bos 172738 hemiadipate

Zeteletinib hemiadipate (BOS-172738; DS-5010) is an orally active compound that functions as a selective inhibitor of RET kinase. It exhibits nanomolar potency against RET and a 300-fold selectivity towards VEGFR2. Notably, Zeteletinib hemiadipate demonstrates exceptional effectiveness against various forms of RET, including the wild type, RET V804M L gatekeeper mutants, and the oncogenic RET mutation M918T. Additionally, Zeteletinib hemiadipate exerts potent antitumor effects.

Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase, demonstrating nanomolar potency against RET and over 300-fold selectivity against VEGFR2. It exhibits remarkable efficacy against wild-type RET, RET V804M/L gatekeeper mutants, and the frequently occurring oncogenic RET mutation M918T, with potent antitumor activity.