ABCMdb

PMID: 20130569

Tomlinson B, Hu M, Lee VW, Lui SS, Chu TT, Poon EW, Ko GT, Baum L, Tam LS, Li EK
ABCG2 polymorphism is associated with the low-density lipoprotein cholesterol response to rosuvastatin.
Clin Pharmacol Ther. 2010 May;87(5):558-62. Epub 2010 Feb 3., [PubMed]

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No. Mutations Sentence Comment

5 ABCG2 p.Gln141Lys Rosuvastatin is one of the few drugs for which regulatory authorities, including the US Food and Drug Administration, have recommended starting with lower doses (5 mg instead of 10 mg) in Asian patients.3 This recommendation was based on data from single-dose pharmacokinetic studies that showed that systemic exposure to rosuvastatin was approximately twice as high in Asians as in non-Asians.4 These -differences are unlikely to be due to ethnicity-related variations in drug metabolizing enzymes, given that -rosuvastatin -undergoes relatively little enzymic modification and is a substrate for a number of drug transporters that influence its disposition.5,6 The efflux transporter ATP-binding cassette G2 (ABCG2) plays a significant role in the disposition of rosuvastatin in -vitro.7 The c.421C>A (rs2231142, Gln141Lys) single-nucleotide polymorphism of ABCG2 influences the pharmacokinetics of rosuvastatin in Chinese and Caucasian subjects.8,9 We examined whether this ABCG2 single-nucleotide polymorphism influences the reduction of LDL-C levels when rosuvastatin is administered to Chinese patients with hypercholesterolemia, including some with familial hypercholesterolemia (FH). Login to comment