Polymorphisms in apolipoprotein E and apolipoprotein A-V do not influence the lipid response to rosuvastatin but are associated with baseline lipid levels in Chinese patients with hyperlipidemia.

Background: Apolipoprotein E (APOE) and APOA5 play an important role in lipid transport and metabolism. Polymorphisms in APOE and APOA5 have been reported to be associated with baseline lipid levels and lipid responses to statins in different populations.

Objective: This study evaluated associations of APOE and APOA5 genotype with baseline lipid levels and response to rosuvastatin in Chinese patients with hyperlipidemia.

Effects of grapefruit juice and SLCO1B1 388A>G polymorphism on the pharmacokinetics of pitavastatin.

Pitavastatin undergoes little hepatic metabolism but it is a substrate for uptake and efflux transporters, particularly OATP1B1 (gene SLCO1B1). A previous study in 8 Japanese healthy subjects showed that co-administration with grapefruit juice (GFJ) resulted in a small increase in systemic exposure to pitavastatin. We examined whether common polymorphisms in SLCO1B1 might influence the pharmacokinetics of pitavastatin or the interaction with GFJ.

Intronic variants in SLCO1B1 related to statin-induced myopathy are associated with the low-density lipoprotein cholesterol response to statins in Chinese patients with hyperlipidaemia.

Whole-genome studies have identified several intronic single nucleotide polymorphisms (SNPs) in SLCO1B1 associated with simvastatin-induced myopathy. The present study determined the effect of an intronic SNP rs4149081 in SLCO1B1 on the lipid-lowering effects of simvastatin and rosuvastatin in Chinese patients with hypercholesterolaemia. Lipid profiles were determined off treatment and after at least 4 weeks of treatment with each of the statins at daily doses of rosuvastatin 10 mg and simvastatin 40 mg.

Impact of CYP2D6 polymorphisms on the pharmacokinetics of lovastatin in Chinese subjects.

Purpose: Although CYP3A4/5 enzymes play the predominant role in the metabolism of simvastatin and lovastatin, polymorphisms in CYP2D6 were reported to be associated with the cholesterol-lowering effect and/or tolerability of simvastatin. This study was performed to examine whether common CYP2D6 polymorphisms affect the pharmacokinetics of lovastatin, which is taken as the inactive prodrug lovastatin lactone and converted to active lovastatin acid.

Methods: A single-dose pharmacokinetic study was performed with lovastatin in 23 Chinese healthy male subjects.

Effect of central obesity, low high-density lipoprotein cholesterol and C-reactive protein polymorphisms on C-reactive protein levels during treatment with Rosuvastatin (10 mg Daily).

Plasma levels of high-sensitivity C-reactive protein (hsCRP) are an important predictor of cardiovascular disease, and achievement of lower targets of hsCRP with rosuvastatin treatment was associated with improved cardiovascular outcomes. The aim of this study was to examine whether hsCRP levels were related to genetic variants and traditional cardiovascular risk factors in Chinese patients treated with rosuvastatin 10 mg/day. The relations were analyzed between on-treatment plasma hsCRP concentrations and cardiovascular risk factors and 14 single-nucleotide polymorphisms in CRP and other candidate genes.

The ABCG2 transporter and its relations with the pharmacokinetics, drug interaction and lipid-lowering effects of statins.

Importance Of The Field: The ABCG2 efflux transporter is expressed in multiple tissues and plays an important role in the disposition of many statins. The functional 421C>A polymorphism in ABCG2 that reduces transporter activity has been found to be associated with increased systemic exposures to certain statins.

Areas Covered In This Review: We review and evaluate the associations of the ABCG2 polymorphism on the pharmacokinetics and clinical efficacy of statins.

Pharmacogenetic analysis of lipid responses to rosuvastatin in Chinese patients.

Lipid changes with statin treatments vary greatly between individuals for reasons which are largely unknown. This study was performed to examine the genetic determinants of lipid responses to rosuvastatin in Chinese patients. A total of 125 polymorphisms in 61 candidate genes from 386 Chinese patients were analyzed for association with the lipid responses to rosuvastatin 10 mg daily.