Development

Structure Therapeutics' aleniglipron achieves 16.3% weight loss in phase 2 obesity trial

Structure Therapeutics (NASDAQ: GPCR), a San Francisco-based clinical-stage biopharmaceutical company, reported topline data from its Phase 2 ACCESS II...

Structure Therapeutics Reports Aleniglipron Phase 2 Data Showing 16.3% Placebo-Adjusted Weight Loss at 44 Weeks

Structure Therapeutics (NASDAQ: GPCR), a San Francisco-based clinical-stage biopharmaceutical company, reported topline data from its Phase 2 ACCESS II trial of aleniglipron, an oral GLP-1 receptor agonist, in adults with obesity or overweight. The aleniglipron Phase 2 results showed placebo-adjusted mean weight loss of 16.3% at the 180 mg dose and 16.0% at the 240 mg dose over 44 weeks, with no evidence of a weight loss plateau. If these findings hold in larger studies, Structure Therapeutics aleniglipron could become the first oral weight loss drug in the GLP-1 class to deliver efficacy in the range typically associated with injectable therapies.

ACCESS II Trial Results: Dose-Response and Efficacy at 44 Weeks

ACCESS II is a randomized, double-blind, placebo-controlled study that enrolled 85 adults with a BMI greater than 25 kg/m² and at least one weight-related comorbidity. Participants were randomized to aleniglipron or placebo, starting at 5 mg once daily and titrating over four weeks to target doses of 120 mg, 180 mg, or 240 mg. The primary efficacy estimand measured mean percent change in body weight from baseline at 44 weeks, assuming all randomized participants remained on treatment without rescue interventions.

The ACCESS II trial results at 44 weeks were as follows: the 120 mg arm achieved a placebo-adjusted mean weight loss of 14.7% (p<0.0001), the 180 mg arm reached 16.3% or approximately 39 lbs (p<0.0001), and the 240 mg arm reached 16.0% or approximately 37 lbs (p<0.0001). The placebo arm gained 1.1% body weight over the same period. The company noted that weight loss curves had not plateaued at 44 weeks, suggesting further reductions may be possible with continued treatment.

The trial was small — 85 participants across four arms — and the primary efficacy estimand models an idealized treatment scenario rather than real-world adherence. The company did not disclose detailed demographic breakdowns, subgroup analyses, or the precise number of participants per arm.

Open-Label Extension and Tolerability With a Lower Starting Dose

Beyond the controlled ACCESS II data, Structure Therapeutics reported interim findings from two additional studies. In the ACCESS open-label extension, participants who had received aleniglipron during the initial 36-week double-blind period continued treatment at up to 120 mg. At a median follow-up of 56 weeks total, aleniglipron weight loss reached 16.2% from baseline, with no plateau. Participants who had been on placebo crossed over to aleniglipron at a lower starting dose of 2.5 mg, titrating monthly to 120 mg.

A separate body composition study enrolled 71 adults on aleniglipron up to 120 mg, also starting at 2.5 mg. After a median follow-up of 20 weeks, participants had lost 6.8% of body weight and were still in the titration phase, at approximately the 30 mg step.

Both the open-label extension and body composition study provided evidence that the 2.5 mg starting dose reduced adverse event-related discontinuations compared to the 5 mg starting dose used in ACCESS and ACCESS II. Discontinuation rates due to adverse events were 2.0% in the open-label extension and 3.4% in the body composition study, compared to 3.7% in ACCESS II among participants on doses of 120 mg or higher between weeks 28 and 44. Across all studies involving more than 625 participants, the company reported no cases of drug-induced liver injury, no persistent liver enzyme elevations, and no QTc prolongation.

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How Aleniglipron Compares to the Obesity Treatment Landscape

The current standard of care for pharmacologic weight management is dominated by injectable GLP-1 receptor agonists. Semaglutide (Wegovy), approved by the US FDA for chronic weight management, produced approximately 15–17% placebo-adjusted weight loss at 68 weeks in the STEP pivotal trials. Tirzepatide (Zepbound), a dual GIP/GLP-1 receptor agonist approved in 2023, achieved placebo-adjusted weight loss of up to approximately 21% at 72 weeks in the SURMOUNT program.

Aleniglipron's 16.3% placebo-adjusted weight loss at 44 weeks falls within the range of injectable semaglutide, though the treatment duration was shorter and the trial far smaller. Cross-trial comparisons are limited by differences in study design, duration, patient populations, and sample sizes. Whether aleniglipron's weight loss trajectory continues to increase beyond 44 weeks — as the absence of a plateau suggests — will be a central question for Phase III.

The oral GLP-1 receptor agonist space is increasingly competitive. Oral semaglutide (Rybelsus) is approved for type 2 diabetes but has not matched injectable efficacy for obesity at its current approved doses, though higher-dose formulations are under study by Novo Nordisk. Eli Lilly's orforglipron, another oral non-peptide GLP-1 receptor agonist, is in Phase II/III development and reported 14.7% placebo-adjusted weight loss at 36 weeks in a Phase II trial. Eli Lilly is also advancing retatrutide, a triple GIP/GLP-1/glucagon receptor agonist, though that molecule is injectable.

Key competitors include:

  • Novo Nordisk's semaglutide (Wegovy), injectable GLP-1 receptor agonist, approved for obesity
  • Eli Lilly's tirzepatide (Zepbound), injectable dual GIP/GLP-1 receptor agonist, approved for obesity
  • Eli Lilly's orforglipron, oral non-peptide GLP-1 receptor agonist, Phase II/III

Regulatory Path and What Comes Next

Structure Therapeutics stated that it has a Type B End-of-Phase 2 meeting with the US FDA scheduled for the second quarter of 2026 to finalize the Phase III design. The company plans to initiate Phase III in the second half of 2026, with a starting titration dose of 2.5 mg and evaluation of multiple doses up to 240 mg. The company did not disclose specific Phase III endpoints, expected enrollment size, or trial duration.

Aleniglipron is a nonpeptide small molecule designed through Structure Therapeutics' structure-based drug discovery platform to function as a biased agonist of the GLP-1 receptor, selectively activating the G-protein signaling pathway. The oral formulation and once-daily dosing could offer a meaningful differentiation from injectable therapies if efficacy and tolerability are confirmed in larger, longer trials. Whether the Phase II effect sizes hold in a registrational setting — and how the tolerability profile compares at scale — remain open questions that Phase III will need to answer.


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