Drug intelligence / Profile preview

liraglutide + orlistat

Development stage
Discontinued
Lead developer
ECU Diabetes & Obesity Institute
Modality
Peptides, Small Molecules
Administration
Subcutaneous, Oral
01

Overview

This combination therapy consists of liraglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist, and orlistat, a gastrointestinal lipase inhibitor. It was investigated by East Carolina University in a pilot clinical study (NCT01597531) to evaluate its potential to improve type 2 diabetes remission rates in patients with persistent diabetes following laparoscopic adjustable gastric banding (LAGB). Liraglutide works by mimicking the incretin hormone GLP-1, which enhances glucose-dependent insulin secretion, suppresses glucagon secretion, and slows gastric emptying. Orlistat acts locally in the lumen of the stomach and small intestine by forming a covalent bond with the active serine site of gastric and pancreatic lipases, thereby preventing the hydrolysis of dietary fat into absorbable free fatty acids and monoglycerides. The study aimed to determine if this pharmacological combination could replicate the high diabetes remission rates typically seen with more invasive Roux-en-Y gastric bypass surgery.

Other names
Liraglutide and Orlistat
02

Targets

LIPF (Gastric lipase)PNLIP (Pancreatic triacylglycerol lipase)GLP1R (GLP-1R)

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