Oral GLP-1 Shows Significant Weight Loss in Patients With Obesity

Positive results have been announced from a phase 2a trial evaluating the safety and efficacy of RGT-075 in helping adult patients who are above a healthy range to lose weight, according to a release from Regor Therapeutics.¹ The therapy, which is also currently in development for the treatment of type 2 diabetes, is an orally bioavailable, small molecule glucagon-like peptide-1 (GLP-1) receptor agonist.

Oral GLP-1 Shows Significant Weight Loss in Patients With Obesity / Win Nondakowit - stock.adobe.com

"The existing GLP-1 peptide drugs have demonstrated immense value and unprecedented promise,” Xiayang Qiu, PhD, CEO at Regor, said in a release.¹ “However, we have heard loud and clear the pleas of physicians and patients for an oral version that can provide sustainable benefits and be accessible for the hundreds of millions of patients living with obesity and weight-related comorbidities."

READ MORE: Long-Acting GLP-1 Shows Positive Results in Phase 2 Study

The study was a multicenter, double-blind, placebo-controlled, phase 2a trial comparing RGT-075 with placebo in adult patients who have overweight or obesity. The study cohort included 73 adult patients aged between 18 and 75 years who had a BMI of 27 kg/m² or greater, 45 kg/m² or greater, and had stable bodyweight for 3 months prior to study initiation. Patients received 125 mg of the therapy once-daily or placebo for 12 weeks. The study took place at 10 clinical centers across the United States.

The study found that patients treated with RGT-075 demonstrated a statistically significant 5% placebo-adjusted weight loss. Additionally, no weight loss plateau was seen up to 12 weeks. Discontinuation rates due to any adverse events were 4%, which was identical for patients receiving placebo. One patient in the study required a dose reduction down to 60 mg once-daily, after which they successfully completed the study. At least 1 event of mild-to-moderate nausea and vomiting was reported in 40% and 24% of patients, respectively.

"We chose to pursue the small molecule route because of its proven suitability for long-term use as once-daily oral medications, along with the inherent advantage of easier manufacturing and supply in desired quantities,” Qiu said in a release.¹ “We succeed when patients have better options, and we believe RGT-075 has achieved an early proof-of-concept milestone through this phase 2a study."

Regor also announced in the release that it is initiating a dose-finding trial for RGT-075. COMO-1 will be a multicenter, randomized, double-blind, placebo-controlled phase 2b study evaluating multiple doses of the therapy up to 225 mg over 36 weeks in adult patients who have obesity or overweight with weight-related comorbidities. The study will enroll approximately 240 patients, with the primary endpoint being percent change in body weight from baseline. Topline data from the study are expected at the end of 2025.

READ MORE: Obesity Management Resource Center

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References

1. Regor Releases Phase 2a Topline Results for RGT-075, an Oral Once-daily Small Molecule GLP-1R Agonist, and Begins Phase 2b Study in the US for the Treatment of Obesity. News Release. Regor Therapeutics. January 10, 2025. Accessed January 14, 2025. https://www.prnewswire.com/news-releases/regor-releases-phase-2a-topline-results-for-rgt-075-an-oral-once-daily-small-molecule-glp-1r-agonist-and-begins-phase-2b-study-in-the-us-for-the-treatment-of-obesity-302348153.html