olverembatinib

inhibits Bcr-Abl kinase to overcome imatinb resistance

Also Known As:

3-((1H-pyrazolo(3,4-b)pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide; 4-methyl-N-(4-((4-methyl-1-piperazinyl)methyl)-3-(trifluoromethyl)phenyl)-3-(2-(1H-pyrazolo(3,4-b)pyridin-5-yl)ethynyl)benzamide; D-824; D-824 dimesylate; D824; GZD-824; GZD-824 dimesylate; GZD824; HQP-1351; HQP-1351 dimesylate; HQP1351; HQP1351 dimesylate; benzamide, 4-methyl-N-(4-((4-methyl-1-piperazinyl)methyl)-3-(trifluoromethyl)phenyl)-3-(2-(1H-pyrazolo(3,4-b)pyridin-5-yl)ethynyl)-, methanesulfonate (1:2); olverembatinib dimesylate

Networked: 21 relevant articles (0 outcomes, 6 trials/studies)

Bio-Agent Context: Research Results

Experts

1.	Fang, Douglas D: 2 articles (01/2022 - 01/2019)
2.	Min, Ping: 2 articles (01/2022 - 01/2019)
3.	Tang, Qiuqiong: 2 articles (01/2022 - 01/2019)
4.	Wang, Guangfeng: 2 articles (01/2022 - 01/2019)
5.	Yang, Dajun: 2 articles (01/2022 - 01/2019)
6.	Zhai, Yifan: 2 articles (01/2022 - 01/2019)
7.	Ding, Ke: 2 articles (04/2020 - 10/2017)
8.	Ren, Xiaomei: 2 articles (04/2020 - 10/2017)
9.	Li, Na: 1 article (01/2022)
10.	Wang, Qixin: 1 article (01/2022)

Related Diseases

1.	BCR-ABL Positive Chronic Myelogenous Leukemia (Chronic Myelogenous Leukemia) 11/09/2023 - "Olverembatinib is a third-generation TKI that has been approved for the treatment of T315I-mutated chronic myeloid leukemia (CML) in China; its usage in Ph+ ALL needs further exploration. " 06/15/2023 - "This method was successfully utilized for the measurement of olverembatinib concentrations in plasma and CSF from chronic myeloid leukemia patients." 11/01/2022 - "Olverembatinib in chronic myeloid leukemia." 01/01/2022 - "A review of the therapeutic role of the new third-generation TKI olverembatinib in chronic myeloid leukemia." 01/01/2019 - "HQP1351, an orally bioavailable multikinase BCR-ABL inhibitor, is currently in clinical trials for the treatment of T315I mutant chronic myelogenous leukemia (CML), but the potential application in imatinib-resistant GISTs carrying secondary KIT mutations has not been explored. "
2.	Precursor Cell Lymphoblastic Leukemia-Lymphoma (Acute Lymphoblastic Leukemia) 01/01/2023 - "Case report: Olverembatinib monotherapy: the chemotherapy-free regimen for an elderly patient with relapsed Ph-positive acute lymphoblastic leukemia." 01/01/2023 - "Olverembatinib in relapsed Philadelphia chromosome-positive B-cell acute lymphoblastic leukemia: a study of 5 cases." 01/31/2023 - "Transcriptome- and metabolome-based candidate mechanism of BCR-ABL-independent resistance to olverembatinib in Philadelphia chromosome-positive acute lymphoblastic leukemia." 01/01/2023 - "Olverembatinib Treatment in Pediatric Patients With Relapsed Philadelphia-Chromosome-Positive Acute Lymphoblastic Leukemia." 10/20/2017 - "GZD824 suppresses the growth of human B cell precursor acute lymphoblastic leukemia cells by inhibiting the SRC kinase and PI3K/AKT pathways."
3.	Philadelphia Chromosome 01/01/2023 - "Olverembatinib in relapsed Philadelphia chromosome-positive B-cell acute lymphoblastic leukemia: a study of 5 cases." 01/31/2023 - "Transcriptome- and metabolome-based candidate mechanism of BCR-ABL-independent resistance to olverembatinib in Philadelphia chromosome-positive acute lymphoblastic leukemia." 01/01/2023 - "Olverembatinib Treatment in Pediatric Patients With Relapsed Philadelphia-Chromosome-Positive Acute Lymphoblastic Leukemia." 11/09/2023 - "Olverembatinib combined with blinatumomab in treating T315I-mutated Philadelphia chromosome-positive acute lymphoblastic leukemia: two-case report." 10/20/2017 - "We previously showed that GZD824, a novel BCR-ABL tyrosine kinase inhibitor, has anti-tumor activity in Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia cells and tumor models. "
4.	Leukemia 01/31/2023 - "This study has illustrated bone marrow cell transcriptome and metabolome profiles among Ph + acute lymphoblastic leukemias (ALL) cases pre- and post-olverembatinib resistance. " 04/01/2020 - "GZD824 as a FLT3, FGFR1 and PDGFRα Inhibitor Against Leukemia In Vitro and In Vivo." 04/01/2020 - "Thus GZD824 suppresses leukemia cells of FLT3-ITD-driven AML and other hematologic malignancies driven by FGFR1 or PDGFRa, and it may be considered to be a novel agent for the treatment of leukemia." 01/01/2022 - "Mechanistically, HQP1351 downregulated expression of myeloid-cell leukemia 1 (MCL-1) by suppressing FLT3-STAT5 (signal transducer and activator of transcription 5) signaling and thus enhanced APG-2575-induced apoptosis in FLT3-ITD mutant AML cells. " 04/01/2020 - "We found that at concentrations below 10 nM, GZD824 significantly suppresses FLT3, FGFR1 and PDGFRα kinase activities and inhibits their signal pathways in MV4-11Flt3-ITD, KG-1FGFR1OP2-FGFR1 and EOL-1FIP1L1-PDGFRa leukemia cells. "
5.	Neoplasms (Cancer) 01/01/2022 - "HQP1351 monotherapy also significantly suppressed growth of FLT3-ITD mutant AML xenograft tumors and prolonged survival of tumor-bearing mice. " 12/01/2020 - "Here, we found that a multikinase inhibitor, GZD824, which we identified using a cell-based assay with ATF4 immunostaining, inhibited the GCN2 pathway in cancer cells. " 01/01/2023 - "Olverembatinib for myeloid/lymphoid neoplasm associated with eosinophilia and FGFR1 rearrangement." 10/20/2017 - "GZD824 consistently reduced tumor loads in Ph- pre-B ALL xenografts but failed to suppress Ph+ pre-B ALL xenografts. " 01/01/2022 - "HQP1351 and APG-2575 synergistically induced apoptosis in FLT3-ITD mutant AML cells and suppressed growth of MV-4-11 xenograft tumors. "

Related Drugs and Biologics

1.	olverembatinib
2.	Tyrosine Kinase Inhibitors
3.	Imatinib Mesylate (Gleevec)
4.	bcr-abl Fusion Proteins
5.	Phosphotransferases (Kinase)
6.	Cytochrome P-450 CYP2C19
7.	Cytochrome P-450 CYP2C9
8.	Cytochrome P-450 CYP2B6 (CYP2B6)
9.	Proto-Oncogene Proteins c-bcr
10.	Cytochrome P-450 CYP3A

Related Therapies and Procedures

1.	Therapeutics
2.	Drug Therapy (Chemotherapy)