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Therapy Name Imatinib + Infigratinib
Synonyms
Therapy Description

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Imatinib Gleevec CGP-57148B|STI571|Imatinib mesylate ABL Inhibitor (pan) 9 BCR-ABL Inhibitor 32 CSF1R Inhibitor 28 KIT Inhibitor 57 PDGFR Inhibitor (Pan) 30 Gleevec (imatinib) is a multi-target inhibitor of c-Kit, Pdgfr, and Bcr-Abl (PMID: 12200353). Gleevec (imatinib) is FDA approved for c-KIT positive GIST and dermatofibrosarcoma protuberans, Philadelphia chromosome positive chronic myeloid leukemia, and FIP1L1-PDGFRA positive chronic eosinophilic leukemia (FDA.gov).
Infigratinib Truseltiq BGJ398|BGJ-398|BGJ 398 FGFR Inhibitor (Pan) 26 Truseltiq (infigratinib) is a pan-FGFR inhibitor, which inhibits tumor angiogenesis and tumor cell proliferation (PMID: 31109923, PMID: 30101387). Truseltiq (infigratinib) is FDA approved for use in patients with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma harboring FGFR2 fusion or rearrangement (FDA.gov).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
KIT V560_Y578del gastrointestinal stromal tumor sensitive Imatinib + Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Truseltiq (infigratinib) and Gleevec (imatinib) combination treatment demonstrated enhanced antiproliferative activity in gastrointestinal stromal tumor cells harboring KIT V560_Y578del in culture (PMID: 25673643). 25673643
KIT K642E gastrointestinal stromal tumor sensitive Imatinib + Infigratinib Preclinical - Cell culture Actionable In a preclinical study, Truseltiq (infigratinib) and Gleevec (imatinib) combination treatment demonstrated enhanced antiproliferative activity in gastrointestinal stromal tumor cells harboring KIT K642E in culture (PMID: 25673643). 25673643
KIT exon9 gastrointestinal stromal tumor no benefit Imatinib + Infigratinib Phase I Actionable In a Phase I trial, Truseltiq (infigratinib) and Gleevec (imatinib) combination therapy resulted in stable disease as best response in 58% (7/12) of patients with advanced gastrointestinal stromal tumor harboring KIT mutations in exon 9 (n=3), exon 11 (n=10), or other (n=3), however, the trial was discontinued due to toxicity concerns (PMID: 30101387). 30101387
KIT exon11 gastrointestinal stromal tumor no benefit Imatinib + Infigratinib Phase I Actionable In a Phase I trial, Truseltiq (infigratinib) and Gleevec (imatinib) combination therapy resulted in stable disease as best response in 58% (7/12) of patients with advanced gastrointestinal stromal tumor harboring KIT mutations in exon 11 (n=10), exon 9 (n=3), or other (n=3), however, the trial was discontinued due to toxicity concerns (PMID: 30101387). 30101387
KIT V560D KIT D820A gastrointestinal stromal tumor predicted - sensitive Imatinib + Infigratinib Preclinical - Cell line xenograft Actionable In a preclinical study, combination treatment with Gleevec (imatinib) and Truseltiq (infigratinib) treatment resulted in tumor shrinkage in a gastrointestinal stromal tumor cell line xenograft model harboring KIT V560D and KIT D820A (PMID: 35625872). 35625872
KIT mutant gastrointestinal stromal tumor sensitive Imatinib + Infigratinib Preclinical - Pdx Actionable In a preclinical study, Truseltiq (infigratinib) and Gleevec (imatinib) combination treatment demonstrated enhanced antitumor activity in patient derived xenograft models of gastrointestinal stromal tumor harboring KIT mutations (PMID: 25673643). 25673643

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT02257541 Phase Ib/II Imatinib + Infigratinib BGJ398 in Combination With Imatinib Mesylate in Patients With Untreated Advanced Gastrointestinal Stromal Tumor (GIST) Completed USA 0


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