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Therapy Name | FF-10101 |
Synonyms | |
Therapy Description |
FF-10101 is a second generation and irreversible inhibitor of Flt3, including the internal tandem duplication (FLT3-ITD) and known resistance mutations (D835Y, Y842C, Y842H, or F691L) and also inhibits Kit and Csf1r (Fms) (PMID: 29187377, PMID: 32722298) |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
FF-10101 | FF-10101-01|FF10101|FF 10101 | CSF1R Inhibitor 28 FLT3 Inhibitor 69 KIT Inhibitor 57 | FF-10101 is a second generation and irreversible inhibitor of Flt3, including the internal tandem duplication (FLT3-ITD) and known resistance mutations (D835Y, Y842C, Y842H, or F691L) and also inhibits Kit and Csf1r (Fms) (PMID: 29187377, PMID: 32722298) |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
FLT3 exon 14 ins | acute myeloid leukemia | sensitive | FF-10101 | Phase I | Actionable | In a Phase I trial, FF-10101 treatment was well tolerated, and resulted in a composite complete remission (CRc) in 13% (4/30) and a partial remission (PR) in 13% (4/30) of patients with relapsed or refractory acute myeloid leukemia, 1 of the patients achieved CRc and 2 of the patients achieved PR harbored FLT3 ITD mutations (J Clin Oncol 39, no. 15_suppl (May 20, 2021) 7008-7008; NCT03194685). | detail... |
FLT3 exon 14 ins FLT3 D835H | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Pdx | Actionable | In a preclinical study, FF-10101 inhibited cell growth in AML-patient-derived xenograft models with FLT3-ITD/D835H compound mutations (PMID: 29187377). | 29187377 |
FLT3 exon 14 ins | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, FF-10101 inhibited Flt3 autophosphorylation and cell growth of leukemic cells in culture and in AML-patient-derived xenograft models with FLT3-ITD mutations (PMID: 29187377). | 29187377 |
FLT3 exon 14 ins FLT3 D835Y | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, FF-10101 inhibited Flt3 autophosphorylation and growth of leukemic cell lines and inhibited growth of cell line xenografts with FLT3-ITD/D835Y compound mutations (PMID: 29187377). | 29187377 |
FLT3 exon 14 ins FLT3 F691L | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, FF-10101 inhibited Flt3 autophosphorylation and growth of leukemic cell lines and inhibited growth of cell line xenografts with FLT3-ITD/F691L compound mutations (PMID: 29187377). | 29187377 |
FLT3 exon 14 ins | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of acute myeloid leukemia cells harboring FLT3-ITD in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 A848P | acute myeloid leukemia | predicted - sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring FLT3-ITD and FLT3 A848P demonstrated sensitivity to treatment with FF-10101 in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 C681S | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 C681S in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 C694S | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 C694S in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 C695S | hematologic cancer | predicted - resistant | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 C695S were resistant to treatment with FF-10101 in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 C790S | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 C790S in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 C807S | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 C807S in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 C828S | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 C828S in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D698N | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D698N in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D698N FLT3 D835V | hematologic cancer | predicted - resistant | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD with FLT3 D698N and D835V were moderately resistant to treatment with FF-10101 in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835A | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835A in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835del | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835del in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835E | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835E in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835F | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835F in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835G | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835G in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835H | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of acute myeloid leukemia cells harboring FLT3-ITD and FLT3 D835H in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835H | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835H in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835I | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835I in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835N | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of acute myeloid leukemia cells harboring FLT3-ITD and FLT3 D835N in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835N | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835N in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835V | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of acute myeloid leukemia cells harboring FLT3-ITD and FLT3 D835V in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835V | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835V in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835Y | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of acute myeloid leukemia cells harboring FLT3-ITD and FLT3 D835Y in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 D835Y | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835Y in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 F691L | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring FLT3-ITD and FLT3 F691L demonstrated sensitivity to treatment with FF-10101 in culture, but were less sensitive compared to cells harboring FLT3-ITD alone (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 F691L | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells harboring FLT3-ITD and FLT3 F691L demonstrated sensitivity to treatment with FF-10101 in culture, but were less sensitive compared to cells expressing FLT3-ITD alone (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 F691L FLT3 D835V | hematologic cancer | predicted - resistant | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD with FLT3 F691L and D835V were moderately resistant to treatment with FF-10101 in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 G697S | hematologic cancer | predicted - resistant | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 G697S were moderately resistant to treatment with FF-10101 in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 K429E | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 K429E in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 M664I | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 M664I in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 N676K | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 N676K in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 N841K | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of acute myeloid leukemia cells harboring FLT3-ITD and FLT3 N841K in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 N841Y | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of acute myeloid leukemia cells harboring FLT3-ITD and FLT3 N841Y in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 Y693C | hematologic cancer | resistant | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 Y693C were resistant to treatment with FF-10101 in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 Y693C FLT3 D835V | hematologic cancer | resistant | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD with FLT3 Y693C and D835V were resistant to treatment with FF-10101 in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 Y693F | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 Y693F in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 Y693N | hematologic cancer | predicted - resistant | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 Y693N were moderately resistant to treatment with FF-10101 in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 Y842C | acute myeloid leukemia | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101 treatment inhibited growth of acute myeloid leukemia cells harboring FLT3-ITD and FLT3 Y842C in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins FLT3 Y842C | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101, as compared to Quizartinib, inhibited Flt3 autophosphorylation and cell proliferation of transformed 32Dcl3 murine myeloid cells expressing a human FLT3-ITD/Y842C compound mutation (PMID: 29187377). | 29187377 |
FLT3 exon 14 ins FLT3 Y842H | hematologic cancer | sensitive | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, FF-10101, as compared to Quizartinib, inhibited Flt3 autophosphorylation and cell proliferation of transformed 32Dcl3 murine myeloid cells expressing a human FLT3-ITD/Y842H compound mutation (PMID: 29187377). | 29187377 |
FLT3 exon 14 ins NRAS G12C | acute myeloid leukemia | resistant | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring a FLT3-ITD mutation and expressing NRAS G12C demonstrated resistance to treatment with FF-10101 in culture (PMID: 35395091). | 35395091 |
FLT3 exon 14 ins NRAS Q61K | acute myeloid leukemia | resistant | FF-10101 | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring a FLT3-ITD mutation and expressing NRAS Q61K demonstrated resistance to treatment with FF-10101 in culture (PMID: 35395091). | 35395091 |
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 |
FLT3 exon 14 ins FLT3 C695S | hematologic cancer | predicted - resistant | FF-10101 | Preclinical - Biochemical | Actionable | In a preclinical study, FF-10101 treatment failed to inhibit Flt3 phosphorylation in transformed human cells expressing FLT3-ITD and FLT3 C695S in culture (PMID: 29187377). | 29187377 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT03194685 | Phase Ib/II | FF-10101 | Study of FF-10101-01 in Patients With Relapsed or Refractory Acute Myeloid Leukemia | Completed | USA | 0 |
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