BH-30236

BH-30236 is an investigational orally bioavailable, macrocyclic inhibitor of the CDC-like kinase family. At clinically relevant concentrations, BH-30236 has also been shown in preclinical studies to inhibit DYRK1A, DYRK1B, DYRK2, PIM3 and FLT3. BH-30236 is currently in clinical development for the treatment of acute myeloid leukemia (AML) and HR-MDS. BH-30236 is designed to modulate aberrant alternative splicing in cancerous tissue, targeting the same aberrant splicing machinery that drives AML and HR-MDS disease biology and that cancer cells exploit to develop resistance to venetoclax, FLT3 inhibitors and chemotherapy.

BH-30236 is being evaluated in a Phase 1/1b multicenter, open-label, first-in-human dose escalation and expansion trial in adults with R/R AML and HR-MDS. The FDA has granted orphan drug designation to BH-30236 for the treatment of AML.