RGT-075 / Regor - LARVOL DELTA

First report on the small-molecule, oral GLP-1 receptor agonist RGT-075 in obesity: a randomised, placebo-controlled phase 2a proof-of concept 12-week study (EASD 2025) - P2 | "However, mainly injectable options are available except for oral semaglutide. RGT-075, a small molecule oral GLP-1 RA, demonstrated a significant weight reduction with robust blood pressure changes and a safety profile consisted with the GLP-1 RA class. These findings support further clinical development of RGT-075."

Clinical • P2a data • Diabetes • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

First Report on the Small Molecule Oral GLP-1 Receptor Agonist RGT-075 in Obesity—A Randomized, Placebo-Controlled Phase 2a Proof-of-Concept Twelve-Week Study (ADA 2025) - P2 | "However, mainly injectable options are available except for oral semaglutide. RGT-075, a small molecule oral GLP-1 RA, demonstrated a significant weight reduction with robust blood pressure changes and a safety profile consisted with the GLP-1 RA class. These findings support further clinical development of RGT-075."

Clinical • P2a data • Diabetes • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

Regor to Present Data on its Lead Obesity Candidate, RGT-075, at the 85th Scientific Sessions of American Diabetes Association (ADA) (PRNewswire) - "Regor Therapeutics Group...announced that it will present results from its Phase 2a trial of RGT-075 in adults with obesity or overweight with weight-related comorbidities at the 85th Scientific Sessions of American Diabetes Association (ADA)....RGT-075 is being evaluated in COMO-1 dose-finding trial, a Phase 2b multicenter, randomized, double-blind, placebo-controlled study to evaluate multiple doses of RGT-075 over 36 weeks in adults with obesity or overweight with weight-related comorbidities. The trial has enrolled approximately 240 participants....Topline data from the Phase 2b study are expected at the end of 2025."

Enrollment status • P2 data • Obesity

Regor to Present Data on its Lead Obesity Candidate, RGT-075, at the 85th Scientific Sessions of American Diabetes Association (ADA) (PRNewswire) - "Regor Therapeutics Group...today announced that it will present results from its Phase 2a trial of RGT-075 in adults with obesity or overweight with weight-related comorbidities at the 85th Scientific Sessions of American Diabetes Association (ADA) taking place June 20-23 in Chicago....Topline data from the Phase 2b study are expected at the end of 2025."

P2a data • P2b data • Obesity

Study of Once-Daily Oral RGT001-075 Compared With Placebo in Adults With Obesity or Are Overweight With Weight-Related Health Conditions (COMO-1) (clinicaltrials.gov) - P2 | N=236 | Active, not recruiting | Sponsor: Regor Pharmaceuticals Inc.

New P2 trial • Genetic Disorders • Obesity

RGT001-075-203: A Study of RGT001-075 in Adult Patients With Obesity (clinicaltrials.gov) - P2 | N=73 | Completed | Sponsor: Regor Pharmaceuticals Inc. | Active, not recruiting ➔ Completed

Trial completion • Genetic Disorders • Obesity

Regor…Begins Phase 2b Study in the US for the Treatment of Obesity (PRNewswire) - "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."

New P2b trial • P2b data • Obesity

Regor Releases Phase 2a Topline Results for RGT-075, an Oral Once-daily Small Molecule GLP-1R Agonist… (PRNewswire) - P2a | N=73 | NCT06277934 | Sponsor: Regor Pharmaceuticals Inc. | "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....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."

P2a data • Obesity

RGT001-075-203: A Study of RGT001-075 in Adult Patients With Obesity (clinicaltrials.gov) - P2 | N=73 | Active, not recruiting | Sponsor: Regor Pharmaceuticals Inc. | Recruiting ➔ Active, not recruiting

Enrollment closed • Genetic Disorders • Obesity

RGT001-075-203: A Study of RGT001-075 in Adult Patients With Obesity (clinicaltrials.gov) - P2 | N=60 | Recruiting | Sponsor: Regor Pharmaceuticals Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Genetic Disorders • Obesity

Regor Initiates Phase 2 Study of Oral Once-daily GLP-1 Agonist RGT-075 for the Treatment of Obesity (PRNewswire) - "Regor Therapeutics Group...today announced that its Phase 2 trial of the highly selective oral GLP-1 agonist RGT-075 is initiated in adults with obesity or overweight with weight-related comorbidities and has First Patient First Visit (FPFV) on Mar 08, 2024. The topline results for this Phase 2 trial are expected to be announced in the second half of 2024."

P2 data • Trial status • Obesity

RGT001-075-203: A Study of RGT001-075 in Adult Patients With Obesity (clinicaltrials.gov) - P2 | N=60 | Not yet recruiting | Sponsor: Regor Pharmaceuticals Inc.

New P2 trial • Genetic Disorders • Obesity

A Study of Oral GLP1RA RGT001-075 in Adults With Type 2 Diabetes (clinicaltrials.gov) - P2 | N=17 | Terminated | Sponsor: Regor Pharmaceuticals Inc. | N=420 ➔ 17 | Active, not recruiting ➔ Terminated; Terminated due to financial constraint.

Enrollment change • Trial termination • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

A Phase 1, Double-Blind, Placebo-Controlled Multiple Escalating Dose Study of RGT-075 Novel Small-Molecule Oral GLP-1 Receptor Agonist in Adults with Type 2 Diabetes (ADA 2022) - "Phase 1 multiple-ascending dose study of RGT-075 in adults with type 2 diabetes (T2DM) results are presented. A Phase 1, randomized, double-blind, placebo-controlled, inpatient study planned multiple daily doses of RGT-075 or matching placebo (6 active/2 placebo per cohort) for up to 28 days in T2DM patients (baseline HbA1c 6-10.5% and concomitant metformin >500 mg/d). RGT-075 GLP1RA oral small molecule (15-180 mg/day) up to 28 days was safe and QD dosing showed promising exploratory efficacy trends despite high baseline variability and short treatment duration."

Clinical • Late-breaking abstract • P1 data • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

A First-in-Human Study of RGT-075, a Novel, Orally Bioavailable, Small-Molecule GLP-1 Receptor Agonist, in Healthy Adult Subjects (ADA 2022) - "Overall, single RGT-075 doses between 15-280 mg were safe and well-tolerated in healthy volunteers. Further clinical development of RGT-075 as a once-daily, oral therapy for T2DM is underway."

Clinical • P1 data • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

RGT-075, an Orally Efficacious Small Molecule GLP-1R Full Agonist in Cynomolgus Monkey Models (ADA 2022) - "In food-induced glucose intolerant and prediabetic cynomolgus monkeys, oral administration of RGT-075 improved glucose tolerance to a level comparable to injectable liraglutide. In food-induced type 2 diabetic monkeys, once-daily oral administration of RGT-075 reduced food intake and fasting plasma glucose levels. Together, these data support the development and advancement of RGT-075 into the clinic as a potential therapeutic for T2D and obesity."

Preclinical • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

A Study of Oral GLP1RA RGT001-075 in Adults With Type 2 Diabetes (clinicaltrials.gov) - P2 | N=420 | Active, not recruiting | Sponsor: Regor Pharmaceuticals Inc. | Recruiting ➔ Active, not recruiting

Enrollment closed • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

A Study of Oral GLP1RA RGT001-075 in Adults With Type 2 Diabetes (clinicaltrials.gov) - P2 | N=420 | Recruiting | Sponsor: Regor Pharmaceuticals Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus