptosis proteins, for the treatment of patients with chronic hepatitis B. Hepatology 2022. 76(suppl 1): S30-S31. [2022 AASLD oral presentation].
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June, 2025
Li Q, Fang DD, Li Z, Yang D, Cao F, Zhai Y. Abstract 1924: Therapeutic potential of Inhibitor of Apoptosis Protein (IAP) inhibitor APG-1387 combined with DR5 agonist monoclonal antibody (mAb) CTB006 in preclinical models of solid tumors. Cancer Res 2021. 81(suppl 13): 1924. [2021 AACR poster presentation].
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June, 2025
Gu S, Li Q, Li C, Wang Q, Fang DD, Wang S, Yang D, Zhai Y. Abstract 2664: Development of covalent KRASG12C inhibitor APG-1842 for the treatment of solid tumors. Cancer Res 2022. 82(suppl 12): 2664. [2022 AACR poster presentation].
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June, 2025
Xiong Y, Yu Z, Hu J, Chen J, Han X, Liang Z, Zhai Y, Yang D. Abstract 5651: Discovery of AS03157 as a highly potent and orally active antagonist of inhibitor of apoptosis proteins (IAPs). Cancer Res 2025. 85(suppl 1): 5651. [2025 AACR poster presentation].
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June, 2025
Zhu Y, Huang J, Wang Y, Han Y, Xue S, Yang Y, Zhu Y, Cai W, Chen S. Olverembatinib treatment in adult patients with newly diagnosed Philadelphia chromosome-positive acute lymphoblastic leukemia. Ann Hematol 2024. 103: 4643-4648.
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June, 2025
Zhou J, Kryczek I, Li S, Li X, Aguilar A, Wei S, Grove S, Vatan L, Yu J, Yan Y, Liao P, Lin H, Li J, Li G, Du W, Wang W, Lang X, Wang W, Wang S, Zou W. The ubiquitin ligase MDM2 sustains STAT5 stability to control T cell-mediated antitumor immunity. Nat Immunol 2021. 22: 460-470.
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June, 2025
Vogler M, Braun Y, Smith VM, Westhoff MA, Pereira RS, Pieper NM, Anders M, Callens M, Vervliet T, Abbas M, Macip S, Schmid R, Bultynck G, Dyer MJ. The BCL2 family: from apoptosis mechanisms to new advances in targeted therapy. Signal Transduct Target Ther 2025. 10: 91.
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June, 2025
Qian H, Gang D, He X, Jiang S. A review of the therapeutic role of the new third-generation TKI olverembatinib in chronic myeloid leukemia. Front Oncol 2022. 12: 1036437.
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June, 2025
Öziskender R, Eşkazan AE. Olverembatinib in chronic myeloid leukemia. Drugs Today (Barc) 2022. 58: 531-538.
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June, 2025
Liu W, Wang C, Ouyang W, Hao J, Ren J, Peng L, Tang S, Liu Y, Zhu Y, Weng X, Jing D, Chen S, Wang J, Mi JQ. Efficacy and safety of olverembatinib in adult BCR::ABL1-positive ALL with T315I mutation or relapsed/refractory disease. Br J Haematol 2024. 205: 2228-2233.
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June, 2025
Liu D, Glubb D, O'Mara T, Ford CE. The multi-kinase inhibitor GZD824 (olverembatinib) shows pre-clinical efficacy in endometrial cancer. Cancer Med 2025. 14: e70531.
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June, 2025
Li Z, Peng D, Deng J, Xiong L, Yin P, Hu J, Qian C, Yao L, Yin H, Hong M, Wu Q. New ABL1 kinase domain mutations in BCR::ABL1-positive acute lymphoblastic leukemia. Cancer Med 2024. 13: e70317.
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June, 2025
Lian J, Zou Y, Huang L, Cheng H, Huang K, Zeng J, Chen L. Hepatitis B virus upregulates cellular inhibitor of apoptosis protein 2 expression via the PI3K/AKT/NF-κB signaling pathway in liver cancer. Oncol Lett 2020. 19: 2043-2052.
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June, 2025
Kondo T. A new face in the treatment of Philadelphia chromosome-positive acute lymphoblastic leukaemia. Br J Haematol 2024. 205: 2131-2133.
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June, 2025
Kato Y, Kunimasa K, Takahashi M, Harada A, Nagasawa I, Osawa M, Sugimoto Y, Tomida A. GZD824 inhibits GCN2 and sensitizes cancer cells to amino acid starvation stress. Mol Pharmacol 2020. 98: 669-676.
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June, 2025
Jiang K, Tang X, Guo J, He R, Chan S, Song X, Tu Z, Wang Y, Ren X, Ding K, Zhang Z. GZD824 overcomes FGFR1-V561F/M mutant resistance in vitro and in vivo. Cancer Med 2021. 10: 4874-4884.
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June, 2025
Ji J, Yu Y, Li ZL, Chen MY, Deng R, Huang X, Wang GF, Zhang MX, Yang Q, Ravichandran S, Feng GK, Xu XL, Yang CL, Qiu MZ, Jiao L, Yang D, Zhu XF. XIAP limits autophagic degradation of Sox2 and is a therapeutic target in nasopharyngeal carcinoma stem cells. Theranostics 2018. 8: 1494-1510.
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June, 2025
Jain J, Pham TNQ, Begum S, Romero-Medina MC, Bellini N, Li Y, Dallaire F, Béland K, Patey N, Guimond JV, Haddad E, Zhai Y, Cohen EA. Bivalent SMAC mimetic APG-1387 reduces HIV reservoirs and limits viral rebound in humanized mice. iScience 2024. 27: 111470.
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June, 2025
Cui Y, Shao X, Yang H, Xin J, Liu Y, Zhang M, Sun C, Chen G, Shen G, Meng X, Chen Y. MDM2 inhibitor APG-115 synergizes with ABT-199 to induce cell apoptosis in chronic lymphocytic leukemia. Front Pharmacol 2024. 15: 1441383.
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June, 2025
Cheng S, Jin P, Li H, Pei D, Shu X. Evaluation of CML TKI induced cardiovascular toxicity and development of potential rescue strategies in a zebrafish model. Front Pharmacol 2021. 12: 740529.
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May, 2025
Yu L, Li W, Xu N, Liu X, Liu B, Zhang Y, Meng L, Zhu H, Du X, Chen S, Hu Y, Song Y, Men L, Jiang Q. Patient-reported outcomes in adults with tyrosine kinase inhibitor-resistant chronic myeloid leukemia receiving olverembatinib therapy. Cancer 2025. 131: e35652.
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May, 2025
Zhang X, Yang Y, Liu B, Du X, Wang X, Zhu H, Yu L, Li Z, Zhao S, Yang L, Ma Y, Meng L, Zhang Y, Li G, Yang L, Wang B, Ran X, Huang J, Gao N, Wen Q, Wen Y, Zhao Y, Zhu Y, Han Y, Liu Z, Du X, Weng J, Gale RP, Zhou L, Zhang Y, Jiang Q. Optimizing olverembatinib dose in chronic phase chronic myeloid leukemia. Haematologica 2025.
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May, 2025
Wen Z, Liu Z, Ye X, Fan Z, Lin R, Huang F, Xuan L, Li X, Jin H, Dai M, Sun J, Zhou X, Wang Q, Liu X, Liu Q, Zhou H, Xu N. Olverembatinib (HQP1351)-based therapy in adults with relapsed or refractory Philadelphia chromosome-positive acute lymphoblastic leukemia or chronic myeloid leukemia in blast phase: results from a real-world study. Front Immunol 2025. 16: 1546371.
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May, 2025
Wang Y, Liu Q, Xu CL, Huang DP, Chen Y. Blinatumomab in combination with olverembatinib and concurrent intrathecal chemotherapy successfully treated a chronic myeloid leukemia relapse with central nervous system blast crisis: case report and literature review. Ann Hematol 2025.
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May, 2025
Vogler M, Braun Y, Smith VM, Westhoff MA, Pereira RS, Pieper NM, Anders M, Callens M, Vervliet T, Abbas M, Macip S, Schmid R, Bultynck G, Dyer MJ. The BCL2 family: from apoptosis mechanisms to new advances in targeted therapy. Signal Transduct Target Ther 2025. 10: 91.
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May, 2025
Mavroeidis L, Kalofonou F, Casey R, Napolitano A, Bulusu R, Jones RL. Identifying and managing rare subtypes of gastrointestinal stromal tumors. Expert Rev Gastroenterol Hepatol 2025. 19: 549-561.
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May, 2025
Liu D, Glubb D, O'Mara T, Ford CE. The multi-kinase inhibitor GZD824 (olverembatinib) shows pre-clinical efficacy in endometrial cancer. Cancer Med 2025. 14: e70531.
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May, 2025
Kong J, Zheng FM, Yan CH, Wang JZ, Fu HX, Wang ZD, Suo P, Hu GH, Lv M, Chen H, Mo XD, Xu LP, Zhang XH, Huang XJ, Wang Y. Efficacy and safety of olverembatinib as maintenance therapy after allogeneic hematopoietic cell transplantation in Philadelphia chromosome-positive acute lymphoblastic leukemia. Ann Hematol 2025. 104: 801-808.
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May, 2025
Kantarjian H, Zhai Y, Oehler VG, Jamy O, Koller PB, Haddad FG, Sasaki K, Jabbour EJ. Olverembatinib in chronic myeloid leukemia-Review of historical development, current status, and future research. Cancer 2025. 131: e35832.
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May, 2025
Eşkazan AE. Patient-reported outcomes in Chinese patients with chronic myeloid leukemia receiving olverembatinib: Quality of life matters!. Cancer 2025. 131: e35737.
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May, 2025
Dedousis D, Gadra E, Van Galen J, von Mehren M. Recent advances in succinate dehydrogenase deficient gastrointestinal stromal tumor systemic therapies. Curr Treat Options Oncol 2025. 26: 227-240.
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December, 2024
Jabbour E, Oehler VG, Koller PB, Jamy O, Lomaia E, Hunter AM, Uspenskaya O, Samarina S, Mukherjee S, Cortes JE, Baer MR, Zherebtsova V, Shuvaev V, Turkina A, Davydkin I, Guo H, Chen Z, Fu T, Jiang L, Wang C, Wang H, Yang D, Zhai Y, Kantarjian H. Olverembatinib after failure of tyrosine kinase inhibitors, including ponatinib or asciminib: a phase 1b randomized clinical trial. JAMA Oncol 2025. 11: 28-35.
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July, 2024
Yan Y, Qu S, Liu J, Li C, Yan X, Xu Z, Qin T, Jia Y, Pan L, Gao Q, Jiao M, Li B, Gale RP, Xiao Z. Olverembatinib for myeloid/lymphoid neoplasm associated with eosinophilia and FGFR1 rearrangement. Leuk Lymphoma 2023. 64: 1605-1610.
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July, 2024
Yang Z, Liu C, Hu Y, Liu H, Li J, Wu L, Liu Q, Zheng Y, Huang P, Wang Y. Tyrosine kinase inhibitors combined with venetoclax and azacytidine as an effective therapy for de novo lymphoid blast phase-chronic myeloid leukemia. Leuk Res 2023. 127: 107039.
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July, 2024
Xiang D, Zhao T, Wang J, Cao Y, Yu Q, Liu L, Yu H, Li X, Li N, Yi Y, Gong X. Determination of olverembatinib in human plasma and cerebrospinal fluid by an LC-MS/MS method: validation and clinical application. J Pharm Biomed Anal . 230: 115382.
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July, 2024
Li X, Zhang J, Liu F, Liu T, Zhang R, Chen Y, Guo Y, Fang Y, Xu X, Pui CH, Zhu X. Olverembatinib Treatment in Pediatric Patients With Relapsed Philadelphia-Chromosome-Positive Acute Lymphoblastic Leukemia. Lymphoma Myeloma Leuk 2023. 23: 660-666.
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July, 2024
Tan X, Wen Q, Chen G, Wan K, Liu X, Ma YY, Wang MH, Zhang X, Zhang C. Novel third-generation tyrosine kinase inhibitor for newly diagnosed Philadelphia chromosome-positive acute lymphoblastic leukemia: a case study. Anticancer Drugs 2023. 34: 599-604.
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July, 2024
Ding J, Li W. Case report: Olverembatinib monotherapy: the chemotherapy-free regimen for an elderly patient with relapsed Ph-positive acute lymphoblastic leukemia. Front Pharmacol 2023. 14: 1320641.
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July, 2024
Yin Z, Liao M, Yan R, Li G, Ou R, Liu Z, Zhong Q, Shen H, Zhu Y, Xie S, Zhang Q, Liu S, Huang J. Transcriptome- and metabolome-based candidate mechanism of BCR-ABL-independent resistance to olverembatinib in Philadelphia chromosome-positive acute lymphoblastic leukemia. Funct Integr Genomics 2023. 23: 53.
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July, 2024
Zhang T, Zhou H, Xu M, Qian C, Sun A, Wu D, Xue S. Combination venetoclax and olverembatinib (HQP1351) as a successful therapeutic strategy for relapsed/refractory (R/R) mixed-phenotype blast phase of chronic myeloid leukemia. Ann Hematol 2023. 102: 973-975.
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July, 2024
Liu C, Zhang X, Mao L, Qian J, Xiao F, Ye X, Wei J, Ye X, Jin J, Yu W. Olverembatinib in relapsed Philadelphia chromosome-positive B-cell acute lymphoblastic leukemia: a study of 5 cases. Leuk Lymphoma 2023. 64: 1208-1211.
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July, 2024
Yi H, Yan X, Luo Q, Yuan L, Li B, Pan W, Zhang L, Chen H, Wang J, Zhang Y, Zhai Y, Qiu MZ, Yang DJ. A novel small molecule inhibitor of MDM2-p53 (APG-115) enhances radiosensitivity of gastric adenocarcinoma. J Exp Clin Cancer Res 2018. 37: 97.
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July, 2024
Rej RK, Wang C, Lu J, Wang M, Petrunak E, Zawacki KP, McEachern D, Fernandez-Salas E, Yang CY, Wang L, Li R, Chinnaswamy K, Wen B, Sun D, Stuckey J, Zhou Y, Chen J, Tang G, Wang S. EEDi-5285: An exceptionally potent, efficacious, and orally active small-molecule inhibitor of embryonic ectoderm development. J Med Chem 2020. 63: 7252-7267.
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July, 2024
Luo Q, Pan W, Zhou S, Wang G, Yi H, Zhang L, Yan X, Yuan L, Liu Z, Wang J, Chen H, Qiu M, Yang D, Sun J. A novel BCL-2 inhibitor APG-2575 exerts synthetic lethality with BTK or MDM2-p53 inhibitor in diffuse large B-cell lymphoma. Oncol Res 2020. 28: 331-344.
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July, 2024
Luo F, Lu FT, Qiu MZ, Zhou T, Ma WJ, Luo M, Zeng KM, Luo QY, Pan WT, Zhang L, Xia ZF, Zhang ZH, Cao JX, Zhao HY, Zhang L, Yang DJ. Gemcitabine and APG-1252, a novel small molecule inhibitor of BCL-2/BCL-XL, display a synergistic antitumor effect in nasopharyngeal carcinoma through the JAK-2/STAT3/MCL-1 signaling pathway. Cell Death Dis 2021. 12: 772.
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July, 2024
Zhao W, Yu D, Zhai Y, Sun SY. ALK inhibitors downregulate the expression of death receptor 4 in ALK-mutant lung cancer cells via facilitating Fra-1 and c-Jun degradation and subsequent AP-1 suppression. Neoplasia 2023. 42: 100908.
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July, 2024
Ailawadhi S, Chen Z, Huang B, Paulus A, Collins MC, Fu L, Li M, Ahmad M, Men L, Wang H, Davids MS, Liang E, Mekala DJ, He Z, Lasica M, Yannakou CK, Parrondo R, Glass L, Yang D, Chanan-Khan A, Yifan Zhai Y. Novel BCL-2 inhibitor lisaftoclax in relapsed or refractory chronic lymphocytic leukemia and other hematologic malignancies: first-in-human open-label trial. Clin Cancer Res 2024. 29: 2385-2393.
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July, 2024
Somaiah N, Paudyal B, Winkler RE, Van Tine BA, Hirbe AC. Malignant peripheral nerve sheath tumor, a heterogeneous, aggressive cancer with diverse biomarkers and no targeted standard of care: review of the literature and ongoing investigational agents. Target Oncol 2024.
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July, 2024
Pan W, Luo Q, Liang E, Shi M, Sun J, Shen H, Lu Z, Zhang L, Yan X, Yuan L, Zhou S, Yi H, Zhai Y, Qiu MZ, Yang D. Synergistic effects of Smac mimetic APG-1387 with anti-PD-1 antibody are attributed to increased CD3 + NK1.1 + cell recruitment secondary to induction of cytokines from tumor cells. Cancer Cell Int 2024. 24: 181.
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July, 2024
Lakhani NJ, Rasco D, Wang H, Men L, Liang E, Fu T, Collins MC, Min P, Yin Y, Davids MS, Yang D, Zhai Y. First-in-human study with preclinical data of BCL-2/BCL-xL inhibitor pelcitoclax in locally advanced or metastatic solid tumors. Clin Cancer Res 2024. 30: 506-521.
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July, 2024
Zhang X, Wen X, Peng R, Pan Q, Weng D, Ma Y, Zhang Y, Yang J, Men L, Wang H, Liang E, Wang C, Yang D, Zhang L, Zhai Y. A first-in-human phase I study of a novel MDM2/p53 inhibitor alrizomadlin in advanced solid tumors. ESMO Open 2024. 9: 103636.
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July, 2024
Luo F, Li H, Ma W, Cao J, Chen Q, Lu F, Qiu M, Zhou P, Xia Z, Zeng K, Zhan J, Zhou T, Luo Q, Pan W, Zhang L, Lin C, Huang Y, Zhang L, Yang D, Zhao H. The BCL-2 inhibitor APG-2575 resets tumor-associated macrophages toward the M1 phenotype, promoting a favorable response to anti-PD-1 therapy via NLRP3 activation. Cell Mol Immunol 2024. 21: 60-79.
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July, 2024
Lipton JH. Maximizing the value of chronic myeloid leukemia management using tyrosine kinase inhibitors in the USA: potential determinants and consequences of healthcare resource utilization and costs, with proposed optimization approaches. Clin Drug Investig 2024. 41: 91-108.
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June, 2023
Rej RK, Wang C, Lu J, Wang M, Petrunak E, Zawacki KP, McEachern D, Yang CY, Wang L, Li R, Chinnaswamy K, Wen B, Sun D, Stuckey JA, Zhou Y, Chen J, Tang G, Wang S. Discovery of EEDi-5273 as an exceptionally potent and orally efficacious EED inhibitor capable of achieving complete and persistent tumor regression. J Med Chem 2021. 64: 14540-14556. DOI:10.1021/acs.jmedchem.1c01059.
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June, 2023
Senapati J, Sasaki K, Issa GC, Lipton JH, Radich JP, Jabbour E, Kantarjian HM. Management of chronic myeloid leukemia in 2023 – common ground and common sense. Blood Cancer J 2023. 13: 58. DOI:10.1038/s41408-023-00823-9.
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March, 2023
Zhang X, Xu X, Guan Y, Liang X, Liu H, Liu Z, Huang X, Xu Z, Sun J, Han X, Lu F, Wang P, Wang H, Xu L, Men L, Wang C, Yang D, Zhai Y, Hou J. First-in-human study of APG-1387, targeting inhibitor of apoptosis proteins, for the treatment of patients with chronic hepatitis B. [Oral presentation presented at: AASLD: The Liver Meeting; November 4-8, 2022; Washington, DC]. Hepatology . 76 (suppl 1)
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January, 2023
Zhao H, Chen J, Song Z, Zhao Y, Guo Y, Wu G, Ma Y, Zhou W, Yu X, Gao F, Dong Y, Zhang R, Yang C, Tian X, Wang H, Tu Y, Yu J, Sun X, Zhang L, Zhai Y. First-in-human phase I results of APG-2449, a novel FAK and third-generation ALK/ ROS1 tyrosine kinase inhibitor (TKI), in patients (pts) with second-generation TKI-resistant ALK/ROS1+ non–small cell lung cancer (NSCLC) or mesothelioma. [Poster presented at: 2022 ASCO Annual Meeting; June 3-7, 2022; Chicago, IL]. J Clin Oncol 2022. 40 (suppl 16): 9071. DOI:10.1200/JCO.2022.40.16_suppl.9071.
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January, 2023
Zhang L, Zhao H, Zhao Y, Cheng Y, Cui J, Ma Y, Yang C, Zhang J, Xu L, Yu J, Men L, Liang Z, Yang D, Zhai Y. Updated study results of pelcitoclax (APG-1252) in combination with osimertinib in patients (pts) with EGFR-mutant non–small cell lung cancer (NSCLC). [Poster presented at: 2022 ASCO Annual Meeting; June 3-7, 2022; Chicago, IL]. J Clin Oncol 2022. 40 (suppl 16): 9116. DOI:10.1200/JCO.2022.40.16_suppl.9116.
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January, 2023
Qin A, Kalemkerian GP, Mohindra NA, Patel JD, Karapetis CS, Carlisle JW, Sands J, Spira AI, Gao B, Amin H, Paudyal B, Frank G, Sun X, Xu Y, Wang C, Fu T, Winkler R, Liang Z, Yang D, Zhai Y. First-in-human study of pelcitoclax (APG-1252) in combination with paclitaxel in patients (pts) with relapsed/refractory small-cell lung cancer (R/R SCLC). J Clin Oncol 2022. 40 (suppl 16): e20612. DOI:10.1200/JCO.2022.40.16_suppl.e20612.
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January, 2023
Zhang X, Xu X, Guan Y, Liang X, Liu H, Liu Z, Huang X, Xu Z, Sun J, Han X, Lu F, Wang P, Wang H, Xu L, Men L, Wang C, Yang D, Zhai Y, Hou J. First-in-human study of APG-1387, targeting inhibitor of apoptosis proteins, for the treatment of patients with chronic hepatitis B. [Oral presentation presented at: AASLD: The Liver Meeting; November 4-8, 2022; Washington, DC]. Hepatology 2022. 76 (suppl 1): S30-S31. DOI:10.1002/hep.32697.
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January, 2023
Zhu S, Fang DD, Li Q, Yang D, Gu S, Wang S, Yang D, Zhai Y. Preclinical development of embryonic ectoderm development (EED) inhibitor APG-5918/EEDi-5273 for cancer therapy. [Poster presented at: AACR Annual Meeting 2022; April 8-13, 2022; New Orleans, LA]. Cancer Res 2022. 82 (suppl 12): 3939. DOI:10.1158/1538-7445.AM2022-3939.
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January, 2023
Tao R, Fang DD, Li Y, Zhai G, Zhou F, Wang Q, Deng J, Yang D, Zhai Y. FAK inhibitor APG-2449 and CDK4/6 inhibitor palbociclib synergistically suppress mesothelioma tumor growth via autophagy induction. [Poster presented at: AACR Annual Meeting 2022; April 8-13, 2022; New Orleans, LA]. Cancer Res 2022. 82 (suppl 12): 2563. DOI:10.1158/1538-7445.AM2022-2563.
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January, 2023
Gu S, Li Q, Li C, Wang Q, Fang DD, Wang S, Yang D, Zhai Y. Development of covalent KRASG12C inhibitor APG-1842 for the treatment of solid tumors. [Poster presented at: AACR Annual Meeting 2022; April 8-13, 2022; New Orleans, LA]. Cancer Res 2022. 82 (suppl 12): 2664. DOI:10.1158/1538-7445.AM2022-2664.
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January, 2023
Wang G, Liang E, Min P, Ge Y, Wu B, Yu H, Yang D, Zhai Y. MDM2-p53 inhibitor alrizomadlin (APG-115) enhances antitumor activity of pomalidomide in multiple myeloma (MM). [Poster presented at: the 64th ASH Annual Meeting and Exposition; December 10-13, 2022; New Orleans, LA]. Blood 2022. 140 (suppl 1): 9953-9954. DOI:10.1182/blood-2022-162666.
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January, 2023
Kadia TM, Benton C, Erba HP, Gandhi M, Levy MY, Percival ME M, Ulrickson M, Yimer H, Yu M, Chen Z, Wang J, Li M, Ahmad M, Yang D, Zhai Y. Trial in progress: Phase 1b/2 study of alrizomadlin (APG-115), alone or combined with 5-azacitidine (AZA), in patients with relapsed/refractory acute myeloid leukemia (AML), chronic myelomonocytic leukemia (CMML), or myelodysplastic syndrome (MDS). Blood 2022. 140 (suppl 1): 11659-11660. DOI:10.1182/blood-2022-162627.
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January, 2023
McKean M, Tolcher AW, Reeves JA, Chmielowski B, Shaheen MF, Beck JT, Orloff MM, Somaiah N, Van Tine BA, Drabick JJ, Spira AI, O'Byrne K, Karapetis CS, Foresto SA, Movva S, Martinez J, Li M, Winkler R, Yang D, Zhai Y. Newly updated activity results of alrizomadlin (APG-115), a novel MDM2/p53 inhibitor, plus pembrolizumab: Phase 2 study in adults and children with various solid tumors. [Poster presented at: 2022 ASCO Annual Meeting; June 3-7, 2022; Chicago, IL]. J Clin Oncol 2022. 40 (suppl 16): 9517. DOI:10.1200/JCO.2022.40.16_suppl.9517.
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January, 2023
Pearson AT, Muzaffar J, Bellile E, Worden FP, Chung CH, Rosenberg A, Vokes E, Fidler MJ, Brenner JC, Zhai Y, Fu T, Winkler R, Swiecicki P. Phase I/II study of a novel MDM-2 inhibitor (APG-115) in TP53 wild type salivary gland cancers. [Poster presented at: the 34th EORTC-NCI-AACR Symposium; October 26-28, 2022; Barcelona, Spain]. Eur J Cancer 2022. 174 (suppl 1): S79-S80. DOI:10.1016/S0959-8049(22)01011-5.
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January, 2023
Wang G, Liang E, Tang C, Rui L, Min P, Lv J, Ge Y, Zhang F, Wang L, Shang J, Yang D, Zhai Y. MDM2 inhibitor alrizomadlin (APG-115) stabilizes p53 and synergizes with proteasome inhibitors in multiple myeloma. [Poster presented at: AACR Annual Meeting 2022; April 8-13, 2022; New Orleans, LA]. Cancer Res 2022. 82 (suppl 12): 5439. DOI:10.1158/1538-7445.AM2022-5439.
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January, 2023
Tang Q, Fang DD, Yu H, Wu B, Yin Y, Yang D, Zhai Y. Inhibition of MDM2-p53 interaction by alrizomadlin (APG-115) induces pyroptotic cell death in gasdermin E (GSDME)-expressing cancer cells. [Poster presented at: AACR Annual Meeting 2022; April 8-13, 2022; New Orleans, LA] . Cancer Res 2022. 82 (suppl 12): 2998. DOI:10.1158/1538-7445.AM2022-2998.
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January, 2023
Zhang Y, Chen W, Pathak A, Yang Y, Yang D, Zhai Y. Disease burden of chronic myeloid leukemia (CML) treatment failure in mainland China: a systematic literature review. [Poster presented at: Virtual ISPOR Europe 2021, Virtual Scientific Program; November 30-December 3, 2021]. Value in Health 2022. 25 (suppl 1): S32. DOI:10.1016/j.jval.2021.11.146.
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January, 2023
Zhang Y, Chen W, Xu Y, Pathak A, Lu Y, Yang D, Zhai Y. Impact of nilotinib reimbursement coverage on the use of tyrosine kinase inhibitors (TKI) for chronic myeloid leukemia (CML) in Chinese tertiary care hospitals: a retrospective analysis. [Poster presented at: ISPOR 2022, Virtual Scientific Program; May 15-18, 2022]. Value in Health 2022. 25 (suppl 7): S474. DOI:10.1016/j.jval.2022.04.971.
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January, 2023
Zhang Y, Chen W, Xu Y, Pathak A, Yang Y, Yang D, Zhai Y. Impact of an imatinib volume-based purchase policy (VBP) on the use of tyrosine kinase inhibitors (TKI) for chronic myeloid leukemia (CML) in Chinese tertiary care hospitals: a retrospective analysis. [Poster presented at: ISPOR 2022, Virtual Scientific Program; May 15-18, 2022]. Value in Health 2022. 25 (suppl 7): S477. DOI:10.1016/j.jval.2022.04.987.
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January, 2023
Jiang Q, Li Z, Qin Y, Hu Y, Li W, Liu X, Xu N, Zhang Y, Song Y, Meng L, Hong Z, Liu B, Li Y, Chen S, Xue M, Zhu H, Li H, Du X, Lou J, Zhang X, Liang Y, Dai YJ, Chen Z, Niu Q, Men L, Yang D, Zhai Y, Huang XJ. A five-year follow-up on safety and efficacy of olverembatinib (HQP1351), a novel third-generation BCR-ABL tyrosine kinase inhibitor (TKI), in patients with TKI-resistant chronic myeloid leukemia (CML) in China. [Oral presentation presented at: the 64th ASH Annual Meeting and Exposition; December 10-13, 2022; New Orleans, LA]. Blood 2022. 140 (suppl 1): 198-199. DOI:10.1182/blood-2022-170868.
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January, 2023
Jiang Q, Li Z, Hou Y, Hu Y, Li W, Liu X, Xu N, Zhang Y, Song Y, Meng L, Hong Z, Liu B, Li Y, Chen S, Xue M, Zhu H, Li H, Du X, Lou J, Zhang X, Liang Y, Dai YJ, Chen Z, Niu Q, Men L, Yang D, Zhai Y, Huang XJ. Updated results of pivotal phase 2 trials of olverembatinib (HQP1351) in patients (Pts) with tyrosine kinase inhibitor (TKI)-resistant chronic- and accelerated-phase chronic myeloid leukemia (CML-CP and CML-AP) with T315I mutation. [Oral presentation presented at: the 64th ASH Annual Meeting and Exposition; December 10-13, 2022; New Orleans, LA]. Blood 2022. 140 (suppl 1): 203-204. DOI:10.1182/blood-2022-170698.
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January, 2023
Jabbour E, Koller PB, Oehler VG, Jamy OH, Mukherjee S, Hunter AM, Baer MR, Beck JT, Chen Z, Guo H, Fu L, Men L, Wang H, Yang D, Zhai Y, Kantarjian H, Jiang L, Wang C. Olverembatinib (HQP1351) overcomes ponatinib resistance in patients with heavily pretreated/refractory chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). [Oral presentation presented at: the 64th ASH Annual Meeting and Exposition; December 10-13, 2022; New Orleans, LA]. Blood 2022. 140 (suppl 1): 200-202. DOI:10.1182/blood-2022-162387.
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January, 2023
Qiu H, Zhou Z, Zhou Y, Wan X, Tao K, Li Y, Wu X, Liu L, Chen Z, Men L, Liang Z, Lu M, Jiang L, Yang D, Xu RH, Zhai Y. Promising antitumor activity of olverembatinib (HQP1351) in patients (pts) with tyrosine kinase inhibitor- (TKI-) resistant succinate dehydrogenase- (SDH-) deficient gastrointestinal stromal tumor (GIST). [Poster discussion presented at: 2022 ASCO Annual Meeting; June 3-7, 2022; Chicago, IL]. J Clin Oncol 2022. 40 (suppl 16): 11513. DOI:10.1200/JCO.2022.40.16_suppl.11513.
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January, 2023
Sun M, Qi J, Song Y, Zhou K, Liu H, Shen A, Geng L, Zhou F, Huang J, Chen Z, Zhang H, Lu M, Ahmad M, Men L, Yang D, Zhai Y, Wang J. Preliminary results of a phase 1 study of novel BCL-2 inhibitor lisaftoclax (APG-2575) in Chinese patients (pts) with relapsed or refractory (R/R) non-Hodgkin lymphomas (NHLs). [Poster presented at: the 30th European Hematology Association Hybrid; June 9-12, 2022]. HemaSphere 2022. 6: 996-997. DOI:10.1097/01.HS9.0000847292.19961.d6.
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January, 2023
Davids MS, Chanan-Khan A, Mudenda B, Nogaieva L, Kriachok I, Usenko H, Ivanov V, Kyselova O, Perekhrestenko T, Muzhychuk I, Myasnikov A, Maslyak Z, Proidakov A, Uspenskaya O, Borisenkova E, Marlton P, Siddiqi T, Winter A, Lysa T, Bakirov B, Fu L, Chen Z, Yu M, Li M, Glass L, Ahmad M, Karpenko O, Osipov I, De A, Paudyal B, Wang H, Winkler R, Gabrail N, Ganju V, Konstantinova TS, Samoylova OS, Yang D, Zhai Y. Lisaftoclax (APG-2575) safety and activity as monotherapy or combined with acalabrutinib or rituximab in patients (pts) with treatment-naïve, relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (R/R CLL/SLL): initial data from a phase 2 global study. [Oral presentation presented at: the 64th ASH Annual Meeting and Exposition; December 10-13, 2022; New Orleans, LA]. Blood 2022. 140 (suppl 1): 2326-2328. DOI:10.1182/blood-2022-160386 .
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January, 2023
Kalinsky K, Tolcher AW, Wang S, Meric-Bernstam F, Winkler R, Li M, Sun X, Pan W, Paudyal B, Liang Z, Lu M, Yang D, Zhai Y. Phase 1b/2 study of BCL-2 inhibitor lisaftoclax (APG-2575) safety and tolerability when administered alone or combined with a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor in patients with estrogen receptor-positive (ER⁺) breast cancer or advanced solid tumors. [Poster presented at: 2022 ASCO Annual Meeting; June 3-7, 2022; Chicago, IL]. J Clin Oncol 2022. 40 (suppl 16): TPS1122. DOI:10.1200/JCO.2022.40.16_suppl.TPS1122.
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January, 2023
Li J, Zhou K, Nian W, Cui G, Wang J, Zhang X, Cen H, Li F, Yi S, Feng R, Xu C, Qian W, Liu L, Li C, Zhao X, Chen Z, Qiao J, Zhang H, Ahmad M, Zhai Y. A phase Ib/II study of lisaftoclax (APG-2575), a novel BCL-2 inhibitor (BCL-2i), in patients (pts) with relapsed/refractory chronic lymphocytic leukemia or small lymphocytic lymphoma (R/R CLL/SLL). [Poster presented at: 2022 ASCO Annual Meeting; June 3-7, 2022; Chicago, IL]. J Clin Oncol 2022. 40 (suppl 16): 7543. DOI:10.1200/JCO.2022.40.16_suppl.7543.
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January, 2023
Deng J, Zhang K, Tang Q, Huang X, Wang Q, Li N, Fang DD, Yang D, Zhai Y. Co-targeting MDM2-p53 and BCL-2 apoptosis pathways overcomes resistance conferred by acquired BCL-2 gene mutations in preclinical models. Cancer Res 2022. 82(suppl 12): 3964. [2022 AACR poster presentation].
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January, 2023
Zhai Y, Tang Q, Fang D, Deng J, Zhang K, Wang Q, Yin Y, Fu C, Xue SL, Li N, Zhou F, Yang D. Lisaftoclax in combination with alrizomadlin overcomes venetoclax resistance in acute myeloid leukemia and acute lymphoblastic leukemia: preclinical studies. Clin Cancer Res 2023. 29: 183-196.
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January, 2023
Yao W, Bai L, Wang S, Zhai Y, Sun SY. Mcl-1 levels critically impact the sensitivities of human colorectal cancer cells to APG-1252-M1, a novel Bcl-2/Bcl-XL dual inhibitor that induces Bax-dependent apoptosis. Neoplasia 2022. 22: 100798. DOI:10.1016/j.neo.2022.100798.
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January, 2023
Selt F, Sigaud R, Valinciute G, Sievers P, Zaman J, Alco C, Schmid S, Peterziel H, Tsai JW, Guiho R, Martínez-Barbera JP, Pusch S, Deng J, Zhai Y, van Tilburg CM, Schuhman MU, Damaty AEL, Bandopadhayay P, Herold-Mende C, von Deimling A, Pfister SM, Montero J, Capper D, Oehme I, Sahm F, Jones DTW, Witt O, Milde T. BH3 mimetics targeting BCL-XL impact the senescent compartment of pilocytic astrocytoma. Neuro-Oncol 2022. DOI:10.1093/neuonc/noac199.
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January, 2023
Qian L, Vallega KA, Yao W, Wang D, Zhai Y, He X, Sunet SY. Therapeutic potential of the novel Bcl-2/Bcl-XL dual inhibitor, APG1252, alone or in combination against non-small cell lung cancer. Mol Carcinog 2022. 61: 1031-1042. DOI:10.1002/mc.23458.
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January, 2023
Ma G, Deng Y, Qian L, Vallega KA, Zhang G, Deng X, Owonikoko TK, Ramalingam SS, Fang DD, Zhai Y, Sun SY. Overcoming acquired resistance to third-generation EGFR inhibitors by targeting activation of intrinsic apoptotic pathway through Mcl-1 inhibition, Bax activation, or both. Oncogene 2022. 41: 1691-1700. DOI:10.1038/s41388-022-02200-5.
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January, 2023
Fang DD, Tao R, Wang G, Li Y, Zhang K, Xu C, Zhai G, Wang Q, Wang J, Tang C, Min P, Xiong D, Chen J, Wang S, Yang D, Zhai Y. Discovery of a novel ALK/ROS1/FAK inhibitor, APG-2449, in preclinical non-small cell lung cancer and ovarian cancer models. BMC Cancer 2022. 22: 752. DOI:10.1186/s12885-022-09799-4.
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January, 2023
Wei W, Huang S, Ling Q, Mao S, Qian Y, Ye W, Li F, Pan J, Lin X, Huang J, Huang X, Zhai Y, Sun J, Jin J. Homoharringtonine is synergistically lethal with BCL-2 inhibitor APG-2575 in acute myeloid leukemia. J Transl Med 2022. 20: 299. DOI:10.1186/s12967-022-03497-2.
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January, 2023
Deng J, Paulus A, Fang DD, Manna A, Wang G, Wang H, Zhu S, Chen J, Min P, Yin Y, Dutta N, Halder N, Ciccio G, Copland JA, Miller J, Han B, Bai L, Liu L, Wang M, McEachern D, Przybranowski S, Yang CY, Stuckey JA, Wu D, Li C, Ryan J, Letai A, Ailawadhi S, Yang D, Wang S, Chanan-Khan A, Zhai Y. Lisaftoclax (APG-2575) is a novel BCL-2 inhibitor with robust antitumor activity in preclinical models of hematologic malignancy. Clin Cancer Res 2022. 28: 5455-5468. DOI:10.1158/1078-0432.CCR-21-4037.
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January, 2023
Zhang Y, Chen W, Pathak A, Yang Y, Yang D, Zhai Y. Burden of tyrosine kinase inhibitor failure in Chinese chronic myeloid leukemia patients: a systematic literature review. J Comp Eff Res 2022. 11: 621-637. DOI:10.2217/cer-2022-0032.
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January, 2023
Yu Z, Lei Z, Yao X, Wang H, Zhang M, Hou Z, Li Y, Zhao Y, Li H, Liu D, Zhai Y. Potential drug-drug interaction of olverembatinib (HQP1351) using physiologically based pharmacokinetic models. Front Pharmacol 2022. 13: 1065130. DOI:10.3389/fphar.2022.1065130.
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January, 2023
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October, 2021
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June, 2021
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June, 2021
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June, 2021
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June, 2021
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May, 2021
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April, 2021
Tao R, Fang DD, Li Y, et al. Focal adhesion kinase (FAK) inhibitor APG-2449 sensitizes ovarian tumors to chemotherapy via CD44 downregulation. The American Association for Cancer Research Annual Meeting 2021. Cancer Res 2021;81 (13_Supplement): Abstract 968. April 10-15 and May 17-21, 2021 (Virtual). DOI:https://doi.org/10.1158/1538-7445.AM2021-968.
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April, 2021
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April, 2021
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April, 2021
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April, 2021
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April, 2021
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April, 2021
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June, 2017
Wang G, et al. APG-1252-12A induces mitochondria-dependent apoptosis through inhibiting the antiapoptotic proteins BCL-2/BCL-xl in HL-60 cells. Int J Oncol 2017. 51 563-572. DOI:10.3892/ijo.2017.4028.
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April, 2017
Chen H, et al. Restoration of p53 using the novel MDM2-p53 antagonist APG115 suppresses dedifferentiated papillary thyroid cancer cells. Oncotarget 2017. 8 43008-43022. DOI:10.18632/oncotarget.17398.
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March, 2017
Aguilar A, et al. Discovery of 4‑((32R,42S,52R)‑63-Chloro-42-(3-chloro-2-ﬂuorophenyl)12-ethyl-23-oxodispiro[cyclohexane-1,22-pyrrolidine-3′,33-indoline]52-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG115): a potent and orally active murine double minute 2 (MDM2) inhibitor in clinical development. J Med Chem March 24, 2017. 60 2819-2839. DOI:10.1021/acs.jmedchem.6b01665.
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October, 2016
Li N, et al. A novel Smac mimetic APG-1387 demonstrates potent antitumor activity in nasopharyngeal carcinoma cells by inducing apoptosis. Cancer Lett 2016. 10: 14-22.
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November, 2014
Lu J, Sheng R, Sun H, et al. A potent and highly efficacious bivalent Smac mimetic APG-1387 in phase I clinical development. 26th EORTC-NCI-AACR Symposium. . Poster 268
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November, 2014
Bai L, Chen L, Liu L, et al. BM-1252 (APG-1252): a potent dual speciﬁc Bcl-2/Bcl-xL inhibitor that achieves complete tumor regression with minimal platelet toxicity. Eur J Cancer 2014:50:109-10 November 01, 2014. Poster 338
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November, 2014
Wang H, et al. Preclinical studies of a dual BCL-2/BCL-XL inhibitor APG-1252 with strong anti-tumor efficacy and significantly reduced platelet toxicity. Abstract 544. Eur J Cancer 2014. 50(Suppl 6) 176-177. DOI:10.1016/S0959-8049(14)70670-7.
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November, 2014
Bai L, et al. BM-1252 (APG-1252): a potent dual speciﬁc BCL-2/BCL-XL inhibitor that achieves complete tumor regression with minimal platelet toxicity. Poster 338. Eur J Cancer 2014. 50 109-110. DOI:10.1016/S0959-8049(14)70464-2 .
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January, 2013
Ren X, et al. Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region‒Abelson (BCR-ABL) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. J Med Chem 2013. 56 879-894. DOI:10.1021/jm301581y.
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