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Therapy Name | Infigratinib |
Synonyms | |
Therapy Description |
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). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
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). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
FGFR2 E596K | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 E596K were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 D133N | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 D133N were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 H544Q | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 H544Q were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 amp | lung squamous cell carcinoma | sensitive | Infigratinib | Phase I | Actionable | In a Phase I trial, patients with lung squamous cell carcinoma harboring an FGFR1 amplification demonstrated a disease control rate of 50% (18/36) when treated with Truseltiq (infigratinib), resulting in 14 patients with stable disease and 4 patients with a partial response (PMID: 27870574). | 27870574 |
FGFR1 positive | uterus leiomyosarcoma | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, uterine leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to Truseltiq (infigratinib) in culture (PMID: 27535980). | 27535980 |
FGFR1 K656E | Advanced Solid Tumor | conflicting | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 K656E were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 K656E | Advanced Solid Tumor | conflicting | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 K656E demonstrated insensitivity to Truseltiq (infigratinib) in culture (PMID: 34114373). | 34114373 |
FGFR2 G364E | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 G364E were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 S267_D273dup | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical | Actionable | In a preclinical study, Truseltiq (infigratinib) prevented oncogenic transformation of cells expressing FGFR2 S267_D273dup (PMID: 26048680). | 26048680 |
FGFR2 N549D | Advanced Solid Tumor | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 N549D were resistant to treatment with Truseltiq (infigratinib) in culture (PMID: 34272467). | 34272467 |
FGFR3 mutant | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical | Actionable | In a preclinical study, tumor cell lines with FGFR3 mutations demonstrated sensitivity to Truseltiq (infigratinib) in culture (PMID: 23002168). | 23002168 |
FGFR2 fusion FGFR2 H683L | intrahepatic cholangiocarcinoma | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 H683L had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). | 31109923 |
FGFR2 C62Y | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 C62Y were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 V564L | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Biochemical | Actionable | In a preclinical study, Truseltiq (infigratinib) failed to inhibit Fgfr2 phosphorylation in cultured cells expressing FGFR2 V564L (PMID: 37270847). | 37270847 |
FGFR2 mutant | endometrial cancer | sensitive | Infigratinib | Preclinical | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited the growth of FGFR2-mutated endometrial cancer cells in vitro and in xenograft models (PMID: 23443805). | 23443805 |
FGFR2 K660E | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of transformed cells expressing FGFR2 K660E in culture (PMID: 23786770). | 23786770 |
FGFR1 positive | synovial sarcoma | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, synovial sarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to Truseltiq (infigratinib) in culture (PMID: 27535980). | 27535980 |
FGFR3 H284fs | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 H284fs (FGFR3 H284fs*10) were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 R809Q | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 R809Q were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 S238N | Advanced Solid Tumor | predicted - resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 S238N were resistant to treatment with Truseltiq (infigratinib) in culture (PMID: 34272467). | 34272467 |
FGFR2 A389T | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 A389T were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 D788N | head and neck squamous cell carcinoma | no benefit | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited proliferation of a head and neck squamous cell carcinoma cell line expressing FGFR3 D788N in culture, however, cells expressing FGFR3 D788N did not demonstrate increased sensitivity to Truseltiq (infigratinib) compared to cells expressing wild-type FGFR3 (PMID: 27053219). | 27053219 |
FGFR3 over exp | urinary bladder cancer | sensitive | Infigratinib | Preclinical - Pdx | Actionable | In a preclinical study, treatment with Truseltiq (infigratinib) led to improved progression-free survival in a patient-derived xenograft (PDX) model of bladder cancer with FGFR3 over expression (PMID: 26270481). | 26270481 |
FGFR2 S252W | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 S252W were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 S249C FGFR3 V555M | urinary bladder cancer | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, a bladder cancer cell line harboring FGFR3 S249C and expressing FGFR3 V555M was resistant to Truseltiq (infigratinib) in culture (PMID: 38437671). | 38437671 |
FGFR2 F276C | intrahepatic cholangiocarcinoma | predicted - sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase II trial, Truseltiq (infigratinib) treatment resulted in partial response after 2 months of therapy and response was maintained for 4 months in a patient with advanced intrahepatic cholangiocarcinoma harboring a FGFR2 F276C mutation, which is consistent with inhibition of Erk signaling in cholangiocarcinoma cells expressing FGFR2 F274C in culture (PMID: 30761385; NCT02150967). | 30761385 |
FGFR2 amp | cholangiocarcinoma | sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase II trial, Truseltiq (infigratinib) treatment demonstrated manageable toxicity, and resulted in a 27% tumor size reduction in a patient with advanced cholangiocarcinoma harboring FGFR2 amplification (PMID: 29182496; NCT02150967). | 29182496 |
FGFR2 amp | cholangiocarcinoma | sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a clinical case study, treatment with Truseltiq (infigratinib) resulted in stable disease for 3.9 months in a patient with cholangiocarcinoma with amplification of FGFR2 (PMID: 34250419). | 34250419 |
FGFR1 V561M | Advanced Solid Tumor | predicted - resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with Truseltiq (infigratinib) failed to inhibit cell growth and Fgfr1 downstream signaling in cells expressing FGFR1 V561M in culture (PMID: 34114373). | 34114373 |
FGFR3 V555M FGFR3 L608V | transitional cell carcinoma | predicted - resistant | Infigratinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with metastatic urothelial carcinoma progressed while being treated with Truseltiq (infigratinib) and subsequent cell-free DNA testing revealed FGFR3 V555M (also corresponds to V443M) and FGFR3 L608V (also corresponds to L496V) (PMID: 29848605). | 29848605 |
FGFR2 G227E | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 G227E were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 fusion | transitional cell carcinoma | sensitive | Infigratinib | Phase I | Actionable | In a Phase I trial, Truseltiq (infigratinib) treatment resulted in complete response in 4% (1/25) and partial response in 32% (8/25) of urothelial carcinoma patients harboring FGFR3 mutations or fusions (J Clin Oncol 34, 2016 (suppl; abstr 4517)). | detail... |
FGFR3 V555M | Advanced Solid Tumor | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 V555M were resistant to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
FGFR3 N540K | Advanced Solid Tumor | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 N540K were resistant to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
FGFR3 amp | urinary system cancer | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 amplification in culture (PMID: 27401245). | 27401245 |
FGFR2 H167_N173del | cholangiocarcinoma | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased viability of a cholangiocarcinoma cell line expressing FGFR2 H167_N173del in culture (PMID: 37964396). | 37964396 |
FGFR2 fusion FGFR2 K660M | intrahepatic cholangiocarcinoma | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 K660M were resistant to treatment as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). | 31109923 |
FGFR2 E768* | breast cancer | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of mouse mammary epithelial cells expressing FGFR2 E673* (corresponding to E768* in human) in culture (PMID: 35948633). | 35948633 |
FGFR2 R664W | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 R664W were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 A391E | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 A391E were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 P483L | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 P483L were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 S371C | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 S371C were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 K650E | Advanced Solid Tumor | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 K650E demonstrated reduced sensitivity to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
FGFR1 K656E | high grade glioma | predicted - sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase II trial, Truseltiq (infigratinib) treatment resulted in limited efficacy with a 6-month progression-free survival (PFS) rate of 16.0%, a median PFS of 1.7 months, an objective response rate of 4.8% (1/21), and median overall survival of 6.7 months in patients with recurrent glioma harboring alterations in FGFR1 or FGFR3; however, resulted in a partial response with PFS of 21.9 months and stable disease with PFS of 13.2 months in two patients harboring FGFR1 K656E (PMID: 35344029; NCT01975701). | 35344029 |
FGFR1 amp NRAS amp | lung non-small cell carcinoma | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, amplification of NRAS was identified in a non-small cell lung cancer cell line harboring FGFR1 amplification that acquired resistance to Truseltiq (infigratinib) in culture (PMID: 28630215). | 28630215 |
FGFR3 K652E | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased viability of a cell line expressing FGFR3 K652E in culture (PMID: 32370101). | 32370101 |
FGFR1 R475Q | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 R475Q were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 V751A | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 V751A were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 N542K | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased viability of a cell line expressing FGFR3 N542K in culture (PMID: 32370101). | 32370101 |
FGFR3 G380R | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G380R were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 C382R | cholangiocarcinoma | no benefit | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) did not decrease viability of a cholangiocarcinoma cell line expressing FGFR2 C382R in culture (PMID: 37964396). | 37964396 |
FGFR2 K659N | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 K659N were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 R399Q | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 R399Q were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 E163K | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 E163K were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 R203C | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 R203C were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 P150S | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 P150S were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 rearrange | cholangiocarcinoma | sensitive | Infigratinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase II trial that supported FDA approval, Truseltiq (infigratinib) treatment demonstrated manageable toxicity, resulted in an objective response rate of 23.1% (25/108, 1 complete response, 24 partial responses) in patients with previously treated advanced cholangiocarcinoma harboring an FGFR2 fusion or rearrangement, with a median duration of response of 5.0 months and a median progression-free survival of 7.3 months (J Clin Oncol 39, no. 3_suppl (January 20, 2021) 265-265; NCT02150967). | detail... detail... detail... |
FGFR2 Y375C | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 Y375C were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 fusion FGFR2 N550H | intrahepatic cholangiocarcinoma | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 N550H had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). | 31109923 |
FGFR3 L608V | Advanced Solid Tumor | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
FGFR2 fusion FGFR2 M538I | intrahepatic cholangiocarcinoma | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 M538I had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). | 31109923 |
FGFR1 D128V | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 D128V were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 positive | leiomyosarcoma | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to Truseltiq (infigratinib) in culture (PMID: 27535980). | 27535980 |
FGFR3 S249C | urinary system cancer | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 S249C in culture (PMID: 27401245). | 27401245 |
FGFR2 V564I | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Biochemical | Actionable | In a preclinical study, Truseltiq (infigratinib) failed to inhibit Fgfr2 phosphorylation in cultured cells expressing FGFR2 V564I (PMID: 37270847). | 37270847 |
FGFR2 M186T | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 M186T were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 K656N | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of a cell line expressing FGFR1 K656N in culture (PMID: 34114373). | 34114373 |
FGFR2 fusion FGFR2 K715R | intrahepatic cholangiocarcinoma | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 K715R were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling, in in vitro assays (PMID: 31109923). | 31109923 |
FGFR2 Y328N | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 Y328N were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 A264T | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 A264T were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 over exp | stomach cancer | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment inhibited growth of FGFR1-overexpressing gastric cancer cells in culture (PMID: 33563752). | 33563752 |
FGFR2 fusion FGFR2 N550K | intrahepatic cholangiocarcinoma | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 N550K were resistant to treatment as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). | 31109923 |
FGFR2 E718K | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 E718K were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 D101Y | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 D101Y were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 D764H | head and neck squamous cell carcinoma | no benefit | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited proliferation of a head and neck squamous cell carcinoma cell line expressing FGFR3 D764H in culture, however, cells expressing FGFR3 D764H did not demonstrate increased sensitivity to Truseltiq (infigratinib) compared to cells expressing wild-type FGFR3 (PMID: 27053219). | 27053219 |
FGFR1 over exp | uterus leiomyosarcoma | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited survival of FGFR1-overexpressing uterus leiomyosarcoma cells in culture (PMID: 27535980). | 27535980 |
FGFR2 K310R | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 K310R were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 mutant | bladder urothelial carcinoma | sensitive | Infigratinib | Phase I | Actionable | In a Phase I trial, patients with bladder urothelial carcinoma harboring an FGFR3 mutation demonstrated a disease control rate of 75% (6/8) when treated with Truseltiq (infigratinib), including 3 patients with a partial response and 3 with stable disease (PMID: 27870574; NCT01004224). | 27870574 |
FGFR2 M537I FGFR2 V564L FGFR2 amp | cholangiocarcinoma | predicted - resistant | Infigratinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with cholangiocarcinoma with amplification of FGFR2 experienced disease progression after 3.9 months of treatment with Truseltiq (infigratinib) and was found to have acquired additional FGFR2 mutations, M537I and V564L (PMID: 34250419). | 34250419 |
FGFR1 T319A | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 T319A were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 I422V | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 I422V were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 K545del | cholangiocarcinoma | no benefit | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) did not decrease viability of a cholangiocarcinoma cell line expressing FGFR2 K545del in culture (PMID: 37964396). | 37964396 |
FGFR1 E592G | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 E592G were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 P582L | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 P582L were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 amp | head and neck carcinoma | predicted - sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase I trial, a patient with head and neck carcinoma harboring an FGFR1 amplification demonstrated a reduction in tumor size when treated with Truseltiq (infigratinib) (PMID: 27870574). | 27870574 |
FGFR2 V564M | Advanced Solid Tumor | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FGFR2 V564M were resistant to Truseltiq (infigratinib) in culture (PMID: 25349422). | 25349422 |
FGFR1 amp | synovial sarcoma | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited survival of FGFR1-amplified synovial sarcoma cells in culture (PMID: 27535980). | 27535980 |
FGFR2 amp | stomach cancer | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). | 30045926 |
FGFR2 amp | stomach cancer | sensitive | Infigratinib | Phase II | Actionable | In a Phase II trial (LB1001-201), Truseltiq (infigratinib) treatment in patients with advanced or metastatic gastric cancer or gastroesophageal junction adenocarcinoma with FGFR2 amplification resulted in a response rate of 25%, disease control rate of 80%, median duration of response of 3.8 months, median progression-free survival of 3.3 months, median overall survival of 8 months, with 15 of 19 patients experiencing tumor shrinkage (Ann Oncol 34 (2023): S761-S762; NCT05019794). | detail... |
FGFR2 amp | stomach cancer | sensitive | Infigratinib | Preclinical | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited proliferation of gastric cancer cell lines harboring FGFR2 amplification in culture (PMID: 26036639). | 26036639 |
FGFR2 amp FGFR2 over exp | stomach cancer | sensitive | Infigratinib | Preclinical - Pdx | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased Myc expression and inhibited tumor growth in patient-derived xenograft (PDX) models of gastric cancer with FGFR2 amplification and over expression (PMID: 27401245). | 27401245 |
FGFR3 V555L | transitional cell carcinoma | resistant | Infigratinib | Case Reports/Case Series | Actionable | In a clinical study, two patients with metastatic urothelial carcinoma progressed while being treated with Truseltiq (infigratinib) and subsequent cell-free DNA testing revealed FGFR3 V555L (also corresponds to V443L) (PMID: 29848605). | 29848605 |
FGFR2 W290_I291delinsC | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical | Actionable | In a preclinical study, Truseltiq (infigratinib) prevented oncogenic transformation of cells expressing FGFR2 W290_I291delinsC (PMID: 26048680). | 26048680 |
FGFR1 D320N | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 D320N were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 N549K | Advanced Solid Tumor | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 N549K were resistant to treatment with Truseltiq (infigratinib) in culture (PMID: 34272467). | 34272467 |
FGFR3 G380E | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G380E were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 mutant | cholangiocarcinoma | sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase I trial, a patient with cholangiocarcinoma harboring an FGFR2 mutation demonstrated a decreased tumor burden when treated with Truseltiq (infigratinib) (PMID: 27870574). | 27870574 |
FGFR1 M456V | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 M456V were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 A67V | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 A67V were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 V561F | Advanced Solid Tumor | resistant | Infigratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment failed to inhibit cell growth, Fgfr1 phosphorylation, and downstream pathway activation in cells expressing FGFR1 V561F in culture and failed to inhibit tumor growth in a cell line xenograft model with a tumor growth inhibition of 2.4% (PMID: 34114373). | 34114373 |
FGFR2 P303L | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 P303L were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 A268S | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 A268S were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 fusion FGFR2 E566A | intrahepatic cholangiocarcinoma | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 E566A had weakened sensitivity, as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). | 31109923 |
FGFR2 C382R | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 C382R were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 A121D | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 A121D were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 V392A | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 V392A were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 R251Q | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 R251Q were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 R330W | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 R330W were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 amp | lung non-small cell carcinoma | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited Erk signaling and growth of FGFR1-amplified non-small cell lung carcinoma cells in culture (PMID: 28630215). | 28630215 |
FGFR2 K659E | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 K659E were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 S436F | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 S436F were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 R189C | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 R189C were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 N546K | Advanced Solid Tumor | predicted - resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 N546K were resistant to treatment with Truseltiq (infigratinib) in culture (PMID: 34272467). | 34272467 |
FGFR2 fusion FGFR2 V565F | intrahepatic cholangiocarcinoma | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 V565F were resistant to treatment as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). | 31109923 |
FGFR2 L33S | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 L33S were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 K650N | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 K650N were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 S791T | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 S791T were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 P253R | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 P253R were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 fusion FGFR2 V564F | cholangiocarcinoma | predicted - resistant | Infigratinib | Case Reports/Case Series | Actionable | In a clinical case study, FGFR2 V564F was identified in the cell-free DNA of 3 cholangiocarcinoma patients harboring FGFR2 fusion after the patients progressed while on Truseltiq (infigratinib) treatment (PMID: 28034880). | 28034880 |
FGFR2 R203H | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 R203H were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 V564F | Advanced Solid Tumor | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR2 V564F were resistant to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
FGFR2 V564F | Advanced Solid Tumor | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FGFR2 V564F were resistant to Truseltiq (infigratinib) in culture (PMID: 25349422). | 25349422 |
FGFR2 N550K | endometrial cancer | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment induced cell death in an endometrial cancer cell line harboring FGFR2 N550K in culture (PMID: 30537101). | 30537101 |
FGFR1 A21T | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 A21T were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 G305R | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 G305R were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 fusion | cholangiocarcinoma | sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase I trial, two patients with cholangiocarcinoma harboring FGFR2 fusions demonstrated a decreased tumor burden when treated with Truseltiq (infigratinib) (PMID: 27870574). | 27870574 |
FGFR2 fusion | cholangiocarcinoma | sensitive | Infigratinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase II trial that supported FDA approval, Truseltiq (infigratinib) treatment demonstrated manageable toxicity, resulted in an objective response rate of 23.1% (25/108, 1 complete response, 24 partial responses) in patients with previously treated advanced cholangiocarcinoma harboring an FGFR2 fusion or rearrangement, with a median duration of response of 5.0 months and a median progression-free survival of 7.3 months (J Clin Oncol 39, no. 3_suppl (January 20, 2021) 265-265; NCT02150967). | detail... detail... detail... |
FGFR2 fusion | cholangiocarcinoma | sensitive | Infigratinib | Guideline | Actionable | Truseltiq (infigratinib) is included in guidelines as second or later-line therapy for patients with cholangiocarcinoma harboring FGFR2 fusions (PMID: 36372281; ESMO.org). | 36372281 detail... |
FGFR1 amp NRAS over exp | lung non-small cell carcinoma | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, overexpression of Nras in FGFR1-amplified non-small cell lung carcinoma cells resulted in decreased response to Truseltiq (infigratinib) in culture (PMID: 28630215). | 28630215 |
FGFR3 V555M | transitional cell carcinoma | resistant | Infigratinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with metastatic urothelial carcinoma progressed while being treated with Truseltiq (infigratinib) and subsequent cell-free DNA testing revealed FGFR3 V555M (also corresponds to V443M) (PMID: 29848605). | 29848605 |
FGFR3 Y373C | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 Y373C were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 E160K | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 E160K were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 E475K | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 E475K were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 R6P | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 R6P were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 H242Y | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 H242Y were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 I548Wfs*8 | cholangiocarcinoma | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased viability of a cholangiocarcinoma cell line expressing FGFR2 I548Wfs*8 in culture (PMID: 37964396). | 37964396 |
FGFR2 amp | colon cancer | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) reduced Myc expression, induced cell-cycle arrest, and inhibited growth of a colon cancer cell line with FGFR2 amplification in culture (PMID: 27401245). | 27401245 |
FGFR2 K660N | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of transformed cells expressing FGFR2 K660N in culture and inhibited tumor growth in xenograft models (PMID: 23786770). | 23786770 |
FGFR2 Q212K | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 Q212K were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 amp | breast cancer | predicted - sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase I trial, a breast cancer patient harboring an FGFR2 amplification demonstrated stable disease when treated with Truseltiq (infigratinib) (PMID: 27870574). | 27870574 |
FGFR1 D128N | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 D128N were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 fusion FGFR2 L618V | intrahepatic cholangiocarcinoma | resistant | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 L618V were resistant to treatment as demonstrated by cell viability and downstream signaling assays (PMID: 31109923). | 31109923 |
FGFR2 C383R | endometrial cancer | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 C383R in culture (PMID: 30537101). | 30537101 |
FGFR2 P253L | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 P253L were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 W290C | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of transformed cells expressing FGFR2 W290C in culture and inhibited tumor growth in xenograft models (PMID: 23786770). | 23786770 |
FGFR2 M640I | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 M640I were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 over exp | head and neck squamous cell carcinoma | sensitive | Infigratinib | Preclinical | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited cell growth and induced apoptosis in HNSCC cells over expressing Fgfr1 in culture and in xenograft models (PMID: 26015511). | 26015511 |
FGFR2 N631_M640del | cholangiocarcinoma | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased viability of a cholangiocarcinoma cell line expressing FGFR2 N631_M640del in culture (PMID: 37964396). | 37964396 |
FGFR2 R210Q | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 R210Q were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 N546K | diffuse midline glioma, H3 K27M-mutant | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited viability of mouse glioma cells expressing H3.3 K28M (reported as H3.3 K27M) and FGFR1 N546K (reported as N457K) in culture (PMID: 37011011). | 37011011 |
FGFR3 R248C | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of transformed cells expressing FGFR3 R248C in culture (PMID: 23786770). | 23786770 |
FGFR1 G703S | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 G703S were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 G613S | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 G613S were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 I288_D304del | cholangiocarcinoma | no benefit | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) did not decrease viability of a cholangiocarcinoma cell line expressing FGFR2 I288_D304del in culture (PMID: 37964396). | 37964396 |
FGFR2 N549S | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 N549S were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 T141R | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 T141R were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 R445W | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 R445W were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 S125L | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 S125L were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 mutant | transitional cell carcinoma | sensitive | Infigratinib | Phase I | Actionable | In a Phase I trial, Truseltiq (infigratinib) treatment resulted in complete response in 4% (1/25) and partial response in 32% (8/25) of urothelial carcinoma patients harboring FGFR3 mutations or fusions (J Clin Oncol 34, 2016 (suppl; abstr 4517); NCT01004224). | detail... |
FGFR3 mutant | transitional cell carcinoma | sensitive | Infigratinib | Clinical Study | Actionable | In a clinical study, Truseltiq (infigratinib) treatment in patients with FGFR3 alterations led to 25.4% (17/67) confirmed responses and a disease control rate of 64% (43/67), which included complete responses, partial responses, and stable disease, and resulted in a median progression-free survival of 3.75 months and a median overall survival of 7.75 months (PMID: 29848605). | 29848605 |
FGFR1 T26I | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 T26I were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 S249C | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) decreased viability of a cell line expressing FGFR3 S249C in culture (PMID: 32370101). | 32370101 |
FGFR3 S249C | Advanced Solid Tumor | sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, Truseltiq (infigratinib) inhibited growth of transformed cells expressing FGFR3 S249C in culture (PMID: 23786770). | 23786770 |
FGFR2 A371V | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 A371V were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 L560F | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 L560F were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 amp | myxoid liposarcoma | sensitive | Infigratinib | Preclinical | Actionable | In a preclinical study, Truseltiq (infigratinib) increased apoptosis, and inhibited cell proliferation and migration of myxoid liposarcoma cell lines harboring FGFR2 amplification in culture (PMID: 26036639). | 26036639 |
FGFR1 R250W | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 R250W were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 S131L | head and neck squamous cell carcinoma | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, a head and neck squamous cell carcinoma cell line expressing FGFR3 S131L demonstrated decreased sensitivity to Truseltiq (infigratinib) compared to cells expressing wild-type FGFR3 in culture (PMID: 27053219). | 27053219 |
FGFR3 V555L | Advanced Solid Tumor | decreased response | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells over expressing FGFR3 V555L demonstrated reduced sensitivity to Truseltiq (infigratinib) in culture (PMID: 28034880). | 28034880 |
FGFR3 G370C | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR3 G370C were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 H416R | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 H416R were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 K310R FGFR2 N550K | endometrial cancer | sensitive | Infigratinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Truseltiq (infigratinib) treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 N550K and K310R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 30537101). | 30537101 |
FGFR1 amp | breast cancer | sensitive | Infigratinib | Phase I | Actionable | In a Phase I trial, 28% (9/32) of breast cancer patients harboring FGFR1 amplification demonstrated stable disease when treated with Truseltiq (infigratinib) (PMID: 27870574). | 27870574 |
FGFR1 T340M | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 T340M were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR1 E467K | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR1 E467K were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR2 N82K | Advanced Solid Tumor | predicted - sensitive | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing FGFR2 N82K were sensitive to treatment with Truseltiq (infigratinib) in culture, demonstrating reduced cell viability (PMID: 34272467). | 34272467 |
FGFR3 K650E | high grade glioma | predicted - sensitive | Infigratinib | Case Reports/Case Series | Actionable | In a Phase II trial, Truseltiq (infigratinib) treatment resulted in limited efficacy with a 6-month progression-free survival (PFS) rate of 16.0%, a median PFS of 1.7 months, an objective response rate of 4.8% (1/21), and median overall survival of 6.7 months in patients with recurrent gliomas harboring alterations in FGFR1 or FGFR3, however, resulted in stable disease with PFS of 12.9 months in a patient harboring FGFR3 K650E (PMID: 35344029; NCT01975701). | 35344029 |
FGFR1 over exp | intrahepatic cholangiocarcinoma | no benefit | Infigratinib | Preclinical - Cell culture | Actionable | In a preclinical study, an intrahepatic cholangiocarcinoma cell line overexpressing FGFR1 was not sensitive to Truseltiq (infigratinib) in culture (PMID: 35420673). | 35420673 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01975701 | Phase II | Infigratinib | A Phase 2 Study of BGJ398 in Patients With Recurrent GBM | Completed | USA | NLD | ESP | CHE | BEL | AUS | 0 |
NCT02160041 | Phase II | Infigratinib | BGJ398 for Patients With Tumors With FGFR Genetic Alterations | Terminated | USA | 0 |
NCT04233567 | Phase II | Infigratinib | Infigratinib for the Treatment of Advanced or Metastatic Solid Tumors in Patients With FGFR Gene Mutations | Active, not recruiting | USA | 0 |
NCT04197986 | Phase III | Infigratinib | Study of Oral Infigratinib for the Adjuvant Treatment of Subjects With Invasive Urothelial Carcinoma With Susceptible FGFR3 Genetic Alterations | Terminated | USA | NLD | ITA | GRC | GBR | FRA | ESP | DEU | CAN | BGR | BEL | 0 |
NCT03773302 | Phase III | Cisplatin + Gemcitabine Infigratinib | Phase 3 Study of BGJ398 (Oral Infigratinib) in First Line Cholangiocarcinoma With FGFR2 Gene Fusions/Translocations | Terminated | USA | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUS | 6 |
NCT04228042 | Phase Ib/II | Infigratinib | Infigratinib Before Surgery for the Treatment of Upper Tract Urothelial Cancer | Completed | USA | 0 |
NCT01004224 | Phase I | Infigratinib | A Dose Escalation Study in Adult Patients With Advanced Solid Malignancies | Completed | USA | TUR | NLD | ITA | ISR | FRA | ESP | DEU | AUT | AUS | 4 |
NCT02312804 | Phase I | Paclitaxel Carboplatin Infigratinib | Ph Ib/BGJ398/Cervix and Other Solid Tumors | Withdrawn | 0 | |
NCT04424966 | Phase 0 | Infigratinib | Infigratinib in Recurrent High-Grade Glioma Patients | Terminated | USA | 0 |
NCT04972253 | Phase I | Infigratinib | Phase I BLASST-3 Trial ((BLASST)-3) | Withdrawn | 0 | |
NCT02150967 | Phase II | Infigratinib | A Phase II, Single Arm Study of BGJ398 in Patients With Advanced Cholangiocarcinoma | Terminated | USA | ITA | GBR | ESP | DEU | BEL | 5 |
NCT02706691 | Phase II | Infigratinib | Pan FGFR Kinase Inhibitor BGJ398 in Treating Patients With FGFR1-3 Translocated, Mutated, or Amplified Recurrent Head and Neck Cancer | Terminated | USA | 0 |
NCT05222165 | Phase Ib/II | Infigratinib | Study With Infigratinib in Subjects With Advanced Solid and CNS Tumors or Recurrent or Progressive Low-Grade Glioma With Selected FGFR1-3 Alterations (NEWEL) | Withdrawn | USA | DEU | CAN | 0 |
NCT05101564 | Phase II | Amcenestrant Alpelisib Infigratinib Tamoxifen Letrozole Amcenestrant + Letrozole | Umbrella Trial Testing Integrative Subtype Targeted Therapeutics in Estrogen Receptor Positive, HER2-Negative Breast Cancer | Active, not recruiting | USA | 0 |
NCT02657486 | Phase 0 | Infigratinib | BGJ398 in Non-Muscle-Invasive Urothelial Carcinoma of the Bladder | Active, not recruiting | USA | 0 |