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

• Regor announced its 12-week single-dose Phase 2a trial results for RGT-075, a once-daily oral GLP-1RA, reporting 5% placebo-adjusted weight-loss with no plateau
• No treatment-related severe adverse events (AEs), with only 4% discontinuation rate due to AEs, same as placebo
• Enrollment opening for its COMO-1 Phase 2b dose-finding study to read out Q4 2025

CAMBRIDGE, Mass., Jan. 11, 2025 /PRNewswire/ -- Regor Therapeutics Group ("Regor"), a privately-held clinical-stage global biopharmaceutical company, announced topline results from its Phase 2a clinical trial for RGT-075, a leading oral once-daily small molecule full agonist of GLP-1 receptor.

In the Phase 2a trial conducted at ten clinical centers across the US, RGT-075 at 125 mg once-daily delivered statistically significant 5% placebo-adjusted weight loss with no plateau at 12 weeks (six weeks on target dose) in patients living with obesity (N = 73).

There were no treatment-related severe adverse events. Discontinuation rates due to any adverse events were 4%, identical for patients receiving the active treatment and those on the placebo. Only one patient (2%) required dose reduction, and she completed the study successfully at the 60 mg once-daily dose.

Regor CEO Xiayang Qiu, Ph.D., commented, "The existing GLP-1 peptide drugs have demonstrated immense value and unprecedented promise. 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."

Dr. Qiu added, "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. 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."

In the RGT-075 treatment arm, at least one event of mild-to-moderate nausea and vomiting was reported for 40% and 24% patients, respectively. Michael Grimm, M.D., Ph.D., Head of Metabolic Diseases at Regor commented, "Even with only six weeks of titration, our tolerability results are already comparable to those observed for semaglutide in longer studies." "Beyond peptide-like weight loss with no plateau at 12 weeks, RGT-075 also showed robust and clinically meaningful efficacy in HbA1c and in Systolic and Diastolic blood pressure."

RGT-075 has previously demonstrated a promising PK-profile, with a peak-to-trough ratio (PTR) of under 5. Developers hypothesize that delivering target 24-hour plasma concentration with a relatively low PTR correlates with improved tolerability to GI-related symptoms.

About the COMO-1 Phase 2b development program

Today Regor also announced the initiation of the COMO-1 dose-finding trial for RGT-075. The Phase 2b multicenter, randomized, double-blind, placebo-controlled study will evaluate multiple doses up to 225 mg of RGT-075 over 36 weeks compared with placebo in adult patients with obesity or overweight with weight-related comorbidities. Approximately 240 adult participants will be enrolled and randomized to RGT-075 or placebo. All participants on RGT-075 will be given RGT-075 once daily (QD) titrated up over 12 weeks. The primary endpoint is percent change in body weight from baseline to week 36. Secondary endpoints include safety and tolerability of the monthly titration scheme, as well as pharmacokinetics of RGT-075. Topline data from the Phase 2b study are expected at the end of 2025.

Dr. Qiu commented, "Building upon the strong results to date, the phase 2b study is designed to provide further insights to optimize phase 3 dose selection and titration design. With our recent $850M up-front deal with Roche in breast cancer, we have the financial means to launch RGT-075 Phase 3 programs on our own, but we are genuinely interested in partnership with expert investors and companies to accelerate its path to patients and to explore rational combination approaches, expanding the potential of this best-in-class oral small molecule GLP-1 drug for sustained management of obesity and numerous weight-related comorbidities"

About RGT-075

RGT-075 is an orally bioavailable, once-daily, small molecule GLP-1R full agonist discovered and developed by Regor for the treatment of metabolic diseases, such as type-2 diabetes mellitus and obesity or overweight with weight-related comorbidities. Regor previously completed Phase 2a studies in patients with obesity, Phase 1 single ascending dose (SAD) in healthy volunteers and multiple ascending dose (MAD) in patients with diabetes. RGT-075 was safe and well-tolerated in clinical trials completed to date, with emerging efficacies comparable to the approved peptide GLP-1 drugs.

About Regor Therapeutics

Regor Therapeutics Group is a clinical-stage biotechnology company, headquartered in Cambridge, MA and with operations in Houston, San Diego, and Shanghai, which is developing innovative and clinically differentiated medicines to address large unmet needs in oncology, metabolism, and auto-immunity.

Regor is powered by the highly efficient drug discovery engine rCARD^TM (Regor Computer Accelerated Rational Discovery) that enables rapid prototyping and validation of candidate molecules. This rapid approach to developing small molecules against high-profile targets is the creation of the four cofounders who collectively brought decades of experience in leading US biopharma and were previously the named inventors of 4 FDA-approved medicines. The power of the rCARD^TM platform and approach has been validated by out-licensing deals with top companies, including Roche/Genentech on next-gen CDK oncology agents RGT-419B and RGT-587 (now GDC-4198 and GDC-0587) for $850M up-front payment in late 2024.

To learn more about Regor, please visit us at www.regor.com. 

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