Therapy Detail

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Therapy Name HQP1351
Synonyms
Therapy Description

HQP1351 is a multikinase inhibitor that inhibits Kit and Abl1, which may lead to tumor growth inhibition (Cancer Res 2018;78(13 Suppl): Abstract nr 1979, Blood 2018 132:791).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
HQP1351 HQP 1351|HQP-1351|GZD824 dimesylate|GZD824 ABL1 Inhibitor 5 FGFR1 Inhibitor 23 FLT3 Inhibitor 54 KIT Inhibitor 50 PDGFR-alpha Inhibitor 9 GZD824 (HQP1351) is a third-generation BCR-ABL inhibitor and multikinase inhibitor that inhibits KIT, ABL1, FGFR1, FLT3, and PDGFRA (PMID: 32247263), which potentially induces apoptosis, and inhibits tumor cell growth, migration, and invasion (PMID: 31673329).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FLT3 D835V hematologic cancer predicted - sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 D835V demonstrated decreased proliferation in response to GZD824 (HQP1351) in culture, but were less sensitive to treatment than cells expressing other FLT3 kinase domain mutations (PMID: 32247263). 32247263
FLT3 exon 14 ins acute myeloid leukemia sensitive HQP1351 Preclinical - Cell line xenograft Actionable In a preclinical study, GZD824 (HQP1351) reduced Flt3 and Stat5 phosphorylation, induced cell cycle arrest and apoptosis, and inhibited growth of acute myeloid leukemia cells harboring FLT3-ITD in culture, and suppressed tumor growth, decreased Flt3 activation, and induced apoptosis in cell line xenograft models (PMID: 32247263). 32247263
FLT3 exon 14 ins FLT3 D835N hematologic cancer sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, GZD824 (HQP1351) inhibited growth of transformed cells expressing FLT3-ITD and FLT3 D835N in culture (PMID: 32247263). 32247263
FLT3 R834Q hematologic cancer predicted - sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 R834Q demonstrated decreased proliferation in response to GZD824 (HQP1351) in culture, but were less sensitive to treatment than cells expressing other FLT3 kinase domain mutations (PMID: 32247263). 32247263
FLT3 D835H hematologic cancer predicted - sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 D835H demonstrated decreased proliferation in response to GZD824 (HQP1351) in culture, but were less sensitive to treatment than cells expressing other FLT3 kinase domain mutations (PMID: 32247263). 32247263
FLT3 exon 14 ins FLT3 F691I hematologic cancer sensitive HQP1351 Preclinical - Cell line xenograft Actionable In a preclinical study, GZD824 (HQP1351) reduced Flt3 and Stat5 phosphorylation and inhibited growth of transformed cells expressing FLT3-ITD and FLT3 F691I in culture, and suppressed tumor growth, decreased Flt3 activation, and induced apoptosis in cell line xenograft models (PMID: 32247263). 32247263
FLT3 exon 14 ins FLT3 D835A hematologic cancer sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, GZD824 (HQP1351) inhibited growth of transformed cells expressing FLT3-ITD and FLT3 D835A in culture (PMID: 32247263). 32247263
KIT V560_Y578del gastrointestinal stromal tumor sensitive HQP1351 Preclinical - Cell line xenograft Actionable In a preclinical study, HQP1351 treatment inhibited Kit activity and proliferation of a gastrointestinal stromal tumor (GIST) cell line harboring KIT V560_Y578del in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 31673329). 31673329
FLT3 exon 14 ins FLT3 Y842H hematologic cancer sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, GZD824 (HQP1351) inhibited growth of transformed cells expressing FLT3-ITD and FLT3 Y842H in culture (PMID: 32247263). 32247263
FLT3 exon 14 ins FLT3 N676D hematologic cancer sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, GZD824 (HQP1351) inhibited growth of transformed cells expressing FLT3-ITD and FLT3 N676D in culture (PMID: 32247263). 32247263
FLT3 exon 14 ins FLT3 D835I hematologic cancer predicted - sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3-ITD and FLT3 D835I demonstrated decreased proliferation in response to GZD824 (HQP1351) in culture, but were less sensitive to treatment than cells co-expressing FLT3-ITD with other FLT3 kinase domain mutations (PMID: 32247263). 32247263
FLT3 exon 14 ins FLT3 D835G hematologic cancer sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, GZD824 (HQP1351) inhibited growth of transformed cells expressing FLT3-ITD and FLT3 D835G in culture (PMID: 32247263). 32247263
FLT3 D835Y hematologic cancer sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, GZD824 (HQP1351) inhibited growth of transformed cells expressing FLT3 D835Y in culture (PMID: 32247263). 32247263
KIT V560_L576del KIT V654A gastrointestinal stromal tumor sensitive HQP1351 Preclinical - Cell line xenograft Actionable In a preclinical study, HQP1351 treatment inhibited Kit downstream signalling, resulted in cell cycle arrest and apoptosis in a Gleevec (imatinib)-resistant gastrointestinal stromal tumor (GIST) cell line harboring KIT V560_L576del and V654A in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 31673329). 31673329
FLT3 exon 14 ins FLT3 D835Y hematologic cancer predicted - sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3-ITD and FLT3 D835Y demonstrated decreased proliferation in response to GZD824 (HQP1351) in culture, but were less sensitive to treatment than cells co-expressing FLT3-ITD with other FLT3 kinase domain mutations (PMID: 32247263). 32247263
FLT3 exon 14 ins FLT3 E654D acute myeloid leukemia predicted - sensitive HQP1351 Preclinical - Patient cell culture Actionable In a preclinical study, GZD824 (HQP1351) reduced Flt3 and Stat5 activation and inhibited growth of patient-derived acute myeloid leukemia cells harboring FLT3-ITD and FLT3 E654D in culture (PMID: 32247263). 32247263
FLT3 exon 14 ins FLT3 G697R hematologic cancer sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, GZD824 (HQP1351) inhibited growth of transformed cells expressing FLT3-ITD and FLT3 G697R in culture (PMID: 32247263). 32247263
FLT3 exon 14 ins FLT3 Y842R hematologic cancer sensitive HQP1351 Preclinical Actionable In a preclinical study, GZD824 (HQP1351) inhibited growth of transformed cells expressing FLT3-ITD and FLT3 Y842R in culture (PMID: 32247263). 32247263
FLT3 exon 14 ins hematologic cancer sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, GZD824 (HQP1351) inhibited growth of transformed cells expressing FLT3-ITD in culture (PMID: 32247263). 32247263
FLT3 exon 14 ins FLT3 D835V hematologic cancer predicted - sensitive HQP1351 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3-ITD and FLT3 D835V demonstrated decreased proliferation in response to GZD824 (HQP1351) in culture, but were less sensitive to treatment than cells co-expressing FLT3-ITD with other FLT3 kinase domain mutations (PMID: 32247263). 32247263

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  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

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Clinical Trial Phase Therapies Title Recruitment Status
NCT04260022 Phase I HQP1351 Study of HQP1351 in Subjects With Refractory Chronic Myeloid Leukemia (HQP1351CU101) Recruiting


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