Drug intelligence / Profile preview

rosuvastatin + ticagrelor

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

Overview

Rosuvastatin + ticagrelor is a combination therapy consisting of two small molecule drugs commonly used in the management of patients with acute coronary syndromes, particularly after percutaneous coronary intervention (PCI). Rosuvastatin is an HMG-CoA reductase inhibitor (statin) that lowers cholesterol and exerts pleiotropic effects such as improving endothelial function and reducing inflammation. Ticagrelor is a P2Y12 receptor antagonist that inhibits platelet aggregation, thereby reducing the risk of thrombotic cardiovascular events. The combination has been shown to decrease the incidence of major adverse cardiovascular events (MACE) and improve cardiac function compared to ticagrelor monotherapy in patients undergoing PCI. However, concomitant use may increase systemic exposure to rosuvastatin due to pharmacokinetic interactions—ticagrelor can inhibit transporters such as breast cancer resistance protein (BCRP) and organic anion transporting polypeptides (OATP), potentially raising rosuvastatin levels and increasing the risk for adverse effects like rhabdomyolysis[1][3][4]. Additionally, ticagrelor may cause acute kidney injury, further elevating rosuvastatin concentrations[1][5].

02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)P2Y12 (Purinergic P2Y12 receptor)ABCG2 (Breast cancer resistance protein)

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