Rosuvastatin–Ticagrelor Drug Interaction
Ticagrelor increases rosuvastatin exposure by inhibiting the transporter BCRP, which increases rosuvastatin plasma concentrations and can increase the risk of myopathy. [1]
Pharmacokinetic data show a ~2.6-fold increase in rosuvastatin AUC with ticagrelor. [1]
Mechanism of Interaction
Rosuvastatin is a substrate of transporters including BCRP and OATP1B1. [1]
Ticagrelor inhibits BCRP-mediated rosuvastatin transport and increases rosuvastatin AUC. [1]
Clinical Significance
The interaction is clinically relevant for muscle toxicity risk, including myopathy and rhabdomyolysis. [1]
Cases of rhabdomyolysis have been reported with concomitant ticagrelor and rosuvastatin, supporting the potential for clinically meaningful toxicity. [2]
Dose Adjustment and Monitoring Guidance
Rosuvastatin should be started at a lower dose when the expected increase in exposure (AUC) is approximately 2-fold or higher due to an interacting drug. [1]
For ticagrelor, the rosuvastatin SmPC recommends considering benefit versus the risk of increased rosuvastatin concentrations and initiating at a reduced starting dose when clinically appropriate. [1]
Clinical monitoring for signs and symptoms of myopathy is recommended when ticagrelor and rosuvastatin are used together. [1]
Practical Management Approach
A rosuvastatin dose reduction is appropriate when ticagrelor is initiated or when rosuvastatin dose is being titrated upward, given the ~2.6-fold AUC increase reported with ticagrelor. [1]
If muscle symptoms occur (e.g., unexplained muscle pain, tenderness, weakness), rosuvastatin should be reassessed promptly for possible statin-associated muscle injury. [1]
Evidence Supporting Increased Rosuvastatin Exposure
A clinical pharmacology study reported that ticagrelor increased rosuvastatin exposure through transporter-mediated interaction. [3]
The rosuvastatin SmPC summarizes the ticagrelor effect as a ~2.6-fold increase in rosuvastatin AUC with ticagrelor 90 mg twice daily for 2 days and a rosuvastatin single 10 mg dose. [1]
Key References
This interaction is described in rosuvastatin product information and supported by clinical pharmacology and case-based literature. [1] [2] [3]