bocodepsin

Bocodepsin (OKI-179) is a novel, orally bioavailable small molecule that acts as a class I-selective histone deacetylase (HDAC) inhibitor. It is a prodrug metabolized to the active compound OKI-006, which potently inhibits class I HDACs 1, 2, 3, and 8 with minimal activity against class IIa HDACs. Bocodepsin is structurally related to the natural product largazole and was developed to improve potency and selectivity while maintaining oral bioavailability. The drug has demonstrated significant anti-tumor activity in preclinical models of solid tumors such as colorectal cancer and triple-negative breast cancer and enhances the efficacy of other agents including immune checkpoint inhibitors and MEK/BRAF inhibitors in RAS-mutated cancers. Clinical studies have shown that bocodepsin is well tolerated with manageable side effects. It is currently being evaluated in phase I/II clinical trials for various solid tumors and hematologic malignancies[1][3][4][7].

Other names

bocodepsinlargazole analog