MPC-0767, a potent, selective, and orally active hsp90 inhibitor, is the L-alanine ester prodrug of MPC-3100, exhibiting enhanced chemical stability.

MPC-0767 (oral administration; 265 mg/kg; single dose) exhibits improved PK properties with Tmax of 1 hour, Cmax of 21562 ng/mL, AUC of 94194 h*ng/mL, and F% of 56%[1]. In an N-87 xenograft tumor model, MPC-0767 (oral administration; 265 mg/kg) demonstrates comparable efficacy with a 46% tumor size reduction and no evidence of weight loss in the study animals[1]. MPC-0767 is well-tolerated when administered at 252 mg/kg po, equivalent to a 200 mg/kg dose of MPC-3100[1].