Drug intelligence / Profile preview

TAK-632

Development stage
Preclinical
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

TAK-632 is a **potent, selective pan-RAF kinase inhibitor** developed as an anticancer agent. It targets and inhibits multiple RAF isoforms (BRAF, CRAF, and BRAF V600E mutant) with high potency (IC50 values: BRAF wild-type 8.3 nM, BRAF V600E 2.4 nM, CRAF 1.4 nM), thereby blocking the RAS-RAF-MEK-ERK signaling cascade (also known as the MAPK pathway) crucial for the proliferation and survival of various cancer cells, including melanoma. TAK-632 is notable for suppressing RAF activity in BRAF wild-type cells with minimal paradoxical activation and shows efficacy in preclinical models of melanoma, including NRAS-mutated and BRAF inhibitor–resistant melanoma. Additionally, TAK-632 inhibits necroptosis through direct inhibition of the kinases RIPK1 and RIPK3, representing a molecular tool for studying regulated cell death beyond cancer. The compound was discovered and developed by Takeda Pharmaceutical Company[1][2][3][5][7][9].

02

Targets

RIPK1 (Receptor-interacting serine/threonine-protein kinase 1)BRAF V600ERAF1 (c-Raf-1 (Y340D/Y341D))RIPK3

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