Drug intelligence / Profile preview

INU-152

Development stage
Preclinical
Lead developer
Incuron
Modality
Small Molecules
01

Overview

INU-152 is a potent and selective small molecule pan-RAF inhibitor designed to target BRAF and RAS mutant cancers. It was developed to overcome the limitations of first-generation BRAF inhibitors, such as the rapid development of resistance and paradoxical activation of CRAF, which can lead to cutaneous toxicity. By inhibiting all isoforms of RAF (ARAF, BRAF, and CRAF), INU-152 aims to completely disrupt the MAPK signaling pathway in cancer cells harboring BRAF V600E or RAS mutations. Preclinical studies have demonstrated its potent anti-tumor activity in models of malignant melanoma and colorectal cancer, suggesting its potential as a therapeutic agent for cancers driven by these specific genetic alterations.

02

Targets

RAF1 (c-Raf-1 (Y340D/Y341D))ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)BRAF (B-Raf proto-oncogene, serine/threonine kinase)

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