S-309309 / Shionogi - LARVOL DELTA

Safety, Tolerability, and Pharmacokinetics of a Novel Anti-obesity Agent, S-309309, in Healthy Adults with or Without Obesity. (PubMed, Clin Drug Investig) - P1 | "S-309309 was well tolerated as single-dose (up to 300 mg) and multiple-dose (50 mg once daily for 14 days) oral administration. The pharmacokinetic characteristics remained unaffected by obesity and food intake. S-309309 did not affect the pharmacokinetics of the cytochrome P450 3A substrate. Overall, S-309309 had an acceptable safety profile and favorable pharmacokinetic and pharmacodynamic characteristics."

Clinical • Journal • PK/PD data • Genetic Disorders • Obesity

S-309309, a MGAT2 Inhibitor, Enhances the Weight-Loss Effect of Semaglutide in DIO Mice (OBESITY WEEK 2024) - "Our results suggest that when combined with semaglutide, S-309309 synergistically enhances the weight-loss effect and have no impact on gastrointestinal adverse events assessed with saccharin preference test. The combination therapy of S-309309 with semaglutide holds promise as weight-loss strategy."

Preclinical • Gastrointestinal Disorder • Genetic Disorders • Obesity

Simultaneous Overcoming Approach for Poor Wettability and Low Stability in Stomach by Simple Methods; Formulation Design and Development of Monoacylglycerol Acyltransferase 2 Inhibitor, S-309309. (PubMed, Chem Pharm Bull (Tokyo)) - "In addition, by encapsulating S-309309, the increase of degradation product amount was suppressed under acidic conditions, suggesting that the suppression of degradation product formation would be expected in the stomach after oral dosing. Overall, these results suggest that the drug property issues of S-309309 can be overcome by mixing S-309309 with a water-soluble polymer and encapsulation."

Journal • Genetic Disorders • Obesity

The Continuous and Reversible Transformation of the Polymorphs of an MGAT2 Inhibitor (S-309309) from the Anhydrate to the Hydrate in Response to Relative Humidity. (PubMed, Pharmaceutics) - "A mechanism for the reversible crystal transformation between the anhydrate and pseudo-polymorphs of the hydrate was discovered. We concluded that S-309309 causes a pseudo-polymorphic transformation; however, this is not a critical issue for pharmaceutical use."

Journal

Safety and Efficacy Study of S-309309 in Obese Adults (clinicaltrials.gov) - P2 | N=365 | Completed | Sponsor: Shionogi | Active, not recruiting ➔ Completed

Trial completion • Genetic Disorders • Obesity

S-309309, a Novel MGAT2 Inhibitor, Enhances Intestinal Fatty Acid Beta Oxidation and Provides Metabolic Benefits in DIO Mice (ADA 2024) - "S-309309 enhanced beta oxidation in the intestine and increased energy expenditure in DIO mice. Also, S-309309 improved insulin sensitivity and fatty liver. Taken together, these results suggest that S-309309 may be a promising anti-obesity drug that improves metabolism with multiple mechanisms of action."

Preclinical • Metabolic Disorders • Obesity

Effect of Administration of Itraconazole on the Pharmacokinetics of S-309309 in Healthy Participants (clinicaltrials.gov) - P1 | N=14 | Completed | Sponsor: Shionogi | Active, not recruiting ➔ Completed

Trial completion • Genetic Disorders • Obesity

Effect of Administration of Itraconazole on the Pharmacokinetics of S-309309 in Healthy Participants (clinicaltrials.gov) - P1 | N=14 | Active, not recruiting | Sponsor: Shionogi | Recruiting ➔ Active, not recruiting

Enrollment closed • Genetic Disorders • Obesity

Safety and Efficacy Study of S-309309 in Obese Adults (clinicaltrials.gov) - P2 | N=365 | Active, not recruiting | Sponsor: Shionogi | Recruiting ➔ Active, not recruiting

Enrollment closed • Genetic Disorders • Obesity • CRP • LEP

Effect of Administration of Itraconazole on the Pharmacokinetics of S-309309 in Healthy Participants (clinicaltrials.gov) - P1 | N=14 | Recruiting | Sponsor: Shionogi | Not yet recruiting ➔ Recruiting

Enrollment open • Genetic Disorders • Obesity

Effect of Administration of Itraconazole on the Pharmacokinetics of S-309309 in Healthy Participants (clinicaltrials.gov) - P1 | N=14 | Not yet recruiting | Sponsor: Shionogi

New P1 trial • Genetic Disorders • Obesity

Safety and Efficacy Study of S-309309 in Obese Adults (clinicaltrials.gov) - P2 | N=320 | Recruiting | Sponsor: Shionogi | Not yet recruiting ➔ Recruiting

Enrollment open • Genetic Disorders • Obesity • CRP • LEP

Safety and Efficacy Study of S-309309 in Obese Adults (clinicaltrials.gov) - P2 | N=320 | Not yet recruiting | Sponsor: Shionogi

New P2 trial • Genetic Disorders • Obesity • CRP • LEP

A Study to Assess S-309309 in Healthy and Obese Participants (clinicaltrials.gov) - P1 | N=74 | Completed | Sponsor: Shionogi | Recruiting ➔ Completed

Trial completion • Genetic Disorders • Obesity