Therapy Detail

Therapy Name TAS-120
Synonym
Therapy Description

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
TAS-120 FGFR Inhibitor (Pan) 18 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).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2-NRAP intrahepatic cholangiocarcinoma sensitive TAS-120 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
FGFR3 fusion Advanced Solid Tumor predicted - sensitive TAS-120 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 fusion FGFR2 N550K intrahepatic cholangiocarcinoma sensitive TAS-120 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 H683L FGFR2 L618V FGFR2 N550H FGFR2 N550T FGFR2 M538I intrahepatic cholangiocarcinoma sensitive TAS-120 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
Unknown unknown esophageal cancer not applicable TAS-120 Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in clinical response in an esophageal cancer patient (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 372PD). detail...
FGFR2 fusion FGFR2 M538I intrahepatic cholangiocarcinoma sensitive TAS-120 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 fusion FGFR2 L618V intrahepatic cholangiocarcinoma sensitive TAS-120 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
FGFR2 rearrange cholangiocarcinoma predicted - sensitive TAS-120 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...
FGFR2 fusion FGFR2 V565F intrahepatic cholangiocarcinoma resistant TAS-120 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
FGFR2 fusion FGFR2 K715R intrahepatic cholangiocarcinoma sensitive TAS-120 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
FGFR2 fusion FGFR2 E566A intrahepatic cholangiocarcinoma sensitive TAS-120 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
FGFR2 fusion FGFR2 H683L intrahepatic cholangiocarcinoma sensitive TAS-120 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
FGFR2 fusion FGFR2 K660M intrahepatic cholangiocarcinoma sensitive TAS-120 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-INA FGFR2 V565L FGFR2 E566A intrahepatic cholangiocarcinoma resistant TAS-120 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
FGFR2 fusion FGFR2 N550H intrahepatic cholangiocarcinoma sensitive TAS-120 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 fusion biliary tract cancer predicted - sensitive TAS-120 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-SORBS1 FGFR2 V565F intrahepatic cholangiocarcinoma resistant TAS-120 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 amp FGFR2 rearrange cholangiocarcinoma predicted - sensitive TAS-120 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-ZMYM4 FGFR2 V563L intrahepatic cholangiocarcinoma resistant TAS-120 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-SORBS1 FGFR2 K660M FGFR2 K715R intrahepatic cholangiocarcinoma sensitive TAS-120 Case Reports/Case Series Actionable In a Phase I trial, a patient with intrahepatic cholangiocarcinoma, harboring an FGFR2-SORBS1 fusion with FGFR2 K660M and K175R 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
Unknown unknown Advanced Solid Tumor not applicable TAS-120 Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in clinical response in 5.5% (2/36) and stable disease over 24 weeks in 5.5% (2/36) of patients with advanced solid tumors (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 372PD). detail...
FGFR2-KIAA1217 intrahepatic cholangiocarcinoma sensitive TAS-120 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 amp stomach cancer predicted - sensitive TAS-120 Phase I Actionable In a Phase I trial, 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-ZMYM4 FGFR2 V565F FGFR2 K660M FGFR2 E566A FGFR2 N550H FGFR2 N550K intrahepatic cholangiocarcinoma sensitive TAS-120 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
FGFR2-NRAP FGFR2 N550K intrahepatic cholangiocarcinoma resistant TAS-120 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 fusion cholangiocarcinoma predicted - sensitive TAS-120 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...
Unknown unknown urinary bladder cancer not applicable TAS-120 Phase I Actionable In a Phase I trial, TAS-120 treatment resulted in stable disease over 24 weeks in a bladder cancer patient (Ann Oncol 2017, Vol 28, Suppl 5, Abstract # 372PD). detail...
Clinical Trial Phase Therapies Title Recruitment Status
NCT02052778 Phase Ib/II TAS-120 A Study of TAS-120 in Patients With Advanced Solid Tumors Recruiting