Drug intelligence / Profile preview

ezetimibe + rimonabant

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

Overview

Ezetimibe + rimonabant is an experimental combination therapy consisting of two small molecule drugs, ezetimibe and rimonabant, used together primarily in research settings for the management of dyslipidemia and obesity in statin-intolerant or overweight/obese patients. Ezetimibe is a cholesterol absorption inhibitor that blocks the Niemann-Pick C1-Like 1 (NPC1L1) protein in the small intestine, reducing intestinal absorption of cholesterol. Rimonabant is a selective cannabinoid receptor type 1 (CB1) inverse agonist that was developed as an anti-obesity agent; it acts centrally to suppress appetite and peripherally to improve metabolic parameters. The combination has been studied for its effects on lipid profiles and anthropometric measures, with evidence suggesting additive or synergistic benefits on triglyceride reduction and HDL-C improvement compared to monotherapy[1][2]. Rimonabant was withdrawn from global markets due to serious psychiatric side effects.

02

Targets

CNR1 (Cannabinoid receptor 1)NPC1L1 (Niemann-pick C1-Like 1 transporter)

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