Pharmacokinetics of Rosuvastatin: A Systematic Review of Randomised Controlled Trials in Healthy Adults

Abstract

Background

Rosuvastatin is a lipid-lowering drug that works by inhibiting 3-hydroxy-3-methylglutaryl coenzyme A reductase, the rate-limiting enzyme responsible for producing cholesterol in humans. The pharmacokinetic data of rosuvastatin are considerably variable across studies.

Objective

To review the pharmacokinetics of rosuvastatin from randomised controlled trials (RCTs) in healthy adults.

Methods

A review of the pharmacokinetics of rosuvastatin was performed using systematic search strategies. The Sheiner method was used to summarise the pharmacokinetics of the drug.

Results

Randomised controlled studies (n = 70) involving healthy subjects (n = 2355) that examined the pharmacokinetics of rosuvastatin following single and multiple doses were included in the review. Rosuvastatin is given once daily in the dose range of 5–80 mg, with 40 mg being the maximum approved daily dose. Rosuvastatin achieves maximum plasma concentration at a median of 5 h (range: 0.5–6 h) under fasting conditions following single and multiple doses. Following single doses, rosuvastatin has a mean absolute oral availability of 20%, an overall mean total clearance of 28.3 L/h and an average terminal elimination half-life of approximately 20 h. The overall mean total clearance of the drug in Caucasian subjects was 1.7-fold higher than that in healthy Chinese subjects. The systemic exposure of rosuvastatin is characterised by a large coefficient of variation (48%.) There is a small accumulation with repeated dosing. The interaction of rosuvastatin with darunavir/ritonavir was considered statistically and clinically relevant. Interactions of rosuvastatin single doses with erythromycin, fluconazole, itraconazole and antacid were statistically significant.

Discussion and Conclusions

There is considerable variation in the pharmacokinetics of rosuvastatin between races. The clinical relevance of the statistically significant drug interactions is yet to be investigated following repeated co-administration for at least 15 days, consistent with a half-life of low-density lipoprotein of 3 days.

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Raju Kanukula, Abdul Salam , Anthony Rodgers and Bishoy Kamel have no conflicts of interest that are directly relevant to the content of this article.

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Kanukula, R., Salam, A., Rodgers, A. et al. Pharmacokinetics of Rosuvastatin: A Systematic Review of Randomised Controlled Trials in Healthy Adults. Clin Pharmacokinet 60, 165–175 (2021). https://doi.org/10.1007/s40262-020-00978-9

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