Drug intelligence / Profile preview

PA32520

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

Overview

PA32520 is a fixed-dose combination small molecule drug consisting of 325 mg of aspirin and 20 mg of omeprazole, developed by Pozen (later acquired by Aralez Pharmaceuticals). It was designed for the secondary prevention of cardiovascular and cerebrovascular diseases in patients at risk for aspirin-associated gastric ulcers. The formulation utilizes a coordinated delivery system where immediate-release omeprazole is layered over an enteric-coated aspirin core; the omeprazole rapidly raises gastric pH to protect the stomach lining before the aspirin is released in the small intestine. Aspirin provides antiplatelet effects by irreversibly inhibiting cyclooxygenase-1 (COX-1), while omeprazole acts as a proton pump inhibitor by targeting the H+/K+-ATPase enzyme. While PA32520 was evaluated in Phase I clinical trials, the developer primarily advanced the PA32540 (325 mg aspirin / 40 mg omeprazole) and PA8140 (81 mg aspirin / 40 mg omeprazole) formulations, the former of which was approved under the brand name Yosprala.

Other names
aspirin + omeprazole (325mg/20mg)aspirin/omeprazole 325/20
02

Targets

ATP4A (Potassium–transporting ATPase alpha chain 1)PGHS-1 (Prostaglandin G/H Synthase 1)

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