ENT-03 / Enterin - LARVOL DELTA

ENT-21: Identification of Oral ENT-03 Form for Obesity and Type 2 Diabetes Management and Modeling of Allosteric Binding to PTP1b (ADA 2026) - "ENT-21 is a prodrug of ENT-03 suitable for oral dosing. Modeling reveals that ENT-03 allosterically inhibits PTP1b and predicts high selectivity for this target."

Diabetes • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus • LEP • PTPN1

Study of Subcutaneously Administered ENT-03 for the Treatment of Obesity and Diabetes (clinicaltrials.gov) - P1 | N=49 | Completed | Sponsor: Metabolics Pharma | Active, not recruiting ➔ Completed

First-in-human • Trial completion • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus • LEP

Metabolics Pharma Announces ENT-03 Generates Sustained Weight Loss and Liver Pathology Improvements in an Animal Model for Obesity (Businesswire) - "This study compared ENT-03 to semaglutide, a combination of the two compounds, and vehicle in Diet Induced Obesity (DIO) mice. While the vehicle-treated mice gained weight through the duration of the study, mice treated with ENT-03, Semaglutide, or a combination of the two drugs all lost weight and reduced insulin and glucose levels. ENT-03 showed a greater reduction in weight than Semaglutide over the 10-week treatment period. Additive weigh loss was seen when the drugs were used in combination....A Phase 1b clinical trial is planned to initiate in the second half of 2025."

New P1 trial • Preclinical • Obesity

ENT-03 Has Additive Weight Loss and Insulin Normalization Effects with Semaglutide in Diet-Induced Obesity (DIO) in Mice (ADA 2025) - "ENT-03 produces greater weight and fat loss than SG over 10 weeks of dosing, with relative preservation of lean mass and an additive effect on fat loss when used in combination with SG. Weight loss and lower insulin persist for at least 10 weeks after treatment with ENT-03 but not SG."

Preclinical • Diabetes • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

Randomized Phase 1 Single-Ascending Dose Study of ENT-03 in Healthy Obese Subjects and Subjects with Type 2 Diabetes (ADA 2025) - "ENT-03 with a novel mechanism of action to treat obesity and/or T2D appears safe and well-tolerated in this Phase 1a study."

Clinical • P1 data • Diabetes • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus • PTPN1

Study of Subcutaneously Administered ENT-03 for the Treatment of Obesity and Diabetes (clinicaltrials.gov) - P1 | N=49 | Active, not recruiting | Sponsor: Enterin Inc. | Recruiting ➔ Active, not recruiting

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

A novel, centrally acting mammalian aminosterol, ENT-03, induces weight loss in obese and lean rodents. (PubMed, Diabetes Obes Metab) - "These data support a role for ENT-03 in the treatment of type 2 diabetes and obesity. Phase 1 studies in subjects with obesity and diabetes are currently in progress."

Journal • Preclinical • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

Study of Subcutaneously Administered ENT-03 for the Treatment of Obesity and Diabetes (clinicaltrials.gov) - P1 | N=49 | Recruiting | Sponsor: Enterin Inc. | Trial completion date: Nov 2023 ➔ Aug 2024 | Trial primary completion date: Nov 2023 ➔ Jun 2024

Trial completion date • Trial primary completion date • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

ENT-03 rapidly decreases glucose prior to weight loss and activates brain regions involved in satiety and appetite regulation: comparison with semaglutide (EASD 2023) - "ENT-03 is a novel, endogenous, centrally acting steroid with PTP1B inhibitory activity which rapidly normalizes glucose independent of body weight by acting on hypothalamic and brainstem circuits that regulate energy and metabolism in mice. The neural circuits affected by ENT-03 appear to differ from those impacted by semaglutide suggesting a different mechanism of action. Phase 1 studies in subjects with obesity and diabetes are underway."

Diabetes • Metabolic Disorders • Obesity • FOS • PTPN1

Study of Subcutaneously Administered ENT-03 for the Treatment of Obesity and Diabetes (clinicaltrials.gov) - P1 | N=49 | Recruiting | Sponsor: Enterin Inc.

New P1 trial • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus • LEP

ENT-03, a Centrally Acting Endogenous Spermine Bile Acid with PTP1B Inhibitory Activity, Has Potent Effects on Metabolism and Weight in a Mouse Model of Diet-Induced Obesity (DIO) (ADA 2023) - "ENT-03 is a novel endogenous, centrally acting mammalian steroid which rapidly normalizes glucose, independent of body weight and causes gradual but marked weight loss in DIO mice. Phase 1 studies will begin in Q2 2023."

Preclinical • Metabolic Disorders • Obesity • PTPN1