Drug intelligence / Profile preview

compound 22

Development stage
Preclinical
Lead developer
University of Brescia
Modality
Small Molecules
Administration
Oral
01

Overview

Compound 22 is a non-steroidal, orally available small molecule fibroblast growth factor (FGF) trap developed as a successor to the steroidal FGF trap NSC12. Identified through a scaffold-hopping approach by researchers at the University of Brescia and the University of Parma, this compound is designed to eliminate the steroid nucleus while maintaining high affinity for FGF ligands, specifically Fibroblast growth factor 2 (FGF2). By binding and sequestering FGF2, Compound 22 prevents the ligand-dependent activation of fibroblast growth factor receptors (FGFRs), thereby inhibiting downstream signaling pathways that drive tumor growth, survival, and angiogenesis. In preclinical studies, it has shown potent anti-tumor activity against multiple myeloma (MM) cell lines and patient-derived primary cells, including those resistant to proteasome inhibitors, suggesting its potential as a therapeutic option for relapsed or refractory multiple myeloma.

02

Targets

FRS2 PTB domain (Fibroblast growth factor receptor substrate 2 phosphotyrosine-binding domain)

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