Cannabinoid blockers have been successful for the treatment of obesity. However, due to CNS side effects drug development programs were halted. We present data from INV-202, a peripherally acting next generation CB1 blocker with very low CNS penetration. This randomized, DB, PC, PG, 28day study (NCT05282446) enrolled subjects with metabolic syndrome. Subjects received INV-202 25 mg or placebo and assessed weekly by lipid profile, weight, waist, and biomarkers. Oral glucose tolerance test (OGTT) was performed at baseline and at the end of study. All statistical comparisons are post-hoc.37 subjects were enrolled (46% Fem, Age 55 years, HgbA1c 5.7%, TG 2.22 mmol/L, BMI 38.1) INV-202 exhibited a mean weight loss of 3.5 kg (3.3%) compared with placebo subjects who gained a mean of 0.6 kg (0.5%). All other biomarkers showed improvements. There were no discontinuations, no SAEs and all AEs were mild to moderate. (nausea, decreased appetite, and diarrhea) INV-202 was well tolerated over 28 days of treatment. Significant improvements were noted. Further studies on the long-term cardiometabolic effect of this novel CB1 blocker are warranted.


G.D.Crater: Employee; Inversago Pharma. F.Ravenelle: Employee; Inversago. K.Lalonde: Employee; Inversago. J.Després: Advisory Panel; Inversago Pharma Inc., Other Relationship; Rockpointe Corporation – Steering Committee.

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