Absolute Bioavailability, Mass Balance, and Metabolic Profiling Assessment of [14C]‐Belumosudil in Healthy Men: A Phase 1, Open‐Label, 2‐Part Study

• Published in: Clinical pharmacology in drug development Vol. 11; no. 7; pp. 786 - 794
• Main Authors: Schueller, Olivier, Skucas, Ed, Regev, Galit, Shaw, Iain, Singh, Nand, Sanghvi, Mitesh, Croft, Marie, Lohmer, Lauren, Alabanza, Anginelle, Patel, Jeegar
• Format: Journal Article
• Language: English
• Published: United States Wiley Subscription Services, Inc 01.07.2022
• Subjects: AME; Bioavailability; graft‐versus‐host disease; Kinases; Metabolism; metabolite profiling; Metabolites; pharmacokinetics; pharmacokinetics; AME; metabolite profiling; graft-versus-host disease

Belumosudil is a selective Rho‐associated coiled‐coil containing protein kinase 2 (ROCK2) inhibitor. ROCK2 has been shown to drive proinflammatory response and fibrosis that occurs with chronic graft‐versus‐host disease; therefore, inhibition of ROCK2 has emerged as a therapeutic target for chronic...