Molecular Profile Detail

Profile Name KIT D816V
Gene Variant Detail

KIT D816V (gain of function)

Relevant Treatment Approaches Avapritinib Dasatinib

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
KIT D816V acute myeloid leukemia sensitive Cytarabine + Dasatinib Case Reports/Case Series Actionable In a clinical case study, a patient with acute myeloid leukemia harboring KIT D816V achieved long-term remission and loss of KIT D816V following treatment with the combination of Sprycel (dasatinib) and Cytosar-U (cytarabine) (PMID: 18986703). 18986703
KIT D816V Advanced Solid Tumor resistant Cabozantinib Preclinical Actionable In a preclinical study, transformed cells expressing KIT D816V demonstrated resistance to Cometriq (cabozantinib) in culture (PMID: 24205792). 24205792
KIT D816V Advanced Solid Tumor resistant Imatinib Preclinical Actionable In a preclinical study, transformed cells expressing KIT D816V demonstrated resistance to Gleevec (imatinib mesylate) in culture (PMID: 15790786). 15790786
KIT D816V Indication other than cancer resistant Imatinib FDA approved Actionable Gleevec (imatinib) is not indicated for patients with aggressive systemic mastocytosis harboring KIT D816V (FDA.gov). detail...
KIT D816V Advanced Solid Tumor resistant Sunitinib Preclinical Actionable In a preclinical study, KIT D816V mutations demonstrated resistance to Sutent (sunitinib) in a biochemical assay (PMID: 19164557). 19164557
KIT D816V Advanced Solid Tumor resistant Sunitinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT D816V were resistant to treatment with Sutent (sunitinib) in culture (PMID: 24205792). 24205792
KIT D816V hematologic cancer sensitive FF-10101 Preclinical - Cell culture Actionable In a preclinical study, FF-10101, as compared to Quizartinib, inhibited cell proliferation of transformed 32Dcl3 murine myeloid cells expressing human Kit D816V (PMID: 29187377). 29187377
KIT D816V Advanced Solid Tumor decreased response Nilotinib Preclinical Actionable In a preclinical study, Tasigna (nilotinib) decreased viability of cells expressing KIT D816V in culture, but did not inhibit KIT phosphorylation or growth of KIT D816V-expressing tumors in mouse models (PMID: 20442311). 20442311
KIT D816V Advanced Solid Tumor resistant Quizartinib Preclinical Actionable In a preclinical study, transformed cells expressing KIT D816V demonstrated resistance to Quizartinib in culture (PMID: 23497317). 23497317
KIT D816V hematologic cancer resistant Imatinib Preclinical Actionable In a preclinical study, a mouse myeloid cell line expressing KIT D816V demonstrated resistance to Gleevec (imatinib) in culture (PMID: 12481435). 12481435
KIT D816V Advanced Solid Tumor resistant Ponatinib Preclinical Actionable In a preclinical study, Iclusig (ponatinib) did not inhibit growth of transformed cells expressing KIT D816V in culture (PMID: 22301675). 22301675
KIT D816V hematologic cancer resistant Sorafenib Preclinical Actionable In a preclinical study, transformed hematopoietic cells expressing KIT D816V demonstrated resistance to Nexavar (sorafenib) in culture (PMID: 17229632). 17229632
KIT D816V Advanced Solid Tumor predicted - sensitive BPR1J373 Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT D816V were sensitive to BPR1J373, demonstrating inhibition of Kit phosphorylation (PMID: 27512117). 27512117
KIT D816V mast cell neoplasm predicted - sensitive Avapritinib Avapritinib Phase I Actionable In a Phase I trial, patients with either aggressive systemic mastocytosis, mast cell leukemia, or systemic mastocytosis with an associated hematologic neoplasm harboring KIT D816V demonstrated a reduction in mast cell burden and a decrease in KIT D816V allelic fraction when treated with BLU-285 (ASH Annual Meeting, Dec 2017, Plenary 2). detail...
KIT D816V Advanced Solid Tumor resistant Flumatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing KIT D816V were resistant to treatment with Flumatinib in culture (PMID: 24205792). 24205792
Clinical Trial Phase Therapies Title Recruitment Status