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    DRUG CLASS:

    FGFR antagonist

    Associations

    News

    Trials
    over2years
    Evaluation of the Cytochrome P450 3A and P-glycoprotein Drug-Drug Interaction Potential of Futibatinib. (PubMed, Clin Pharmacol Drug Dev)
    Phase I studies investigated the drug-drug interactions of futibatinib with itraconazole (a dual P-gp and strong CYP3A inhibitor), rifampin (a dual P-gp and strong CYP3A inducer), or midazolam (a sensitive CYP3A substrate) in healthy adult participants. These findings suggest that concomitant use of dual P-gp and strong CYP3A inhibitors/inducers with futibatinib should be avoided, but futibatinib can be concomitantly administered with other drugs metabolized by CYP3A. Drug-drug interaction studies with P-gp-specific substrates and inhibitors are planned.
    Journal
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1)
    |
    FGFR2 fusion
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    Lytgobi (futibatinib) • itraconazole • midazolam hydrochloride • rifampicin
    over2years
    MC200402-Single-Arm Phase 2 Study of the FGFR Inhibitor Futibatinib in Combination with Pembrolizumab in Patients with FGF19 Expressing Advanced or Metastatic Hepatocellular Carcinoma (NCCN 2023)
    Hosted by NCCN Oncology Research Program (ORP)
    Clinical • P2 data • Combination therapy • Metastases
    |
    FGF19 (Fibroblast growth factor 19)
    |
    FGF19 expression
    |
    Keytruda (pembrolizumab) • Lytgobi (futibatinib)
    over2years
    The future of fibroblast growth factor receptor inhibitors and mechanisms of resistance for cholangiocarcinoma. (PubMed, Expert Opin Pharmacother)
    Infigratinib, futibatinib, and pemigatinib are being evaluated in an open phase III trial versus gemcitabine/cisplatin as first line treatment for locally advanced or metastatic CCA with FGFR GA (PROOF-301 NCT03773302, FOENIX-CCA3 NCT04093362, FIGHT-302 NCT03656536). Unfortunately, the effectiveness of FGFR therapy is often limited by acquired resistance mechanisms and continued work is needed to understand and overcome these mechanisms of resistance.
    Journal
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    FGFR (Fibroblast Growth Factor Receptor)
    |
    cisplatin • gemcitabine • Truseltiq (infigratinib) • Lytgobi (futibatinib) • Pemazyre (pemigatinib)
    over2years
    Phase 1b/2 Study of Futibatinib in Combination With Binimetinib in Patients With Advanced KRAS Mutant Cancer (clinicaltrials.gov)
    P1b/2, N=36, Active, not recruiting, Taiho Oncology, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed • Combination therapy • Metastases
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
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    Mektovi (binimetinib) • Lytgobi (futibatinib)
    over2years
    Futibatinib: A Potent and Irreversible Inhibitor of Fibroblast Growth Factor Receptors for Treatment of the Bile Duct Cancer. (PubMed, Curr Med Chem)
    The approval of this medicine was based on phase 3 clinical trial results including an overall response rate (ORR) of 42% and a duration of response (DoR) of 9.7 months. This short perspective summarizes Futibatinib's synthesis, physicochemical properties, dosage, route of administration, mechanism of action, binding mode, pharmacodynamics, pharmacokinetics, drug interactions, adverse events, and possible mechanism of resistance.
    Journal
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor)
    |
    FGFR2 mutation
    |
    Lytgobi (futibatinib)
    over2years
    FOENIX-CCA3: Futibatinib Versus Gemcitabine-Cisplatin Chemotherapy as First-Line Treatment of Patients With Advanced Cholangiocarcinoma Harboring FGFR2 Gene Rearrangements (clinicaltrials.gov)
    P3, N=216, Active, not recruiting, Taiho Oncology, Inc. | Trial completion date: Mar 2023 --> Sep 2023 | Trial primary completion date: Mar 2023 --> Sep 2023
    Trial completion date • Trial primary completion date • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 rearrangement
    |
    cisplatin • gemcitabine • Lytgobi (futibatinib)
    over2years
    FOENIX-MBC2 TAS-120-201: A Study of TAS-120 in Patients With Metastatic Breast Cancer (clinicaltrials.gov)
    P2, N=168, Active, not recruiting, Taiho Oncology, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • FGFR2 (Fibroblast growth factor receptor 2)
    |
    HER-2 amplification • HER-2 negative • FGFR1 amplification • FGFR2 amplification
    |
    fulvestrant • Lytgobi (futibatinib)
    almost3years
    Inhibition of FGFR4 with futibatinib combined with inhibition of IGF1R, Src family kinases, or AKT is synergistic against rhabdomyosarcoma (AACR 2023)
    The IC50 of futibatinib was ~500 nM for RMS559 and ~10 μM for RH4. Western blot showed that futibatinib inhibited FGFR4 phosphorylation in a dose dependent manner. The kinome activity assay found that futibatinib treatment resulted in SFK, AKT, and IGF1R activation.
    Late-breaking abstract
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    FGFR4 (Fibroblast growth factor receptor 4) • PAX3 (Paired Box 3)
    |
    FGFR4 mutation • FGFR4 overexpression • PAX3-FOXO1 fusion
    |
    Lytgobi (futibatinib)
    almost3years
    FOENIX-CCA4: Study of Futibatinib in Patients With Advanced Cholangiocarcinoma With FGFR2 Fusion or Rearrangement (clinicaltrials.gov)
    P2, N=120, Not yet recruiting, Taiho Oncology, Inc.
    New P2 trial
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 fusion • FGFR2 rearrangement
    |
    Lytgobi (futibatinib)
    almost3years
    FOENIX-CCA3: Futibatinib Versus Gemcitabine-Cisplatin Chemotherapy as First-Line Treatment of Patients With Advanced Cholangiocarcinoma Harboring FGFR2 Gene Rearrangements (clinicaltrials.gov)
    P3, N=216, Active, not recruiting, Taiho Oncology, Inc. | Recruiting --> Active, not recruiting | Trial completion date: Apr 2028 --> Mar 2023 | Trial primary completion date: Apr 2027 --> Mar 2023
    Enrollment closed • Trial completion date • Trial primary completion date • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 rearrangement
    |
    cisplatin • gemcitabine • Lytgobi (futibatinib)