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Vepugratinib · LY3866288, LOXO-435

Small molecule · Inhibitor of fibroblast growth factor receptor 3 (FGFR3) · developed by ELI LILLY &

Phase 2 Most advanced trial

LLY Developer

1 Registered trials

What is Vepugratinib?

Vepugratinib is an orally bioavailable, selective inhibitor of the receptor tyrosine kinase FGFR3, including FGFR3 gatekeeper resistance mutations. It blocks FGFR3-mediated signaling and is being studied in urinary bladder neoplasms and other urologic neoplasms.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as: LY3866288, LOXO-435
Drug type: Small molecule
Targets: fibroblast growth factor receptor 3 (FGFR3)
Mechanism: Inhibitor of fibroblast growth factor receptor 3 (FGFR3)
Pathways: FGFR3-mediated signaling, angiogenesis, tumor cell proliferation, differentiation and survival
Therapy area: Oncology
Developer: ELI LILLY & (LLY)
FDA status: Investigational, not approved in the US. Most advanced trial: Phase 2
UNII: SN3C4ZE59P

🧪 Clinical trials

Trial	Phase	Condition	Status	Sponsor
NCT07827612	Phase 2	Urinary Bladder Neoplasms	Not yet recruiting	LLY

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Receptor, Fibroblast Growth Factor, Type 3Urinary Bladder NeoplasmsUrologic Neoplasms

Other drugs acting on FGFR3

Nintedanib FDA approved BHV-1530 Phase 1 CGT4859 Phase 1/2

More from ELI LILLY &

Abemaciclib FDA approved Baricitinib FDA approved Donanemab FDA approved Dulaglutide FDA approved Imlunestrant FDA approved Lebrikizumab FDA approved Mirikizumab FDA approved Orforglipron FDA approved Pirtobrutinib FDA approved Selpercatinib FDA approved Tirzepatide FDA approved Brenipatide Phase 3

Sources

NCI Thesaurus

Updated Oct 11, 2026. Something wrong or missing? Report it on the LLY page.

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Data: FDA (Drugs@FDA, Purple Book, DailyMed), NIH (NCI Thesaurus, GSRS, RxNorm), ClinicalTrials.gov • Informational purposes only, not medical or investment advice. • All drugs A–Z