Drug intelligence / Profile preview

FIIN-4

Development stage
Preclinical
Lead developer
Dana-Farber Cancer Institute
Modality
Small Molecules
Administration
Oral
01

Overview

FIIN-4 is a first-in-class, orally active, covalent pan-FGFR inhibitor that targets a conserved cysteine in the P-loop of FGFR1-4. It exhibits potent inhibitory activity against FGFR1, FGFR2, FGFR3, and FGFR4 with IC50 values of 2.6 nM, 2.6 nM, 5.6 nM, and 9.2 nM, respectively. Developed by researchers at Dana-Farber Cancer Institute and Purdue University, FIIN-4 has demonstrated preclinical efficacy in overcoming drug resistance (such as resistance to trastuzumab emtansine or lapatinib) and inhibiting metastatic tumor growth in breast cancer models, particularly within the pulmonary microenvironment.

Other names
FIIN4FIIN-4FIIN 4
02

Targets

FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)

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