Drug intelligence / Profile preview

zoligratinib

Development stage
Phase 2
Lead developer
Debiopharm
Modality
Small Molecules
Administration
Oral
01

Overview

Zoligratinib (DEBIO-1347, CH5183284) is an orally available, highly selective small molecule inhibitor of fibroblast growth factor receptor subtypes 1, 2, and 3 (FGFR1–3). It acts as an ATP-competitive inhibitor that binds to the ATP-binding site of FGFR1–3 and blocks their kinase activity. This inhibition disrupts FGFR-mediated signal transduction pathways involved in tumor cell proliferation and angiogenesis. Zoligratinib demonstrates potent antitumor effects in preclinical models with FGFR genetic alterations—including mutations, amplifications, or fusions—and has shown clinical activity in patients with advanced solid tumors harboring such alterations. The drug is being developed primarily for unresectable or metastatic tumors with specific FGFR gene alterations[2][3][4][5][6][7]. Developed by Debiopharm.

Other names
zoligratinib1265229-25-1
02

Targets

FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR1 (Fibroblast growth factor receptor 1)

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