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    DRUG:

    vepugratinib (LY3866288)

    i
    Other names: LY3866288, LY-3866288, LY 3866288, LOXO435, LOXO-435, LOXO 435, LOX-24350, LOX 24350, LOX24350
    Associations

    News

    Trials
    Company:
    Eli Lilly
    Drug class:
    FGFR3 inhibitor
    Related drugs:
    Associations

    News

    Trials
    30d
    FORAGER-2: A Study of Vepugratinib (LY3866288) in Participants With Cancer in the Urinary Tract (clinicaltrials.gov)
    P3, N=450, Recruiting, Eli Lilly and Company | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Keytruda (pembrolizumab) • Padcev (enfortumab vedotin-ejfv) • vepugratinib (LY3866288)
    3ms
    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
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR (Fibroblast Growth Factor Receptor) • FGFR4 (Fibroblast growth factor receptor 4)
    |
    Balversa (erdafitinib) • Lytgobi (futibatinib) • Pemazyre (pemigatinib) • lirafugratinib (RLY-4008) • dabogratinib (TYRA-300) • ABSK061 • vepugratinib (LY3866288)
    3ms
    FORAGER-2: A Study of Vepugratinib (LY3866288) in Participants With Cancer in the Urinary Tract (clinicaltrials.gov)
    P3, N=450, Not yet recruiting, Eli Lilly and Company
    New P3 trial
    |
    Keytruda (pembrolizumab) • Padcev (enfortumab vedotin-ejfv) • vepugratinib (LY3866288)
    9ms
    FORAGER-1: A Study of LOXO-435 (LY3866288) in Participants With Cancer With a Change in a Gene Called FGFR3 (clinicaltrials.gov)
    P1, N=535, Recruiting, Eli Lilly and Company | Trial completion date: Jun 2025 --> Jun 2027 | Trial primary completion date: Jun 2025 --> Jun 2027
    Trial completion date • Trial primary completion date
    |
    Keytruda (pembrolizumab) • Padcev (enfortumab vedotin-ejfv) • vepugratinib (LY3866288)
    10ms
    FORAGER-1: A Study of LOXO-435 (LY3866288) in Participants With Cancer With a Change in a Gene Called FGFR3 (clinicaltrials.gov)
    P1, N=535, Recruiting, Eli Lilly and Company | N=180 --> 535
    Enrollment change
    |
    Keytruda (pembrolizumab) • Padcev (enfortumab vedotin-ejfv) • vepugratinib (LY3866288)
    10ms
    A Study of LY3866288 in Healthy Participants (clinicaltrials.gov)
    P1, N=15, Completed, Eli Lilly and Company | N=30 --> 15 | Recruiting --> Completed
    Trial completion • Enrollment change
    |
    vepugratinib (LY3866288)
    12ms
    A Study of [14C]-LY3866288 in Healthy Participants (clinicaltrials.gov)
    P1, N=15, Completed, Eli Lilly and Company | Recruiting --> Completed
    Trial completion
    |
    vepugratinib (LY3866288)
    1year
    A Study of [14C]-LY3866288 in Healthy Participants (clinicaltrials.gov)
    P1, N=16, Recruiting, Eli Lilly and Company | Not yet recruiting --> Recruiting
    Enrollment open
    |
    vepugratinib (LY3866288)
    1year
    A Study of LY3866288 in Healthy Participants (clinicaltrials.gov)
    P1, N=30, Recruiting, Eli Lilly and Company | Not yet recruiting --> Recruiting
    Enrollment open
    |
    vepugratinib (LY3866288)
    over1year
    A Study of [14C]-LY3866288 in Healthy Participants (clinicaltrials.gov)
    P1, N=16, Not yet recruiting, Eli Lilly and Company
    New P1 trial
    |
    vepugratinib (LY3866288)
    over1year
    A Study of LY3866288 in Healthy Participants (clinicaltrials.gov)
    P1, N=30, Not yet recruiting, Eli Lilly and Company
    New P1 trial
    |
    vepugratinib (LY3866288)
    almost2years
    FGFR-targeted therapeutics: clinical activity, mechanisms of resistance and new directions. (PubMed, Nat Rev Clin Oncol)
    Various agents, including pan-FGFR inhibitors (erdafitinib and futibatinib), FGFR1/2/3 inhibitors (infigratinib and pemigatinib), as well as a range of more-specific agents, have been developed and several have entered clinical use. The next generation of small-molecule inhibitors, such as lirafugratinib and LOXO-435, and the FGFR2-specific antibody bemarituzumab are expected to have a reduced risk of hyperphosphataemia and the ability to overcome certain resistance mutations. In this Review, we describe the development and current clinical role of FGFR inhibitors and provide perspective on future research directions including expansion of the therapeutic indications for use of FGFR inhibitors, combination of these agents with immune-checkpoint inhibitors and the application of novel technologies, such as artificial intelligence.
    Review • Journal
    |
    TP53 (Tumor protein P53) • FGFR2 (Fibroblast growth factor receptor 2) • FGFR (Fibroblast Growth Factor Receptor)
    |
    TP53 mutation • FGFR2 fusion • FGFR mutation • FGFR1 fusion
    |
    Balversa (erdafitinib) • Truseltiq (infigratinib) • Lytgobi (futibatinib) • Pemazyre (pemigatinib) • bemarituzumab (AMG 552) • lirafugratinib (RLY-4008) • vepugratinib (LY3866288)