First-in-Human Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASP1617, a Cathepsin-S Inhibitor, in Healthy Adult Subjects.

ABSTRACT: ASP1617 is a novel, highly selective inhibitor of cathepsin-S, an important protease for antigen peptide loading onto major histocompatibility complex class II molecules. Preclinically, ASP1617 prevented progression of lupus-like glomerulonephritis in an NZB/W F1 mouse model of systemic lupus erythematosus. In this double-blind, randomized, placebo-controlled, first-in-human study in healthy subjects, ASP1617 was generally well tolerated. Treatment-emergent adverse events of rash and throat tightness were reported in two subjects receiving the highest doses of 110 mg BID in multiple ascending dose (MAD) cohorts, leading to withdrawal of ASP1617 in both subjects. Mean elimination half-life was 10.4-15.9 h in single ascending dose (SAD) cohorts and 13.7-20.5 h in MAD cohorts. ASP1617 exposur

SUBMITTER: Kojima T 

PROVIDER: S-EPMC12830235 | biostudies-literature | 2026 Feb

REPOSITORIES: biostudies-literature