Drug intelligence / Profile preview

otrezetil + omeprazole

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

Overview

Otrezetil (CP-945,598) is a potent and selective cannabinoid receptor 1 (CB1) antagonist developed by Pfizer, primarily investigated for the treatment of obesity and smoking cessation. Omeprazole is a well-established proton pump inhibitor (PPI) used to reduce gastric acid secretion. The combination of otrezetil and omeprazole was specifically evaluated in Phase 1 clinical pharmacology studies to assess potential drug-drug interactions (DDI). These trials aimed to determine if the elevation of gastric pH or the inhibition of CYP2C19 by omeprazole would significantly alter the pharmacokinetic profile of otrezetil. Development of otrezetil was ultimately discontinued by Pfizer following the withdrawal of other CB1 antagonists from the market due to psychiatric safety concerns.

Other names
CP-945,598 + omeprazole
02

Targets

ATP4A (Potassium–transporting ATPase alpha chain 1)CNR1 (Cannabinoid receptor 1)

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