Annotation of Swissmedic Label for rosuvastatin and ABCG2, SLCO1B1
PharmGKB ID
Summary
The Swiss drug label for rosuvastatin (Crestor) states that genetic polymorphisms in SLCO1B1 and ABCG2 may lead to an increase in rosuvastatin exposure, a reduction in the dosage is recommended.
Please note that this drug label annotation was created from a collaboration between PharmGKB and Pharmaceutical Care Research Group in University of Basel in 2019. The label has not been subsequently reviewed or updated.
Prescribing
Increased plasma levels of rosuvastatin have been observed in Asians (see "Warnings and Precautions" and "Pharmacokinetics"). The recommended starting dose for Asians is 5 mg and the dose of 40 mg is contraindicated.
Genetic polymorphisms Specific types of genetic polymorphisms are known that may lead to an increase in rosuvastatin exposure (see "Pharmacokinetics"). In patients known to have such a polymorphism, a reduction in the dosage of Crestor is recommended.
Genetic polymorphisms Specific types of genetic polymorphisms are known that may lead to an increase in rosuvastatin exposure (see "Pharmacokinetics"). In patients in whom such a polymorphism is known, a reduction in the dosage of ezetimib-rosuvastatin mepha is recommended.
Annotation
Please note that the information contained within this drug label annotation is available through a collaboration with the Pharmaceutical Care Research Group (PCRG), Department of Pharmaceutical Sciences, University of Basel, who provided a translation of the pharmacogenetic information contained in the Swiss drug labels. The original label in German can be accessed using the link under "Source" below.
Excerpts from the rosuvastatin (Crestor) label:
Pharmacokinetics: ethnicity: Pharmacokinetic studies conducted in Asia showed a 2-fold increase in mean AUC in Asians compared to Caucasians living in Asia or Europe. The involvement of environmental influences and genetic factors in these observed differences was not investigated. A pharmacokinetic analysis showed no clinically relevant differences between Caucasians, Hispanics and blacks or persons of Afro-Caribbean origin.
Genetic polymorphisms: The availability of HMG-CoA reductase inhibitors such as rosuvastatin depends, among other things, on the transport proteins OATP1B1 and BCRP. Patients with different sequence variations of the SLCO1B1 gene (OATP1B1) and/or the ABCG2 gene (BCRP) are at risk of increased exposure to rosvastatin. The genotype variants SLCO1B1 c.521CC and ABCG2 c.421AA are associated with approximately 1.7-fold higher exposure to rosuvastatin (AUC) and 2.4-fold higher exposure respectively than the variants SLCO1B1 c.521TT and ABCG2 c.421CC.
Dosage: race: Increased plasma levels of rosuvastatin have been observed in Asians (see "Warnings and Precautions" and "Pharmacokinetics"). The recommended starting dose for Asians is 5 mg and the dose of 40 mg is contraindicated.
Genetic polymorphisms: Specific types of genetic polymorphisms are known that may lead to an increase in rosuvastatin exposure (see "Pharmacokinetics"). In patients known to have such a polymorphism, a reduction in the dosage of Crestor is recommended.
For the complete drug label text with pharmacogenetic information highlighted, see the Crestor drug label (in German).
*Disclaimer: The contents of this page have not been endorsed by Swissmedic and are the sole responsibility of PharmGKB.
Evidence for Clinical Annotations
This annotation has been used as evidence for the following clinical annotations.