ACEA Biosciences has announced the completion of its Phase 1 clinical study of AC0058, a novel irreversible Bruton’s Tyrosine Kinase (BTK) inhibitor in development for the treatment of B cell-related autoimmune diseases, including rheumatoid arthritis and systemic lupus erythematosus.
Fifty-six healthy subjects participated in the double-blind, placebo-controlled trial to evaluate AC0058’s safety, tolerability, pharmacokinetics, pharmacodynamics, and target engagement when administered orally in either a single ascending dose (SAD) or seven-day multiple ascending dose (MAD). Both the SAD and MAD trials successfully met their primary endpoints, and the maximum tolerated dose was not reached in either case.
"AC0058 is the product of ACEA’s unique drug discovery and development capabilities which have, over the past two years, advanced multiple molecules into the clinic in both China and the United States," said Xiao Xu, M.D., Chief Executive Officer of ACEA. "By leveraging our expertise in covalent tyrosine kinase inhibitors, we’ve been able to develop AC0058 rapidly. The properties of this small molecule make it well-suited for the treatment of chronic diseases, where safety is paramount. Based on the preliminary and encouraging safety and PK/PD data, and the fact that AC0058 has a profile that is amenable to chronic oral dosing, we are moving forward with plans to initiate Phase 2 trials. We’ll be announcing additional details from the trial and complete data outcomes at future professional conferences.”
AC0058 is a small molecule that selectively inhibits Bruton's tyrosine kinase (BTK) phosphorylation and its resultant downstream signaling. In preclinical studies AC0058 was shown to inhibit lymphocyte (predominantly B-cell) activation as well as inflammatory cytokine production in monocytes.