Sagimet Doses First Participants In Phase 1 Pharmacokinetic Trial Of Combination Of Oral Once-Daily FASN Inhibitor, Denifanstat, And THR-β Agonist, Resmetirom; Topline Data Expected In H1 2026

Author: Benzinga Newsdesk | October 01, 2025 07:17am

• Dosing has successfully commenced with healthy volunteers
• Primary endpoints for the Phase 1 trial include safety, tolerability, and pharmacokinetic (PK) profile of the combination
• Topline data are anticipated in the first half of 2026
   

SAN MATEO, Calif., Oct. 01, 2025 (GLOBE NEWSWIRE) -- Sagimet Biosciences Inc. ((Sagimet, NASDAQ:SGMT), a clinical-stage biopharmaceutical company developing novel therapeutics targeting dysfunctional metabolic and fibrotic pathways, today announced that the Company has dosed the first participants in a Phase 1 pharmacokinetic (PK) trial of a combination of its oral once-daily fatty acid synthase (FASN) inhibitor, denifanstat, and a thyroid hormone receptor beta (THR-β) agonist, resmetirom. Topline data from this trial are anticipated in the first half of 2026 and, if positive, are planned to be used to advance the development of the combination for patients living with metabolic dysfunction-associated steatohepatitis (MASH) into Phase 2, subject to consultation with regulatory authorities.

The Phase 1 PK trial of denifanstat and resmetirom is an open-label, 2-cohort study and will enroll approximately 40 healthy adult participants. The objectives are to evaluate multiple-dose and single-dose pharmacokinetics, identify any potential drug-drug interactions (DDI), and assess the safety and tolerability of the combination. Results from this Phase 1 PK trial will be used to inform the optimal dose levels of denifanstat and resmetirom to evaluate in a Phase 2 combination proof-of-concept efficacy trial in F4 MASH patients.

Denifanstat, Sagimet's lead product candidate, is an oral, once daily selective FASN inhibitor in development for the treatment of MASH, whose strong anti-fibrotic mechanism of action coupled with its inhibition of liver fat synthesis and inflammation may be complementary to a fat oxidizer molecule such as resmetirom. Pre-clinical data presented at EASL in 2024 for two mouse models of MASH showed that the combination of a FASN inhibitor (TVB-3664, a mouse surrogate for denifanstat) and resmetirom had a synergistic effect on important markers of liver disease, including improvement of NAS (NAFLD Activity Score) by histologic analysis and more robust improvement in hepatic collagen content compared to the single agents.

Posted In: SGMT