BLU-667 is a highly potent and selective next generation inhibitor of oncogenic RET fusion and activating mutation with IC50s in low nMs for Wt RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion, displaying broad and robust anti-tumor activity against multiple RET-driven solid tumor types. It is highly active against V804 gatekeeper substitutions that are mKI resistant. In vivo, BLU-667 potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR2. In first-in-human testing, BLU-667 significantly inhibited RET signaling and induced durable clinical responses in patients with RET-altered NSCLC and MTC without notable off-target toxicity.

KEYWORDS: BLU-667 | Supplier | RET inhibitor | Pralsetinib | RG 6396 | BLU667 | BLU 667 | RG6396 | RG 6396 | X 581238 | X581238 | CT-BLU667 | CAS [2097132-94-8] | GDNF | RET | Inhibitor | Receptors