Olverembatinib for the treatment of chronic myeloid leukemia in chronic phase. Ann Blood . 2024;9: 27.
. ViewOlverembatinib (HQP1351) overcomes ponatinib and/or asciminib resistance in patients with heavily pretreated/refractory chronic myeloid leukemia (CML). Oral presentation presented at: 2024 ESH John Goldman Conference on Chronic Myeloid Leukemia; September 27-29, 2024; Prague, Czech Republic. .
. ViewOlverembatinib (HQP1351) overcomes ponatinib and/or asciminib resistance in patients with heavily pretreated/refractory chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Clin Lymphoma Myeloma Leuk . 2024;24(suppl 1): S371. [Poster presented at: SOHO 2024 Annual Meeting; September 4-7, 2024; Houston, TX].
. View1722MO: Updated efficacy results of olverembatinib (HQP1351) in patients with succinate dehydrogenase (SDH)-deficient gastrointestinal stromal tumors (GIST) and potential mechanisms of action (MOA). Ann Oncol . 2024;35(suppl 2): S1032. [Mini oral presentation presented at: ESMO Congress 2024; September 13-17, 2024; Barcelona, Spain].
. ViewP1550: Embryonic ectoderm development (EED) inhibitor APG-5918 improves chronic kidney disease- (CKD)-induced hemoglobin (Hb) insufficiency in preclinical models of anemia. HemaSphere . 2024;8(suppl 1): 2869-2870. [Poster presented at: 2024 EHA Congress; June 13-16, 2024; Madrid, Spain].
. ViewP722: Olverembatinib overcomes ponatinib and asciminib resistance in patients (pts) with heavily pretreated chronic myeloid leukemia (CML) and Philadelphia-positive acute lymphoblastic leukemia (Ph⁺ ALL). HemaSphere . 2024;8(suppl 1): 1255-1256. [Poster presented at: 2024 EHA Congress; June 13-16, 2024; Madrid, Spain].
. ViewP917: Lisaftoclax (APG-2575) combined with novel therapeutic regimens in patients (pts) with relapsed or refractory (R/R) multiple myeloma (MM) or immunoglobulin light-chain (AL) amyloidosis. HemaSphere . 2024;8(suppl 1): 1623-1624. [Poster presented at: 2024 EHA Congress; June 13-16, 2024; Madrid, Spain].
. ViewSafety and efficacy of lisaftoclax, a novel BCL-2 inhibitor, in combination with azacitidine in patients with treatment-naïve or relapsed or refractory acute myeloid leukemia. J Clin Oncol . 2024;42(suppl 16): 6541. [Poster presented at: 2024 ASCO Annual Meeting; May 31 - June 4, 2024; Chicago, IL].
. ViewUpdated efficacy results of olverembatinib (HQP1351) in patients with tyrosine kinase inhibitor (TKI)-resistant succinate dehydrogenase (SDH)-deficient gastrointestinal stromal tumors (GIST) and paraganglioma. J Clin Oncol . 2024;42(suppl 16): 11502. [Oral presentation presented at: 2024 ASCO Annual Meeting; May 31 - June 4, 2024; Chicago, IL] .
. ViewUpdated study results of novel FAK/ALK/ROS1 inhibitor APG-2449 in patients (pts) with non-small-cell lung cancer (NSCLC) resistant to second-generation ALK inhibitors. J Clin Oncol . 2024;42(suppl 16): 3124. [Poster presented at: 2024 ASCO Annual Meeting; May 31 - June 4, 2024; Chicago, IL].
. ViewUpdated efficacy and safety results of BCL-2 inhibitor lisaftoclax (APG-2575) alone or combined with ibrutinib or rituximab in patients (pts) with Waldenström macroglobulinemia (WM). J Clin Oncol . 2024;42(suppl 16): 7078. [Poster presented at: 2024 ASCO Annual Meeting; May 31 - June 4, 2024; Chicago, IL].
. ViewAbstract 4569. APG-2449, a novel focal adhesion kinase (FAK) inhibitor, inhibits metastasis and enhances the antitumor efficacy of PEGylated liposome doxorubicin (PLD) in epithelial ovarian cancer (EOC). Cancer Res . 2024;84 (suppl 6): 4569. [Poster presented at: AACR Annual Meeting 2024; April 5-10, 2024; San Diego, CA].
. ViewAbstract 3223: Embryonic ectoderm development (EED) inhibitor APG-5918 (EEDi-5273) and MDM2 inhibitor alrizomadlin (APG-115) synergistically inhibit tumor growth in preclinical models of prostate cancer (PCa). Cancer Res . 2024;84(suppl 6): 3223. [Poster presented at: AACR Annual Meeting 2024; April 5-10, 2024; San Diego, CA].
. ViewAbstract 1971. Olverembatinib, a novel multikinase inhibitor, demonstrates superior antitumor activity in succinate dehydrogenase (SDH)-deficient neoplasms. Cancer Res . 2024; 2024;84(suppl 6): 1971. [Poster presented at: AACR Annual Meeting 2024; April 5-10, 2024; San Diego, CA].
. ViewPharmacotherapy and cardiovascular challenges: a case report of olverembatinib-induced myocardial infarction with non-obstructive coronary arteries. BMC Cardiovasc Disord . 2024;24 332.
. ViewPharmacokinetics of olverembatinib (HQP1351) in the presence of a strong CYP3A4 inhibitor (itraconazole) or inducer (rifampin) in healthy volunteers. Clin Transl Sci . 2024;17: e70021.
. ViewOlverembatinib combined with inotuzumab ozogamicin in relapsed refractory Philadelphia chromosome-positive acute lymphoblastic leukemia: A case report. Medicine (Baltimore) 2024. 103: e38985.
. ViewOlverembatinib for myeloid/lymphoid neoplasm associated with eosinophilia and FGFR1 rearrangement. Leuk Lymphoma 2023. 64: 1605-1610.
. ViewDetermination of olverembatinib in human plasma and cerebrospinal fluid by an LC-MS/MS method: validation and clinical application. J Pharm Biomed Anal 2023. 230: 115382.
. ViewOlverembatinib Treatment in Pediatric Patients With Relapsed Philadelphia-Chromosome-Positive Acute Lymphoblastic Leukemia. Lymphoma Myeloma Leuk 2023. 23: 660-666.
. ViewNovel third-generation tyrosine kinase inhibitor for newly diagnosed Philadelphia chromosome-positive acute lymphoblastic leukemia: a case study. Anticancer Drugs 2023. 34: 599-604.
. ViewCase report: Olverembatinib monotherapy: the chemotherapy-free regimen for an elderly patient with relapsed Ph-positive acute lymphoblastic leukemia. Front Pharmacol 2023. 14: 1320641.
. ViewOlverembatinib in relapsed Philadelphia chromosome-positive B-cell acute lymphoblastic leukemia: a study of 5 cases. Leuk Lymphoma 2023. 64: 1208-1211.
. ViewA novel small molecule inhibitor of MDM2-p53 (APG-115) enhances radiosensitivity of gastric adenocarcinoma. J Exp Clin Cancer Res 2018. 37: 97.
. ViewEEDi-5285: An exceptionally potent, efficacious, and orally active small-molecule inhibitor of embryonic ectoderm development. J Med Chem 2020. 63: 7252-7267.
. ViewA 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.
. ViewNovel 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.
. ViewFirst-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.
. ViewA first-in-human phase I study of a novel MDM2/p53 inhibitor alrizomadlin in advanced solid tumors. ESMO Open 2024. 9: 103636.
. ViewManagement of chronic myeloid leukemia in 2023 – common ground and common sense. Blood Cancer J 2023. 13: 58. DOI:10.1038/s41408-023-00823-9.
. ViewFirst-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)
. ViewFirst-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.
. ViewUpdated 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.
. ViewFirst-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.
. ViewFirst-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.
. ViewPreclinical 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.
. ViewFAK 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.
. ViewDevelopment 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.
. ViewMDM2-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.
. ViewTrial 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.
. ViewNewly 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.
. ViewPhase 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.
. ViewMDM2 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.
. ViewInhibition 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.
. ViewDisease 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.
. ViewImpact 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.
. ViewImpact 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.
. ViewA 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.
. ViewUpdated 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.
. ViewOlverembatinib (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.
. ViewPromising 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.
. ViewPreliminary 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.
. ViewLisaftoclax (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 .
. ViewPhase 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.
. ViewA 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.
. ViewCo-targeting MDM2-p53 and BCL-2 apoptosis pathways overcomes resistance conferred by acquired BCL-2 gene mutations in preclinical models. [Poster presented at: AACR Annual Meeting 2022; April 8-13, 2022; New Orleans, LA]. Cancer Res 2022. 82 (suppl 12): 3964. DOI:10.1158/1538-7445.AM2022-3964.
. ViewTherapeutic 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.
. ViewHomoharringtonine 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.
. ViewLisaftoclax (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.
. ViewBurden 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.
. ViewPotential drug-drug interaction of olverembatinib (HQP1351) using physiologically based pharmacokinetic models. Front Pharmacol 2022. 13: 1065130. DOI:10.3389/fphar.2022.1065130.
. ViewOlverembatinib inhibits SARS-CoV-2-Omicron variant-mediated cytokine release. EMBO Mol Med 2022. 14: e15919. DOI:10.15252/emmm.202215919.
. ViewOlverembatinib: First Approval. Drugs 2022. 82: 469-475. DOI:10.1007/s40265-022-01680-9.
. ViewAntitumor Activity of Dual BCL-2/BCL-Xl Inhibitor Pelcitoclax (APG-1252) in Natural Killer/T-Cell Lymphoma (NK/TCL). American Society of Hematology Annual Meeting 2021. Blood 2021; 138 (Supplement 1): 2062 December 11-14, 2021. DOI:doi: https://doi.org/10.1182/blood-2021-152207.
. ViewUpdated 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). American Society of Hematology annual meeting 2021. Blood 2021; 138 (Supplement 1): 3598 December 11-14, 2021. DOI:doi: https://doi.org/10.1182/blood-2021-153937.
. ViewUpdated 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). American Society of Hematology annual meeting 2021. Blood 2021; 138 (Supplement 1): 311 December 11-14, 2021. DOI:doi: https://doi.org/10.1182/blood-2021-153065.
. ViewTrial 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.
. ViewA 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). American Society of Hematology annual meeting 2021. Blood 2021; 138 (Supplement 1): 3730. December 11-14, 2021. DOI:doi: https://doi.org/10.1182/blood-2021-152235.
. ViewA 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). American Society of Hematology annual meeting 2021. Blood 2021; 138 (Supplement 1): 3730 December 11-14, 2021. DOI:doi: https://doi.org/10.1182/blood-2021-152235.
. ViewTrial 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). American Society of Hematology annual meeting 2021. Blood 2021; 138 (Supplement 1): 1554 December 11-14, 2021. DOI:doi: https://doi.org/10.1182/blood-2021-152811.
. ViewTrial 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).. Presented at the Society for Immunotherapy of Cancer annual meeting 2021 Journal for ImmunoTherapy of Cancer 2021. . 9: Abstract 445 DOI:doi: 10.1136/jitc-2021-SITC2021.445.
. ViewTrial 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.. Presented at the Society for Immunotherapy of Cancer annual meeting 2021. Journal for ImmunoTherapy of Cancer 2021 November 10-14, 2021. 9: Abstract 450
. ViewTrial 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 (Supplement 1): 4764 November 5, 2021. DOI:doi: https://doi.org/10.1182/blood-2021-151631.
. ViewCollaborative crosstalk between two apoptosis pathways drives synergy of dual inhibition of BCL-2/MDM2 in preclinical models of neuroblastoma [abstract]. AACR-NCI-EORTC Virtual International Conference on Molecular Targets and Cancer Therapeutics. Mol Cancer Ther 2021;20(12 Suppl):Abstract nr P209 Oct 7-10, 2021. DOI:https://doi.org/10.1158/1535-7163.TARG-21-P209.
. ViewSynergistic 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 [abstract]. AACR-NCI-EORTC Virtual International Conference on Molecular Targets and Cancer Therapeutics. Mol Cancer Ther 2021; 20(12 Suppl): Abstract nr P208. Oct 7-10, 2021. DOI:https://doi.org/10.1158/1535-7163.TARG-21-P208.
. ViewPhase 1b Study of Pelcitoclax (APG-1252) in combination with osimertinib in patients with EGFR TKI-resistant NSCLC Virtual. 2021 World Conference on Lung Cancer. Journal of Thoracic Oncology 2021 September 8-14, 2021. DOI:https://doi.org/10.1016/j.jtho.2021.08.115.
. ViewTrial 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. Presented at the American Society of Clinical Oncology (ASCO) annual meeting 2021. Journal of Clinical Oncology June 4-8, 2021. 39, no. 15_suppl: Abstract TPS6094
. ViewPreliminary results of a phase II study of alrizomadlin (APG-115), a novel, small-molecule MDM2 inhibitor, in combination with pembrolizumab in patients (pts) with unresectable or metastatic melanoma or advanced solid tumors that have failed immuno-oncologic (I-O) drugs. Oral presentation. Presented at the American Society of Clinical Oncology (ASCO) annual meeting 2021. Journal of Clinical Oncology June 4-8, 2021. no. 15_suppl: Abstract 2506 DOI:DOI: 10.1200/JCO.2021.39.15_suppl.2506.
. ViewTrial 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). American Society of Clinical Oncology (ASCO) annual meeting 2021. Journal of Clinical Oncology 39, no. 15_suppl: Abstract TPS8589 June 4-8, 2021.
. ViewFirst-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). American Society of Clinical Oncology (ASCO) annual meeting 2021. Journal of Clinical Oncology 39, no. 15_suppl: Abstract 7502 June 4-8, 2021. DOI:DOI: 10.1200/JCO.2021.39.15_suppl.7502.
. ViewMDM2 inhibitor APG-115 exerts potent antitumor activity and synergizes with standard-of-care agents in preclinical acute myeloid leukemia models. Cell Death Discovery 2021. 7: 90. DOI:10.1038/s41420-021-00465-5.
. ViewFocal 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.
. ViewTherapeutic potential of inhibitor of apoptosis protein (IAP) inhibitor APG-1387 combined with DR5 agonist monoclonal antibody (mAb) CTB-006 in preclinical models of solid tumors.. The American Association for Cancer Research Annual Meeting 2021. Cancer Res 2021;81(13_Suppl): Abstract 1924 April 10-15 and May 17-21, 2021 (Virtual). DOI:https://doi.org/10.1158/1538-7445.AM2021-1924.
. ViewTargeting BCL-xL addiction with APG-1252 (pelcitoclax) to overcome apoptotic blockade in neuroendocrine neoplasm (NEN). American Association for Cancer Research Annual Meeting 2021. Cancer Res 2021;81(13_Suppl): Abstract 984 April 10-15 and May 17-21, 2021 (Virtual). DOI:https://doi.org/10.1158/1538-7445.AM2021-984.
. ViewATP-site inhibitor olverembatinib, HQP1351, enhanced the effect of allosteric inhibitor on the resistance conferred by the compound mutations of BCR-ABL. American Association for Cancer Research Annual Meeting 2021. Cancer Res 2021;81 (13_Supplement): Abstract 1463 April 10-15 and May 17-21, 2021 (Virtual). DOI:https://doi.org/10.1158/1538-7445.AM2021-1463.
. ViewFMS-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). American Association for Cancer Research Annual Meeting 2021. Cancer Res 2021;81 (13_Supplement): Abstract 1096 April 10-15 and May 17-21, 2021 (Virtual). DOI:https://doi.org/10.1158/1538-7445.AM2021-1096.
. ViewBCL-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) [abstract]. American Association for Cancer Research Annual Meeting 2021. Cancer Res 2021;81(13_Suppl): Abstract nr 981 Apr 10-15 and May 17-21, 2021. DOI:https://doi.org/10.1158/1538-7445.AM2021-981.
. ViewInhibition of BCL-2 (by APG-2575) and CDK4/6 synergistically induces cell cycle arrest and apoptosis in ER+ breast cancer [abstract]. American Association for Cancer Research Annual Meeting 2021. Cancer Res 2021;81(13_Suppl):Abstract nr 976. Apr 10-15 and May 17-21, 2021 . DOI:https://doi.org/10.1158/1538-7445.AM2021-976 .
. ViewA phase Ib/II study of APG-115 in combination with pembrolizumab in patients with unresectable or metastatic melanomas or advanced solid tumors. Abstract 20. Ann Oncol 2019. 30 (Supplement 1) i2-i3. DOI:10.1093/annonc/mdz027.
. ViewAn updated safety and efficacy results of phase 1 study of HQP1351, a novel 3rd- generation of BCR-ABL tyrosine kinase inhibitor (TKI), in patients with TKI-resistant chronic myeloid leukemia. American Society of Hematology Annual Meeting. Blood 2019; 134 (Supplement_1): 493. December 8, 2019. Abstract 493 DOI:doi: https://doi.org/10.1182/blood-2019-124295.
. ViewPhase I study of a novel Bcl-2 inhibitor, AT-101 in combination with lenalidomide and dexamethasone in patients with relapsed and/or refractory multiple myeloma (RRMM). American Society of Hematology Annual Meeting. Blood 2019; 134 (Supplement_1): 3137 December 8, 2019. Abstract 3137 DOI:doi: https://doi.org/10.1182/blood-2019-128610.
. ViewMDM2 inhibitor APG-115 synergizes with PD-1 blockade through enhancing antitumor immunity in the tumor microenvironment. J Immunother Cancer November 28, 2019. 7 327. DOI:10.1186/s40425-019-0750-6.
. ViewA novel BCL-2/BCL-Xl dual inhibitor overcomes ibrutinib-resistance conferred by the upregulation of integrin pathway and BCL-Xl. Blood 2019;134(Supplement 1): 2573 November 13, 2019. Abstract 2573
. ViewThe inhibition of MDM2 by new antagonist APG-115 triggers apoptosis in p53 wild-type cancer cells in both in vitro and in vivo models. New Horizons in Cancer Research: Delivering Cures Through Cancer Science (AACR). . Poster presentation #2017
. ViewBCL-2 selective inhibitor APG-2575 synergizes with BTK inhibitor in preclinical xenograft models of follicular lymphoma and diffuse large B-cell lymphoma. Proceedings of the American Association for Cancer Research Annual Meeting 2019; March 29 to April 3, 2019; Atlanta, GA USA. Cancer Res 2019. 79(13 Suppl): Abstract 2058. DOI:10.1158/1538-7445.AM2019-2058 .
. ViewA novel BCL-2/BCL-XL inhibitor APG-1252-12A as a potential therapeutic strategy for gastric carcinoma. Abstract 2054. In: Proceedings of the American Association for Cancer Research Annual Meeting 2019; March 29 to April 3, 2019; Atlanta, GA USA. Cancer Res 2019. 79(13 Suppl) Abstract 2054. DOI:10.1158/1538-7445.AM2019-2054.
. ViewPredicting drug sensitivity to a novel BCL-2 and BCL-XL dual inhibitor in solid tumor PDX trials. Proceedings of the American Association for Cancer Research Annual Meeting 2019; March 29 to April 3, 2019: Atlanta, GA USA. Cancer Res 2019. 79(13 Suppl) Abstract 2503. DOI:10.1158/1538-7445.AM2019-2503.
. ViewActivation of p53 in the tumor microenvironment by MDM2 inhibitor APG-115 synergizes with PD-1 blockade independently of p53 status of tumor cells. Abstract 3192. In: Proceedings of the American Association for Cancer Research Annual Meeting 2019; March 29 to April 3, 2019; Atlanta, GA. Cancer Res July 1, 2019. 79(13 Suppl) Abstract 3192. DOI:10.1158/1538-7445.AM2019-3192.
. ViewA phase I study of a novel MDM2-P53 antagonist APG-115 in Chinese patients with advanced soft tissue sarcomas. American Society of Clinical Oncology 2019 Annual Meeting. J Clin Oncol 2019;37(15 Suppl): Abstract 3124 June 1, 2019. DOI:DOI: 10.1200/JCO.2019.37.15_suppl.3124.
. ViewA phase I study of a novel IAP inhibitor APG-1387 as a monotherapy or in combination with pembrolizumab in treatments of patients with advanced solid tumors. American Society of Clinical Oncology . J Clin Oncol 2019;37(15 Suppl):3125. NCT03386526 June 1, 2019. Abstract 3125
. ViewA phase I study of a novel MDM2 antagonist APG-115 in patients with advanced solid tumors. J Clin Oncol 2019;37(15 suppl): 3126. NCT02935907 May 26, 2019. Abstract 3126
. ViewA phase I study of a novel MDM2-P53 antagonist APG-115 in Chinese patients with advanced soft tissue sarcomas. J Clin Oncol 2019. 37(15 Suppl): Abstract 3124. DOI:10.1200/JCO.2019.37.15_suppl.3124.
. ViewA phase I study of a novel MDM2 antagonist APG-115 in patients with advanced solid tumors. J Clin Oncol . 37(15 suppl). Abstract 3126 DOI:10.1200/JCO.2019.37.15_suppl.3126 .
. ViewA novel small molecule inhibitor of MDM2-p53 (APG-115) has antitumor activity in gastric adenocarcinoma. Proceedings of the American Association for Cancer Research (AACR) Annual Meeting 2019. Cancer Res 2019;79(13 Suppl) March 29 to April 3, 2019. Abstract 2061
. ViewMDM2 inhibitor APG-115 synergizes with CDK4/6 inhibitors in a patient-derived xenograft model of dedifferentiated liposarcoma. American Association for Cancer Research Annual Meeting 2019. Cancer Res 2019;79 (13 Suppl) March 29 to April 3, 2019. Abstract 1253
. ViewActivation of p53 in the tumor microenvironment by MDM2 inhibitor APG-115 synergizes with PD-1 blockade independently of p53 status of tumor cells. American Association for Cancer Research Annual Meeting 2019. Cancer Res 2019;79(13 Suppl) March 29 to April 3, 2019. Abstract 3192
. ViewFAK blockade enhances antitumor effect of BTK inhibitor in esophageal squamous cell carcinoma via EGFR-ERK-Akt pathway inhibition. American Association for Cancer Research Annual Meeting 2019. American Association for Cancer Research Annual Meeting March 31, 2019. 60:78-79 DOI:https://doi.org/10.1158/1538-7445.AM2019-309.
. ViewSynergistic effect of BCL-2 inhibitor APG-2575 and CDK9 inhibitor in acute myeloid leukemia and DLBCL preclinical tumor models. Proceedings of the American Association for Cancer Research Annual Meeting 2019; March 29 to April 3, 2019; Atlanta, GA USA. Cancer Res 2019. 79(13 Suppl): Abstract 3068 DOI:10.1158/1538-7445.AM2019-3068 .
. ViewPredicting drug sensitivity to a novel BCL-2 and BCL-xL dual inhibitor in solid tumor PDX trials. American Association for Cancer Research Annual Meeting 2019. Cancer Res 2019;79(13 Suppl): Abstract 2503 March 29 - April 3, 2019.
. ViewFAK inhibition reduces tumor infiltration of Tregs via restricting CCL5 release and boosts the present therapeutic regimen for BRAFV600E-mutated colorectal carcinoma. American Association for Cancer Research Annual Meeting 2019. Cancer Res 2019;79(13 Suppl):Abstract 3958 March 29 - April 3, 2019 . DOI:https://doi.org/10.1158/1538-7445.AM2019-3958.
. ViewNovel FAK/ALK/ROS1 inhibitor APG-2449 synergizes with osimertinib in preclinical xenograft models of EGFR-mutant NSCLC. American Association for Cancer Research Annual Meeting 2019 . Cancer Res 2019;79(13 Suppl): Abstract 2204. March 29 - April 3, 2019. Poster Session PO. ET06-11. Abstract No. 19-A-2864. DOI:https://doi.org/10.1158/1538-7445.AM2019-2204.
. ViewActivation of p53 in the tumor microenvironment by MDM2 inhibitor APG-115 synergizes with PD-1 blockade independently of p53 status of tumor cells. American Association for Cancer Research Annual Meeting 2019. Cancer Res 2019;79(13 Suppl): Abstract 3192. March 29 - April 3, 2019.
. ViewA phase Ib/II study of APG-115 in combination with pembrolizumab in patients with unresectable or metastatic melanomas or advanced solid tumors. European Society for Medical Oncology Targeted Anticancer Therapies International Congress 2019. Ann Oncol 2019;30 (Supplement 1):i2–i3 February 25-27, 2019. Abstract 20 DOI:doi: https://doi.org/10.1093/annonc/mdz027. NCT03611868.
. ViewProbing distinct oncogene addiction by novel BCL-2 inhibitors. 60th American Society of Hematology (ASH) Annual Meeting. Blood 2018;132(Suppl 1): 2616. Poster 2616 December 1-4, 2018.
. ViewSafety and efficacy of HQP1351, a 3rd generation oral BCR-ABL inhibitor in patients with tyrosine kinase inhibitor-resistant chronic myelogenous leukemia: preliminary results of phase I study. 60th American Society of Hematology Annual Meeting. Blood 2018;132(Supplement 1):791. December 1-4, 2018.
. ViewProbing distinct oncogene addiction by novel BCL-2 inhibitors. 60th American Society of Hematology (ASH) Annual Meeting. Blood 2018;132(Suppl 1) December 1-4, 2018. Poster 2616 DOI:doi: https://doi.org/10.1182/blood-2018-99-119816.
. ViewA phase I study of novel BCL-2/BCL-XL inhibitor APG-1252 in patients with advanced SCLC or other solid tumor. Abstract OA12. J Thorac Oncol 2018. 132(Supplement 1) S1048-S1049. DOI:10.1016/j.jtho.2018.10.022.
. ViewProbing distinct oncogene addiction by novel BCL-2 inhibitors. Blood 2018. 132(Suppl 1) 2616. DOI:10.1182/blood-2018-99-119816 .
. ViewProbing distinct oncogene addiction by novel BCL-2 inhibitors. Blood November 29, 2018. 132(Suppl 1) Abstract 2616. DOI:10.1182/blood-2018-99-119816.
. ViewThe SMAC mimetic APG-1387 sensitizes immune-mediated cell apoptosis in hepatocellular carcinoma. Front Pharmacol 2018. 9 1298. DOI:10.3389/fphar.2018.01298.
. ViewTargeting cIAPs, a new option for functional cure of chronic hepatitis B infection. Virol Sin 2018. 33 459-461. DOI:10.1007/s12250-018-0062-x.
. ViewInhibitors of anti-apoptotic BCL-2 family proteins are effective in non-Hodgkin’s lymphoma. Chinese Society of Clinical Oncology (CSC0) 18th annual meeting. .
. ViewThe multi-faceted immunomodulatory function of Smac mimetic APG-1387 and its application in cancer immunotherapy. Chinese Society of Clinical Oncology (CSC0) 18th Annual Meeting. .
. ViewInhibitors of anti-apoptotic BCL-2 family proteins are effective in non-Hodgkin’s lymphoma. Chinese Society of Clinical Oncology (CSC0) 18th Annual Meeting. .
. ViewTargeting BCL-2 and BCL-XL with a novel dual inhibitor APG-1252 triggers cell death and inhibits tumor growth in small cell lung cancer models. Proceedings of the American Association for Cancer Research Annual Meeting; April 14‒18, 2018; Chicago, IL USA. Cancer Res 2018. 78(13 Suppl) Abstract 307. DOI:10.1158/1538-7445.AM2018-307.
. ViewTargeting the anti-apoptotic BCL-2 family protein provides an effective and precise therapeutic strategy for NHL. Proceedings of the American Association for Cancer Research Annual Meeting; April 14‒18, 2018; Chicago, IL USA. Cancer Res 2018. 78(13 Suppl) Abstract 301. DOI:10.1158/1538-7445.AM2018-301.
. ViewA phase I study of a novel IAP inhibitor APG-1387 in patients with advanced solid tumors. J Clin Oncol 2018. 36(15_suppl) 2593. DOI:10.1200/JCO.2018.36.15_suppl.2593 .
. ViewA 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 June 1, 2018. 36(Suppl 15) Abstract 2594. DOI:10.1200/JCO.2018.36.15_suppl.2594.
. ViewA novel small molecule inhibitor of MDM2-p53 (APG-115) enhances radiosensitivity of adenocarcinoma. J Exp Clin Cancer Res 2018. 37 97. DOI:10.1186/s13046-018-0765-8.
. ViewSmac mimetics APG-1387 synergizes with immune checkpoint inhibitors in preclinical models. American Association for Cancer Research Annual Meeting 2018. Cancer Res 2018;78(13 Suppl): Abstract 1754 April 14-18, 2018.
. ViewA novel MDM2-p53 antagonist APG-115 induces p53-mediated apoptosis and enhances radiosensitivity in colorectal cancer. American Association for Cancer Research Annual Meeting. Cancer Res 2018;78(13 Suppl) April 14-18, 2018. Abstract 314
. ViewHQP1351, a novel multikinase inhibitor in clinical development, overcomes drug resistance for the treatment of gastrointestinal stromal tumors in preclinical models. Proceedings of the American Association for Cancer Research Annual Meeting 2018; April 14‒18, 2018; Chicago, IL USA. Cancer Res 2018. 78(13 Suppl): Abstract 1979 DOI:10.1158/1538-7445.AM2018-1979.
. ViewNovel smac mimetic APG-1387 elicits ovarian cancer cell killing through TNF-alpha, ripoptosome and autophagy mediated cell death pathway. J Exp Clin Cancer Res 2018. 37 53. DOI:10.1186/s13046-018-0703-9.
. ViewAPG-1252-12A induces mitochondria-dependent apoptosis through inhibiting the antiapoptotic proteins Bcl-2/Bcl-xl in HL-60 cells. Int J Oncol 2017;51:563-72 June 6, 2017.
. ViewAPG-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.
. ViewRestoration 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.
. ViewDiscovery 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.
. ViewA potent and highly efficacious bivalent Smac mimetic APG-1387 in phase I clinical development. 26th EORTC-NCI-AACR Symposium. . Poster 268
. ViewBM-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
. ViewPreclinical 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.
. ViewIdentification 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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