Elenestinib (BLU-263, BLU263) is a potent, selective, oral next-generation KIT D816V inhibitor with IC50 of 0.2 nM.
BLU-263 has ELISA IC50 of 6 nM against HMC1.2 human mast cells (V560G/D816V).
BLU-263 exhibits limited central nervous system penetration, shows potential for systemic mastocytosis (SM).
1. Dave N, et al. Safety and pharmacokinetics of BLU-263, a next-generation KIT inhibitor, in healthy volunteers[C]//Cancer Res (AACR Annual Meeting Abstracts). 2021, 122.
