A Phase 1 Dose-Escalation, Food Effect, and Drug-Drug Interaction Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the MALT1 Inhibitor, SGR-1505, in Healthy Volunteers.

ABSTRACT: SGR-1505 is a novel small-molecule inhibitor of MALT1, a key mediator of NF-κB signaling implicated in the pathogenesis of B-cell malignancies. This study evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of SGR-1505 in healthy volunteers. In this four-part, open-label study, 73 participants received single or multiple oral doses of SGR-1505 (25-225 mg). A food effect study assessed SGR-1505 exposure with and without a high-calorie, high-fat meal. The CYP3A4 drug-drug interaction potential of SGR-1505 was evaluated by co-administration with posaconazole, a strong CYP3A4 inhibitor. SGR-1505 was rapidly absorbed (median T_max 2-4 h) with a dose-proportional increase in exposure up to 100 mg. Twice daily dosing at 100 mg over 10 days resulted in a 1.6-fold i

SUBMITTER: Gupta VK 

PROVIDER: S-EPMC12813652 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature