Drug intelligence / Profile preview

ARV-806

Development stage
Phase 2
Lead developer
Arvinas
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

ARV-806 is an investigational small molecule proteolysis-targeting chimera (PROTAC) designed to selectively degrade the KRAS G12D mutant protein. KRAS G12D is a common oncogenic driver mutation found in several solid tumors, including pancreatic, colorectal, and lung cancers. By inducing targeted degradation of the mutant KRAS G12D protein, ARV-806 aims to inhibit tumor growth and progression in cancers harboring this mutation. The drug is being developed by Arvinas and represents a novel approach compared to traditional inhibitors by leveraging targeted protein degradation rather than inhibition alone. The first-in-human clinical trial for ARV-806 began in 2025, focusing on adults with advanced solid tumors carrying the KRAS G12D mutation[3][5][6][8].

02

Targets

KRASG12D (Kirsten rat sarcoma viral oncogene homolog (KRAS) G12D mutant)

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