Therapy Detail

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Therapy Name Futibatinib
Synonyms
Therapy Description

Futibatinib (TAS-120) is a third-generation pan-FGFR inhibitor, which result in the inhibition of FGFR-mediated signal transduction pathways and tumor cell proliferation (PMID: 31109923).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Futibatinib TAS-120 FGFR Inhibitor (Pan) 23 Futibatinib (TAS-120) is a third-generation pan-FGFR inhibitor, which result in the inhibition of FGFR-mediated signal transduction pathways and tumor cell proliferation (PMID: 31109923).

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR1 R250W Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 R250W were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 rearrange FGFR3 Y373C multiple myeloma sensitive Futibatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in a multiple myeloma cell line harboring an FGFR3 rearrangement and FGFR3 Y373C in culture, and led to tumor regression in a cell line xenograft model (PMID: 32973082). 32973082
FGFR2 R203H Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R203H were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 fusion intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Phase II Actionable In a Phase II trial (FOENIX-CCA2), Futibatinib (TAS-120) demonstrated manageable toxicity profile, resulted in an objective response rate (ORR) of 37.3% (25/67), a median duration of response of 8.3 months, and a disease control rate of 82% in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (82%) or other rearrangements (18%), ORR was 36.2% (21/58) in patients harboring FGFR2 fusions (Annals of Oncology (2020) 31 (suppl_4): S261-S262; NCT02052778). detail...
FGFR2 K659N Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 K659N were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 P582L Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 P582L were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 R210Q Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R210Q were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 E718K Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 E718K were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 C62Y Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 C62Y were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - SHTN1 FGFR2 L617M cholangiocarcinoma resistant Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 L617M demonstrated resistance to treatment with Futibatinib (TAS-120) in culture (PMID: 31911531). 31911531
FGFR1 amp Advanced Solid Tumor predicted - sensitive Futibatinib Phase I Actionable In a Phase I trial (FOENIX-101), Futibatinib (TAS-120) treatment demonstrated manageable safety profile, and resulted in a partial response in 6% (5/86) and stable disease in 48% (41/86) of patients with advanced solid tumors harboring FGF/FGFR aberrations, among whom 20% (15/74) harbored FGFR1 amplification (PMID: 32622884; NCT02052778). 32622884
BRAF L597Q FGFR2 H167_N173del FGFR2 L618F intrahepatic cholangiocarcinoma predicted - resistant Futibatinib Case Reports/Case Series Actionable In a clinical case study, acquisition of BRAF L597Q was identified in an intrahepatic cholangiocarcinoma patient harboring FGFR2 H167_N173del and FGFR2 L618F who developed resistance to treatment with Futibatinib (TAS-120) (PMID: 33926920). 33926920
FGFR2 fusion FGFR2 L618V intrahepatic cholangiocarcinoma sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 L618V were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR1 V751A Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 V751A were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - SORBS1 FGFR2 V565F intrahepatic cholangiocarcinoma resistant Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-SORBS1 fusion, responded to TAS-120 for 15.8 months before progressing due to an acquired FGFR2 V565F mutation, detected in cell-free DNA (PMID: 31109923; NCT02052778). 31109923
FGFR2 R203C Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R203C were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 A264T Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 A264T were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 Y375C Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR3 Y375C were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 S238N Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 S238N were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 fusion FGFR2 V565F intrahepatic cholangiocarcinoma resistant Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 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
FGFR3 fusion Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell line xenograft Actionable In a preclinical study, TAS-120 demonstrated growth inhibition and reduced FGFR phosphorylation in human cancer cell lines and xenograft models harboring FGFR mutations (Mol Cancer Ther 2013;12(11 Suppl):A270). detail...
FGFR2 R6P Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R6P were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 rearrange cholangiocarcinoma predicted - sensitive Futibatinib Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in partial response in 2 patients with cholangiocarcinoma harboring FGFR2 rearrangements (Annals of Oncology, Volume 29, Issue suppl_5). detail...
FGFR1 N546K Advanced Solid Tumor predicted - resistant Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 N546K were resistant to treatment with Futibatinib (TAS-120) in culture (PMID: 34272467). 34272467
FGFR2 V392A Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 V392A were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - SHTN1 FGFR2 E565A cholangiocarcinoma resistant Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with Futibatinib (TAS-120) in culture (PMID: 31911531). 31911531
FGFR2 fusion cholangiocarcinoma predicted - sensitive Futibatinib Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in an objective response rate of 25% (7/28, 7 partial responses) in patients with cholangiocarcinoma harboring FGFR2 fusions, with 71% of patients experienced tumor shrinkage, 54% (15/28) achieved stable disease (Annals of Oncology, Volume 29, Issue suppl_5). detail...
FGFR2 fusion FGFR2 N550H intrahepatic cholangiocarcinoma sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 N550H were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 N549H Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 N549H were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 H167_N173del intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) inhibited growth of an intrahepatic cholangiocarcinoma cell line expressing FGFR2 H167_N173del in culture (PMID: 33926920). 33926920
FGFR2 - INA FGFR2 V565L FGFR2 E566A intrahepatic cholangiocarcinoma resistant Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-INA fusion with FGFR2 H683L, L618V, N550H, N550T, M538I mutations, responded to TAS-120 for 5.1 months before progressing due to acquired FGFR2 V565L and E566A mutations, detected in cell-free DNA (PMID: 31109923; NCT02052778). 31109923
FGFR1 A121D Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 A121D were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 - TACC3 stomach cancer predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment led to an overall objective response rate of 22% (2/9, 2 partial responses) and a disease control rate of 55.6% (5/9) in patients with gastric cancer harboring an FGFR2 amplification or FGFR3 rearrangement, including a partial response with a progression-free survival of 6.7 months and a duration of response of 5.4 months in a gastric cancer patient harboring FGFR3-TACC3 (PMID: 34551969; NCT02052778). 34551969
FGFR2 S252W endometrial cancer predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in an endometrial cancer cell line harboring FGFR2 S252W in culture (PMID: 32973082). 32973082
FGFR3 K650N Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR3 K650N were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 fusion FGFR2 K715R intrahepatic cholangiocarcinoma sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 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 (PMID: 31109923). 31109923
FGFR1 M563I FGFR1 K687E oligodendroglioma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial (FOENIX-101), Futibatinib (TAS-120) treatment resulted in a partial response in a patient with anaplastic oligodendroglioma harboring FGFR1 M563I and FGFR1 K687E (PMID: 32622884; NCT02052778). 32622884 detail... detail...
FGFR2 K310R Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 K310R were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 amp breast cancer predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in a breast cancer cell line harboring FGFR1 amplification in culture (PMID: 32973082). 32973082
FGFR2 C383R intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment at a dose of 20mg led to an objective response rate of 15.6% (10/64) and a median progression-free survival of 5.1 months in patients with cholangiocarcinoma harboring FGF or FGFR 1-4 alterations, including a partial response with a progression-free survival of 9.2 months and a duration of response of 6.5 months in a patient with intrahepatic cholangiocarcinoma harboring FGFR2 C383R (PMID: 34551969; NCT02052778). 34551969
FGFR1 T340M Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 T340M were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 M640I Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 M640I were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - BICC1 intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial (FOENIX-101), Futibatinib (TAS-120) treatment resulted in a partial response in two patients with intrahepatic cholangiocarcinoma harboring FGFR2-BICC1 fusion (PMID: 32622884; NCT02052778). 32622884
FGFR2 - BICC1 intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase II trial (FOENIX-CCA2), Futibatinib (TAS-120) demonstrated manageable toxicity profile, resulted in an objective response rate (ORR) of 37.3% (25/67), a median duration of response of 8.3 months, and a disease control rate of 82% in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (82%) or other rearrangements (18%), ORR was 33.3% (5/15) in patients harboring FGFR2-BICC1 fusion (Annals of Oncology (2020) 31 (suppl_4): S261-S262; NCT02052778). detail...
FGFR1 D133N Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 D133N were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 N82K Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 N82K were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - NRAP FGFR2 N550K intrahepatic cholangiocarcinoma resistant Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-NRAP fusion responded to TAS-120 for 17.2 months before progressing due to an acquired FGFR2 N550K mutation, detected in cell-free DNA and the tumor biopsy (PMID: 31109923; NCT02052778). 31109923
FGFR2 G305R Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 G305R were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 H242Y Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 H242Y were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 fusion FGFR2 M538I intrahepatic cholangiocarcinoma sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 M538I were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 R664W Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R664W were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - WAC intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment at a dose of 16mg led to a partial response in 42.1% (8/19) of patients with intrahepatic cholangiocarcinoma harboring FGF or FGFR alterations, including a partial response with a progression-free survival of 6.9 months and a duration of response of 4.2 months in a patient harboring FGFR2-WAC (PMID: 34551969; NCT02052778). 34551969
FGFR1 S436F Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 S436F were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 A371V Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 A371V were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 R809Q Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 R809Q were sensitive to treatment with Pemazyre (pemigatinib) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 over exp stomach cancer sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) treatment inhibited growth of FGFR1-overexpressing gastric cancer cells in culture (PMID: 33563752). 33563752
FGFR1 T141R Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 T141R were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 E160K Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 E160K were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - SORBS1 intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial (FOENIX-101), Futibatinib (TAS-120) treatment resulted in a partial response in a patient with intrahepatic cholangiocarcinoma harboring FGFR2-SORBS1 fusion (PMID: 32622884; NCT02052778). 32622884
FGFR2 fusion FGFR2 K660M intrahepatic cholangiocarcinoma sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 K660M were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 S791T Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 S791T were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - CCDC6 intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment at a dose of 16mg led to a partial response in 42.1% (8/19) of patients with intrahepatic cholangiocarcinoma harboring FGF or FGFR alterations, including a partial response with a progression-free survival of 6.8 months and a duration of response of 8.8 months in a patient harboring FGFR2-CCDC6 (PMID: 34551969; NCT02052778). 34551969
FGFR3 rearrange NRAS act mut multiple myeloma no benefit Futibatinib Preclinical - Cell culture Actionable In a preclinical study, a multiple myeloma cell line harboring an FGFR3 rearrangement and an NRAS activating mutation was not sensitive to treatment with Futibatinib (TAS-120) in culture (PMID: 32973082). 32973082
FGFR1 K656N Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) inhibited growth of a cell line expressing FGFR1 K656N in culture (PMID: 34114373). 34114373
FGFR2 rearrange FGFR2 amp cholangiocarcinoma predicted - sensitive Futibatinib Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in partial response in a patient with cholangiocarcinoma harboring FGFR2 rearrangement and FGFR2 amplification (Annals of Oncology, Volume 29, Issue suppl_5). detail...
FGFR2 W290C Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 W290C were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 D128V Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 D128V were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 S252W Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 S252W were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 E475K Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 E475K were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 P253R Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 P253R were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 fusion FGFR2 E566A intrahepatic cholangiocarcinoma sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 E566A were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR1 amp lung cancer predicted - sensitive Futibatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in lung cancer cell lines harboring FGFR1 amplification in culture, and led to inhibition of tumor growth in a cell line xenograft model with a daily dosing regimen, but not with an intermittent dosing regimen (PMID: 32973082). 32973082
FGFR1 - TACC1 glioblastoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment led to a partial response lasting 5.8 months and progression-free survival of 7.0 months in a glioblastoma patient harboring FGFR1-TACC1 (PMID: 34551969; NCT02052778). 34551969
FGFR2 L33S Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 L33S were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 A67V Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 A67V were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 M186T Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 M186T were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 rearrange intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase II trial (FOENIX-CCA2), Futibatinib (TAS-120) demonstrated manageable toxicity profile, resulted in an objective response rate (ORR) of 37.3% (25/67), a median duration of response of 8.3 months, and a disease control rate of 82% in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (82%) or other rearrangements (18%), ORR was 44.4% (4/9) in patients harboring FGFR2 rearrangements (Annals of Oncology (2020) 31 (suppl_4): S261-S262; NCT02052778). detail...
FGFR2 - AHCYL1 Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2-AHCYL1 were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 fusion Advanced Solid Tumor predicted - sensitive Futibatinib Phase I Actionable In a Phase I trial (FOENIX-101), Futibatinib (TAS-120) treatment demonstrated manageable safety profile, and resulted in a partial response in 6% (5/86) and stable disease in 48% (41/86) of patients with advanced solid tumors harboring FGF/FGFR aberrations, among whom 20% (15/74) harbored FGFR2 fusions (PMID: 32622884; NCT02052778). 32622884
FGFR2 N549S Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 N549S were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 A389T Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 A389T were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - PPHLN1 Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2-PPHLN1 were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 H544Q Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 H544Q were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - SORBS1 FGFR2 K660M FGFR2 K715R intrahepatic cholangiocarcinoma sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-SORBS1 fusion with FGFR2 K660M and K715R mutations, responded to TAS-120 for 15.8 months before progressing due to an acquired FGFR2 V565F mutation, detected in cell-free DNA (PMID: 31109923; NCT02052778). 31109923
FGFR2 R251Q Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R251Q were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 R399Q Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R399Q were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 M563T intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment led to an overall objective response rate of 15.8% (3/19, 3 partial responses) and a disease control rate of 47.4% (9/19), with stable disease in 6, in patients with urothelial cancer harboring an FGFR3 mutation or FGFR1 mutation, including a partial response with a progression-free survival of 6.8 mo and a duration of response of 5.6 mo in a urothelial cancer patient harboring FGFR1 M563T and amplifications in FGF3 and FGF19 (PMID: 34551969; NCT02052778). 34551969
FGFR2 amp breast cancer predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment resulted in a partial response in a patients with breast cancer harboring FGFR2 amplification, with 37% tumor shrinkage (Annals of Oncology (2020) 31 (suppl_4): S475). detail...
FGFR2 - TTC28 intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment at a dose of 16mg led to a partial response in 42.1% (8/19) of patients with intrahepatic cholangiocarcinoma harboring FGF or FGFR alterations, including a partial response with a progression-free survival of 24.1 months and a duration of response of 12.7 months in a patient harboring FGFR2-TTC28 (PMID: 34551969; NCT02052778). 34551969
FGFR2 L560F Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 L560F were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 fusion FGFR2 N550K intrahepatic cholangiocarcinoma sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 N550K were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR2 - INA FGFR2 M538I FGFR2 N550H FGFR2 N550T FGFR2 L618V FGFR2 H683L intrahepatic cholangiocarcinoma sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-INA fusion with FGFR2 H683L, L618V, N550H, N550T, M538I mutations, responded to TAS-120 for 5.1 months before progressing due to acquired FGFR2 V565L and E566A mutations, detected in cell-free DNA (PMID: 31109923; NCT02052778). 31109923
FGFR3 - TACC3 FGFR3 over exp urinary bladder cancer sensitive Futibatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in bladder cancer cell lines with FGFR3 overexpression and harboring FGFR3-TACC3 in culture, and led to inhibition of tumor growth in a cell line xenograft model (PMID: 32973082). 32973082
FGFR2 R330W Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R330W were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 G364E Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 G364E were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 T26I Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 T26I were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 amp FGFR2 amp breast cancer sensitive Futibatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in breast cancer cell lines harboring FGFR1 and FGFR2 amplification in culture, and led to inhibition of tumor growth in a cell line xenograft model (PMID: 32973082). 32973082
FGFR2 fusion FGFR2 H683L intrahepatic cholangiocarcinoma sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, TAS-120 treatment of intrahepatic cholangiocarcinoma cells with an FGFR2 fusion in context with FGFR2 H683L were sensitive to treatment as demonstrated by decreased cell viability and decreased activation of downstream signaling (PMID: 31109923). 31109923
FGFR1 R475Q Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 R475Q were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - NRAP intrahepatic cholangiocarcinoma sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-NRAP fusion responded to TAS-120 for 17.2 months before progressing due to an acquired FGFR2 N550K mutation, detected in cell-free DNA and the tumor biopsy (PMID: 31109923; NCT02052778). 31109923
FGFR2 - SHTN1 Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FGFR2-SHTN1 were sensitive to treatment with Futibatinib (TAS-120), demonstrating decreased cell viability in culture (PMID: 31911531). 31911531
FGFR1 M456V Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 M456V were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 N549K endometrial cancer predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in an endometrial cancer cell line harboring FGFR2 N549K in culture (PMID: 32973082). 32973082
FGFR2 amp stomach cancer predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) treatment inhibited growth of gastric cancer cells harboring FGFR2 amplification in culture (PMID: 33563752). 33563752
FGFR2 amp stomach cancer predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment resulted in a partial response in 2 patients with gastric cancer harboring FGFR2 amplification, with 59% and 90% tumor shrinkage, respectively (Annals of Oncology (2020) 31 (suppl_4): S475). detail...
FGFR2 amp stomach cancer predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment led to an overall objective response rate of 22% (2/9, 2 partial responses) and a disease control rate of 55.6% (5/9) in patients with gastric cancer harboring an FGFR2 amplification or FGFR3 rearrangement, including a progression-free survival of 4.8 months and a duration of response of 3.5 months in a patient with FGFR2 amplification (PMID: 34551969; NCT02052778). 34551969
FGFR2 amp stomach cancer predicted - sensitive Futibatinib Phase I Actionable In a Phase I trial, Futibatinib (TAS-120) treatment resulted in clinical response in a gastric cancer patient harboring FGFR2 amplification (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 372PD). detail...
FGFR2 - CCDC6 Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2-CCDC6 were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 K659E Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 K659E were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 P303L Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 P303L were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 V561F Advanced Solid Tumor predicted - resistant Futibatinib Preclinical - Cell culture Actionable In a preclinical study, treatment with Futibatinib (TAS-120) failed to inhibit cell growth and Fgfr1 downstream signaling in cells expressing FGFR1 V561F in culture (PMID: 34114373). 34114373
FGFR2 - SHTN1 cholangiocarcinoma sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cholangiocarcinoma cells expressing FGFR2-SHTN1 were sensitive to treatment with Futibatinib (TAS-120), demonstrating decreased cell viability in culture (PMID: 31911531). 31911531
FGFR2 amp Advanced Solid Tumor predicted - sensitive Futibatinib Phase I Actionable In a Phase I trial (FOENIX-101), Futibatinib (TAS-120) treatment demonstrated manageable safety profile, and resulted in a partial response in 6% (5/86) and stable disease in 48% (41/86) of patients with advanced solid tumors harboring FGF/FGFR aberrations, among whom 5% (4/74) harbored FGFR2 amplification (PMID: 32622884; NCT02052778). 32622884
FGFR1 N546D intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial (FOENIX-101), Futibatinib (TAS-120) treatment resulted in a partial response in a patient with glioblastoma harboring FGFR1 N546D (PMID: 32622884; NCT02052778). 32622884
FGFR2 W290C intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment at a dose of 20mg led to an objective response rate of 15.6% (10/64) and a median progression-free survival of 5.1 months in patients with cholangiocarcinoma harboring FGF or FGFR 1-4 alterations, including a partial response with a progression-free survival of 12.7 months and a duration of response of 9.9 months in an intrahepatic cholantiocarcinoma patient harboring FGFR2 W290C (PMID: 34551969; NCT02052778). 34551969
FGFR2 I422V Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 I422V were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 A21T Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 A21T were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 C382R Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 C382R were sensitive to treatment with Pemazyre (pemigatinib) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 S588T Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 S588T were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 Q212K Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 Q212K were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 E467K Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 E467K were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - TNS1 intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment at a dose of 16mg led to a partial response in 42.1% (8/19) of patients with intrahepatic cholangiocarcinoma harboring FGF or FGFR alterations, including a partial response with a progression-free survival of 11 months and a duration of response of 9.1 months in a patient harboring FGFR2-TNS1 (PMID: 34551969; NCT02052778). 34551969
FGFR2 K310R FGFR2 N549K endometrial cancer predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in an endometrial cancer cell line harboring FGFR2 K310R and FGFR2 N549K in culture (PMID: 32973082). 32973082
FGFR1 K656E Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) inhibited growth of a cell line expressing FGFR1 K656E in culture (PMID: 34114373). 34114373
FGFR2 E596K Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 E596K were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - ZMYM4 FGFR2 N550H FGFR2 N550K FGFR2 V565F FGFR2 E566A FGFR2 K660M intrahepatic cholangiocarcinoma sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-ZMYM4 fusion with FGFR2 V565F, K660M E566A, N550H, and N550K mutations, responded to TAS-120 for 7.2 months before progressing due to an acquired FGFR2 V563L mutation, detected in cell-free DNA (PMID: 31109923; NCT02052778). 31109923
FGFR1 S125L Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 S125L were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 G613S Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 G613S were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 H167_N173del FGFR2 L618F intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment led to a partial response with 61% tumor reduction and response duration of 17 months in an intrahepatic cholangiocarcinoma patient harboring FGFR2 H167_N173del and FGFR2 L618F, which was consistent with inhibition of growth in an intrahepatic cholangiocarcinoma cell line expressing FGFR2 H167_N173del and FGFR2 L618F in culture (PMID: 33926920). 33926920
FGFR3 S249C transitional cell carcinoma predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment led to an overall objective response rate of 15.8% (3/19, 3 partial responses) and a disease control rate of 47.4% (9/19), with stable disease in 6, in urothelial cancer patients harboring an FGFR3 mutation or FGFR1 mutation, including partial responses in 2 patients with urothelial cancer harboring FGFR3 S249C with a progression-free survival of 2.7 and 4.7 mo, and a duration of response of 1.4 and 3.4 mo, respectively (PMID: 34551969; NCT02052778). 34551969
FGFR2 P253L Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 P253L were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 rearrange FGFR3 F384L multiple myeloma no benefit Futibatinib Preclinical - Cell culture Actionable In a preclinical study, a multiple myeloma cell line harboring an FGFR3 rearrangement and FGFR3 F384L was not sensitive to treatment with Futibatinib (TAS-120) in culture (PMID: 32973082). 32973082
FGFR2 amp triple-receptor negative breast cancer predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment led to a partial response lasting 20.8 months and progression-free survival of 22.1 months in a triple-receptor negative breast cancer patient harboring an FGFR2 amplification (PMID: 34551969; NCT02052778). 34551969
FGFR2 - PHGDH intrahepatic cholangiocarcinoma predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) inhibited growth of an intrahepatic cholangiocarcinoma cell line expressing FGFR2-PHGDH in culture PMID: 33926920). 33926920
FGFR2 H416R Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 H416R were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 P483L Advanced Solid Tumor predicted - resistant Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 P483L were resistant to treatment with Futibatinib (TAS-120) in culture (PMID: 34272467). 34272467
FGFR2 fusion biliary tract cancer predicted - sensitive Futibatinib Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in stable disease over 24 weeks in two biliary tract cancer patients harboring FGFR2 fusions (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 372PD). detail...
FGFR2 N549D Advanced Solid Tumor sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 N549D were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 amp head and neck cancer predicted - sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment led to a partial response lasting 5.6 months and progression-free survival of 6.9 months in a head and neck cancer patient harboring FGFR1-PLAG1 (PMID: 34551969; NCT02052778). 34551969
FGFR2 - ZMYM4 FGFR2 V563L intrahepatic cholangiocarcinoma resistant Futibatinib Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-SORBS1 fusion with FGFR2 V565F, K660M E566A, N550H, and N550K mutations, responded to TAS-120 for 7.2 months before progressing due to an acquired FGFR2 V563L mutation, detected in cell-free DNA and tumor biopsy (PMID: 31109923; NCT02052778). 31109923
FGFR2 E163K Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 E163K were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 G227E Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 G227E were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 D101Y Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 D101Y were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 - SHTN1 FGFR2 E565A Advanced Solid Tumor resistant Futibatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing both FGFR2-SHTN1 and FGFR2 E565A demonstrated resistance to treatment with Futibatinib (TAS-120) in culture (PMID: 31911531). 31911531
FGFR3 rearrange FGFR3 K650E multiple myeloma predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, Futibatinib (TAS-120) treatment led to inhibition of cell proliferation in a multiple myeloma cell line harboring an FGFR3 rearrangement and FGFR3 K650E in culture (PMID: 32973082). 32973082
FGFR1 V561M Advanced Solid Tumor predicted - resistant Futibatinib Preclinical - Cell culture Actionable In a preclinical study, treatment with Futibatinib (TAS-120) failed to inhibit cell growth and Fgfr1 downstream signaling in cells expressing FGFR1 V561M in culture (PMID: 34114373). 34114373
FGFR2 - KIAA1217 intrahepatic cholangiocarcinoma sensitive Futibatinib Preclinical - Pdx Actionable In a preclinical study, TAS-120 treatment of an intrahepatic cholangiocarcinoma patient-derived xenograft model, harboring an FGFR2-KIAA1217 fusion, decreased tumor growth and suppressed MEK/ERK signaling (PMID: 31109923). 31109923
FGFR2 - KIAA1217 intrahepatic cholangiocarcinoma sensitive Futibatinib Case Reports/Case Series Actionable In a Phase I trial, Futibatinib (TAS-120) treatment at a dose of 16mg led to a partial response in 42.1% (8/19) of patients with intrahepatic cholangiocarcinoma harboring FGF or FGFR alterations, including a partial response with a progression-free survival of 6.8 months and a duration of response of 5.6 months in a patient harboring FGFR2-KIAA1217 (PMID: 34551969; NCT02052778). 34551969
FGFR1 D320N Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 D320N were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 Y328N Advanced Solid Tumor predicted - sensitive Futibatinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 Y328N were sensitive to treatment with Futibatinib (TAS-120) in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT04024436 Phase II Fulvestrant + Futibatinib Futibatinib A Study of TAS-120 in Patients With Metastatic Breast Cancer Recruiting USA | ITA | FRA | ESP | CAN 2
NCT02052778 Phase Ib/II Futibatinib A Study of TAS-120 in Patients With Advanced Solid Tumors Active, not recruiting USA | ITA | FRA | ESP | DEU | CAN 7
NCT04189445 Phase II Futibatinib Futibatinib in Patients With Specific FGFR Aberrations Recruiting USA | ITA | FRA | ESP | DEU | BEL 9
NCT04093362 Phase III Futibatinib Cisplatin + Gemcitabine Futibatinib Vs Gemcitabine-Cisplatin Chemotherapy as 1st-Line Treatment of Patients With Advanced Cholangiocarcinoma (CCA) Harboring FGFR2 Gene Rearrangements (FOENIX-CCA3) Recruiting USA | ITA | FRA | ESP | DEU | BEL 14
NCT03784014 Phase III Ceritinib Dabrafenib + Trametinib Capmatinib Durvalumab + Olaparib Nilotinib Futibatinib Trametinib Palbociclib Glasdegib Lapatinib Molecular Profiling of Advanced Soft-tissue Sarcomas (MULTISARC) Recruiting FRA 0
NCT04507503 Expanded access Futibatinib Expanded Access Study of TAS-120 in Patients With Advanced Cholangiocarcinoma Harboring FGFR2 Gene Rearrangements Available USA 0


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