Drug intelligence / Profile preview

orlistat + phentermine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Orlistat + phentermine is a combination of two weight-loss medications, orlistat and phentermine, used off-label for the management of obesity. Orlistat is a reversible inhibitor of gastrointestinal lipases that reduces the absorption of dietary fats in the intestines, leading to decreased caloric intake. Phentermine is a sympathomimetic amine anorectic that acts as an appetite suppressant by stimulating the central nervous system, increasing norepinephrine release and reducing hunger. While both drugs are individually approved for weight loss (orlistat as Xenical/Alli and phentermine as Adipex-P/Lomaira), there is no FDA-approved fixed-dose combination product containing only orlistat and phentermine; combinations with other agents (e.g., phentermine-topiramate) are approved. The primary indication for this combination would be adjunctive therapy to diet and exercise in adults with obesity.

02

Targets

SERT (Sodium-dependent serotonin transporter)DAT (Dopamine plasma membrane transport protein)LIPF (Gastric lipase)PNLIP (Pancreatic triacylglycerol lipase)NET (Norepinephrine Transporter)

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