Lena Klopp-Schulze, Sathej Gopalakrishnan, Özkan Yalkinoglu, Yoshihiro Kuroki, Hong Lu, Kosalaram Goteti, Axel Krebs-Brown, Marco Nogueira Filho, Ulrike Gradhand, Markus Fluck, Jamie Shaw, Jennifer Dong, Karthik Venkatakrishnan
Enpatoran is a novel, highly selective, and potent dual toll-like receptor (TLR)7 and TLR8 inhibitor currently under development for the treatment of autoimmune disorders including systemic lupus erythematosus (SLE), cutaneous lupus erythematosus (CLE), and myositis. The ongoing phase II study (WILLOW; NCT05162586) is evaluating enpatoran for 24 weeks in patients with active SLE or CLE and is currently recruiting. To support development of WILLOW as an Asia-inclusive multiregional clinical trial (MRCT) according to International Conference on Harmonisation E5 and E17 principles, we have evaluated ethnic sensitivity to enpatoran based on clinical pharmacokinetic (PK), pharmacodynamic (PD), and safety data from an ethno-bridging study (NCT04880213), supplemented by relevant quantitative PK, PD, and disease trajectory modeling (DTM) results, and drug metabolism/disease knowledge...
February 28, 2024: Clinical Pharmacology and Therapeutics