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vepugratinib

Development stage: Phase 3
Lead developer: Eli Lilly
Modality: Small Molecules
Administration: Oral

Overview

**Vepugratinib** is an isoform-selective, small molecule inhibitor specifically targeting Fibroblast Growth Factor Receptor 3 (**FGFR3**). It is being investigated for the treatment of solid tumors, principally **metastatic urothelial carcinoma** and other cancers that harbor FGFR3 gene alterations. The drug is administered orally and aims to block aberrant FGFR3 signaling that drives tumor growth in certain cancers. Early clinical trials (Phase 1a/b as of July 2025) are studying vepugratinib alone and in combination with pembrolizumab or enfortumab vedotin plus pembrolizumab[1][5][13].

Brand names: vepugratinib
Other names: LY3866288LY-3866288LY 3866288LOXO-435LOXO435LOXO 435

Targets

FGFR3 (Fibroblast growth factor receptor 3)

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