Drug intelligence / Profile preview

velneperit + orlistat

Development stage
Unknown
Lead developer
Shionogi
Modality
Small Molecules
Administration
Oral
01

Overview

This drug is a **combination of velneperit and orlistat** developed and tested for the treatment of obesity. **Velneperit** is a small molecule neuropeptide Y5 receptor antagonist that targets central nervous mechanisms regulating food intake, thereby reducing appetite[5]. **Orlistat** is a gastrointestinal lipase inhibitor that prevents the absorption of dietary fats by inhibiting pancreatic and gastric lipases in the gastrointestinal tract, leading to decreased caloric intake[6]. Combined therapy with velneperit and orlistat was evaluated in phase 2 clinical trials for obesity, with the combination aiming to enhance weight loss through distinct but complementary mechanisms—central appetite suppression and peripheral fat absorption blockade[1][2][5][6].

02

Targets

LIPF (Gastric lipase)NPY5R (Neuropeptide Y receptor type 5)PNLIP (Pancreatic triacylglycerol lipase)

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