Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET , RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T . Zeteletinib has potent antitumor activity.
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