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Therapy Name SKI-G-801
Synonyms
Therapy Description

SKI-G-801 is a multi-kinase inhibitor that has activity against wild-type and mutant forms of FLT3, which blocks FLT3 signaling and potentially inhibits proliferation of FLT3-overexpressing tumor cells, and has additional activity against AXL, potentially leading to decreased tumor cell metastasis, as well as MER, RET, VEGFR1, FMS, FGFR1, FGFR3, AURKB, and AURKC (NCI Drug Dictionary; Cancer Res 2019;79(13 Suppl):Abstract nr 2010).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
SKI-G-801 FLT3 kinase inhibitor SKI G-801|SKI G-801|G-801|G-749 HCl Aurkb Inhibitors 21 Aurkc Inhibitors 3 AXL Inhibitor 30 FGFR1 Inhibitor 28 FGFR3 Inhibitor 19 FLT3 Inhibitor 69 MERTK Inhibitor 13 RET Inhibitor 53 VEGFR1 Inhibitor 6 SKI-G-801 is a multi-kinase inhibitor that has activity against wild-type and mutant forms of FLT3, which blocks FLT3 signaling and potentially inhibits proliferation of FLT3-overexpressing tumor cells, and has additional activity against AXL, potentially leading to decreased tumor cell metastasis, as well as MER, RET, VEGFR1, FMS, FGFR1, FGFR3, AURKB, and AURKC (NCI Drug Dictionary; Cancer Res 2019;79(13 Suppl):Abstract nr 2010).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FLT3 exon 14 ins FLT3 F691L hematologic cancer sensitive SKI-G-801 Preclinical - Cell culture Actionable In a preclinical study, cells co-expressing a FLT3 internal tandem duplication and FLT3 F691L were sensitive to SKI-G-801 in culture, demonstrating inhibition of cell growth and inhibition of Flt3 autophosphorylation (PMID: 24532805). 24532805
FLT3 N676D FLT3 D835Y hematologic cancer sensitive SKI-G-801 Preclinical - Cell culture Actionable In a preclinical study, cells co-expressing FLT3 D835Y and FLT3 N676D were sensitive to SKI-G-801 in culture, demonstrating inhibition of cell growth and inhibition of Flt3 autophosphorylation (PMID: 24532805). 24532805
FLT3 exon 14 ins FLT3 N676D hematologic cancer sensitive SKI-G-801 Preclinical - Cell culture Actionable In a preclinical study, cells co-expressing a FLT3 internal tandem duplication and FLT3 N676D were sensitive to SKI-G-801 in culture, demonstrating inhibition of cell growth and inhibition of Flt3 autophosphorylation (PMID: 24532805). 24532805
FLT3 exon 14 ins acute myeloid leukemia sensitive SKI-G-801 Preclinical - Cell line xenograft Actionable In a preclinical study, SKI-G-801 induced apoptosis in acute myeloid leukemia cells harboring a FLT3 internal tandem duplication in culture, and inhibited tumor growth and induced tumor regression in cell line xenograft models (PMID: 24532805). 24532805
FLT3 D835Y hematologic cancer sensitive SKI-G-801 Preclinical - Cell culture Actionable In a preclinical study, cells expressing FLT3 D835Y were sensitive to SKI-G-801 in culture, demonstrating inhibition of cell growth and inhibition of Flt3 autophosphorylation (PMID: 24532805). 24532805

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT03564288 Phase I SKI-G-801 Study to Find a Safe and Effective Dose of SKI-G-801 in the Treatment of Patients With Acute Myeloid Leukemia (AML) Completed USA 0


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