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Profile Name | FGFR1 act mut |
Gene Variant Detail | |
Relevant Treatment Approaches | FGFR Inhibitor (Pan) FGFR1 Inhibitor |
Molecular Profile | Indication/Tumor Type | Response Type | Relevant Treatment Approaches | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|---|
FGFR1 act mut | Advanced Solid Tumor | sensitive | FGFR1 Inhibitor | Debio 1347 | Phase I | Actionable | In a Phase I trial, Debio 1347 (CH5183284) dosing regimen has been determined in solid tumor patients with activating FGFR1 alterations (JCO, Vol 33, No 15_suppl (May 20 Supplement), 2015: 2540). | detail... |
FGFR1 act mut | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | Ponatinib | Preclinical | Actionable | In a preclinical study, Iclusig (ponatinib) inhibited receptor phosphorylation and cell growth in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). | 22238366 |
FGFR1 act mut | Advanced Solid Tumor | sensitive | FGFR Inhibitor (Pan) | Dovitinib | Preclinical | Actionable | In a preclinical study, Dovitinib (TKI258) inhibited receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). | 22238366 |
FGFR1 act mut | Advanced Solid Tumor | decreased response | Cediranib | Preclinical | Actionable | In a preclinical study, transformed cells expressing constitutively active FGFR1 demonstrated reduced sensitivity to inhibition of receptor phosphorylation and cell proliferation by Cediranib (AZD-2171) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). | 22238366 | |
FGFR1 act mut | Advanced Solid Tumor | decreased response | FGFR Inhibitor (Pan) | Nintedanib | Preclinical | Actionable | In a preclinical study, transformed cells expressing constitutively active FGFR1 demonstrated reduced sensitivity to Ofev (Nintedanib) in culture, when compared to other tyrosine kinase inhibitors (PMID: 22238366). | 22238366 |
FGFR1 act mut | Advanced Solid Tumor | no benefit | FGFR1 Inhibitor | Brivanib | Preclinical | Actionable | In a preclinical study, Brivanib (BMS-540215) did not inhibit receptor phosphorylation and cell proliferation in transformed cells expressing constitutively active FGFR1 in culture (PMID: 22238366). | 22238366 |
FGFR1 act mut | Advanced Solid Tumor | predicted - sensitive | FGFR Inhibitor (Pan) | Erdafitinib | Phase I | Actionable | In a Phase I trial, Balversa (erdafitinib) treatment resulted in stable disease in 70% (16/23) and partial response in 22% (5/23) of patients with advanced solid tumors harboring FGFR 1-4 activating mutations (including amplifications, mutations and translocations), while no antitumor activity was observed in patients with unknown or no known changes in FGFR (PMID: 26324363; NCT01703481). | 26324363 |
FGFR1 act mut | breast cancer | sensitive | FGFR Inhibitor (Pan) | FIIN-1 | Preclinical | Actionable | In a preclinical study, FIIN-1 inhibited Fgfr1 activation-induced proliferation and transformation of human breast epithelial cell lines in culture (PMID: 20338520). | 20338520 |