Drug intelligence / Profile preview

rabeprazole + clopidogrel

Development stage
Phase 4
Lead developer
Eisai
Modality
Small Molecules
Administration
Oral
01

Overview

**Rabeprazole + clopidogrel** is a fixed-dose combination therapy of two small molecule drugs: rabeprazole, a proton pump inhibitor (PPI), and clopidogrel, a thienopyridine antiplatelet agent. Rabeprazole works by irreversibly inhibiting the gastric hydrogen/potassium ATPase in parietal cells, suppressing gastric acid secretion to reduce gastrointestinal (GI) bleeding risk. Clopidogrel is a prodrug activated chiefly via CYP2C19; its active metabolite irreversibly blocks the P2Y12 subtype of adenosine diphosphate (ADP) receptor on platelet cell membranes, inhibiting platelet aggregation and decreasing the risk of arterial thrombotic events, particularly in cardiovascular disease. This combination is used primarily to reduce GI bleeding risk in patients requiring clopidogrel, particularly after percutaneous coronary intervention. The interaction between clopidogrel and most PPIs (due to shared metabolism by CYP2C19) may reduce clopidogrel's antiplatelet efficacy, but evidence suggests that rabeprazole does not significantly interfere with clopidogrel's activation or antiplatelet action[1][2][3][4].

02

Targets

ATP4A (Potassium–transporting ATPase alpha chain 1)P2Y12 (Purinergic P2Y12 receptor)

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