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    1m
    Next-generation isoform-selective fibroblast growth factor receptor inhibitors. (PubMed, Trends Pharmacol Sci)
    Pan-FGFR-selective inhibitors (erdafitinib, pemigatinib, and futibatinib) have been developed in clinical practice...FGFR2-selective inhibitor lirafugratinib, FGFR3-selective inhibitors LOXO-435 and TYRA-300, FGFR2/3-selective inhibitor ABSK061, and FGFR4-selective inhibitors are in clinical development. Additionally, novel isoform-selective FGFR-targeting degraders, FGFR2b/FGFR3-selective antibodies, and de novo-designed 'c' isoform-selective proteins provide novel treatment strategies. This review provides an overview of the current FGFR-targeted therapeutics and limitations and evaluates next-generation inhibitor development to guide future research.
    Review • Journal
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    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR (Fibroblast Growth Factor Receptor) • FGFR4 (Fibroblast growth factor receptor 4)
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    Balversa (erdafitinib) • Lytgobi (futibatinib) • Pemazyre (pemigatinib) • lirafugratinib (RLY-4008) • dabogratinib (TYRA-300) • ABSK061 • vepugratinib (LY3866288)
    6ms
    A Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of ABSK061 Mini-tablets in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=42, Recruiting, Abbisko Therapeutics Co, Ltd
    New P1 trial
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    ABSK061
    1year
    A Phase 2 Clinical Study of ABSK061 and ABSK043 (clinicaltrials.gov)
    P2, N=202, Recruiting, Abbisko Therapeutics Co, Ltd | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
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    HER-2 (Human epidermal growth factor receptor 2) • FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
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    FGFR3 overexpression • FGF3 overexpression
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    ABSK043 • ABSK061
    1year
    A Phase 2 Clinical Study of ABSK061 and ABSK043 (clinicaltrials.gov)
    P2, N=202, Not yet recruiting, Abbisko Therapeutics Co, Ltd
    New P2 trial • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
    |
    FGFR3 overexpression • FGF3 overexpression
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    ABSK043 • ABSK061
    over3years
    A Study to Assess Safety, Tolerability, and Pharmacokinetics of ABSK061 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=85, Recruiting, Abbisko Therapeutics Co, Ltd | Not yet recruiting --> Recruiting | Initiation date: Mar 2022 --> Jun 2022
    Enrollment open • Trial initiation date
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    FGFR2 (Fibroblast growth factor receptor 2)
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    FGFR2 mutation • FGFR2 fusion • FGFR3 mutation • FGFR3 fusion
    |
    ABSK061
    almost4years
    A Study to Assess Safety, Tolerability, and Pharmacokinetics of ABSK061 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=85, Not yet recruiting, Abbisko Therapeutics Co, Ltd
    New P1 trial
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR3 mutation • FGFR3 fusion
    |
    ABSK061