{"entity":{"id":"tinengotinib","kind":"drug","name":"Tinengotinib","aka":[],"tldr":"A next-generation FGFR inhibitor designed to work after pemigatinib or futibatinib stop working, now in a global phase 3.","summary":"Tinengotinib is a type I multi-kinase inhibitor active against FGFR1-3, including the FGFR2 kinase-domain resistance mutations (N550, V565) that emerge after pemigatinib or futibatinib, plus VEGFR, Aurora and JAK kinases. It is aimed at FGFR-altered cholangiocarcinoma that has progressed on a prior FGFR inhibitor, a group with no approved targeted option. A phase 1/2 study in heavily pretreated patients, including after prior FGFR inhibitors, showed disease control with median PFS of about 5 to 6 months. The global phase 3 FIRST-308 trial randomises FGFR inhibitor-refractory patients to tinengotinib versus FOLFOX or FOLFIRI, primary endpoint PFS; the first US patient was dosed in 2025. Whether its broad kinase profile adds toxicity without benefit over selective FGFR2 inhibitors is open. For a newcomer, it is a drug for bile duct cancer that has outgrown the existing FGFR pills.","status":"phase-3","asOf":"2026-09-07","links":[{"label":"ClinicalTrials.gov NCT05948475: tinengotinib versus physician's choice in FGFR-altered cholangiocarcinoma (phase 3)","url":"https://clinicaltrials.gov/study/NCT05948475"},{"label":"ClinicalTrials.gov NCT05253053: TT-00420 (tinengotinib) monotherapy and combinations (phase 1/2)","url":"https://clinicaltrials.gov/study/NCT05253053"}],"tags":[],"related":[],"cancers":["cholangiocarcinoma"],"sections":[],"technologies":["kinase-inhibitors"],"targets":["fgfr2"],"drugs":[],"companies":["transthera"],"institutions":[],"pathways":[],"terms":["fgfr2-fusion"],"trials":["first-308","nct07052253","nct07498478","nct05948475"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"TT-00420","modality":"Small-molecule multi-kinase inhibitor (FGFR1-3, VEGFR, Aurora, JAK)","mechanism":"Type I inhibitor active against FGFR2 kinase-domain resistance mutations (N550, V565) plus VEGFR and Aurora kinases.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},"route":"/drugs/tinengotinib/","neighbours":{"cancer":[{"id":"cholangiocarcinoma","kind":"cancer","name":"Biliary tract cancer (cholangiocarcinoma)","route":"/cancers/cholangiocarcinoma/"},{"id":"intrahepatic-cholangiocarcinoma","kind":"cancer","name":"Intrahepatic cholangiocarcinoma","route":"/cancers/intrahepatic-cholangiocarcinoma/"}],"technology":[{"id":"kinase-inhibitors","kind":"technology","name":"Small-molecule kinase inhibitors","route":"/technologies/kinase-inhibitors/"}],"target":[{"id":"fgfr2","kind":"target","name":"FGFR2","route":"/targets/fgfr2/"}],"company":[{"id":"transthera","kind":"company","name":"TransThera Sciences","route":"/companies/transthera/"}],"term":[{"id":"fgfr2-fusion","kind":"term","name":"FGFR2 fusions and rearrangements","route":"/terms/fgfr2-fusion/"}],"trial":[{"id":"nct07052253","kind":"trial","name":"A Phase II Clinical Study of AK104/AK112 in Combination With TT-00420 Tablet for Advanced HCC.","route":"/trials/nct07052253/"},{"id":"nct07498478","kind":"trial","name":"Efficacy and Safety of Tinengotinib Tablets Combined With Fulvestrant Injection in Patients With HR Positive and HER-2 Negative Recurrent or Metastatic Breast Cancer Who Have Failed Prior Treatment","route":"/trials/nct07498478/"},{"id":"first-308","kind":"trial","name":"FIRST-308","route":"/trials/first-308/"},{"id":"nct05948475","kind":"trial","name":"Study of Tinengotinib VS. Physician's Choice a Treatment of Subjects With FGFR-altered in Cholangiocarcinoma","route":"/trials/nct05948475/"}],"idea":[{"id":"idea-btc-ctdna-fgfr-resistance","kind":"idea","name":"ctDNA-guided switching among FGFR inhibitors","route":"/ideas/idea-btc-ctdna-fgfr-resistance/"}]}}