Drug intelligence / Profile preview

rimonabant + metformin

Development stage
Discontinued
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

**Rimonabant + metformin** is a combination therapy involving two small molecule drugs: rimonabant, a selective cannabinoid type 1 (CB1) receptor antagonist/inverse agonist, and metformin, a biguanide insulin sensitizer. Rimonabant was originally developed by Sanofi-Aventis for obesity and type 2 diabetes, acting centrally to reduce appetite and improve metabolic risk factors via CB1 receptor blockade[3][1]. Metformin is a first-line antihyperglycemic agent that decreases hepatic glucose production and increases insulin sensitivity[4]. The combination was investigated primarily for glycemic control, weight loss, and cardiometabolic risk reduction in overweight or obese patients with type 2 diabetes inadequately controlled by metformin monotherapy[1][3][6][7]. Clinical studies included assessment of effects on HbA1c, body weight, lipid profile, and abdominal obesity in this population[1][2][3]. Rimonabant was withdrawn from the market due to psychiatric adverse effects; investigations of this combination have since been terminated[1][7].

02

Targets

CNR1 (Cannabinoid receptor 1)ND1 (Mitochondrial electron transport chain complex I)

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