Rosuvastatin pharmacokinetics and pharmacogenetics in white and Asian subjects residing in the same environment

Lee, Edmund; Ryan, Stephen G.; Birmingham, Bruce K.; Zalikowski, Julie; March, Ruth; Ambrose, Helen; Moore, Rachael L.; Lee, Caroline; Chen, Yusong; Schneck, Dennis W.

doi:10.1016/j.clpt.2005.06.013

Cited by 428 publications

(421 citation statements)

References 18 publications

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“…This specific ethnic effect has been also observed with regard to other statin acid forms such as rosuvastatin [16,17] and simvastatin acid [16,18].…”

Section: Introductionmentioning

confidence: 78%

“…Available data suggest that this ethnic variability is due to intrinsic rather than extrinsic such as environmental factors, as it exists even between individuals in the same environment [17,20]. However, this ethnic variability cannot be fully attributed to differences in the population allele frequencies of the up-to-date known clinically important polymorphisms (e.g.…”

Section: Introductionmentioning

confidence: 99%

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Modelling of atorvastatin pharmacokinetics and the identification of the effect of a BCRP polymorphism in the Japanese population

Tsamandouras

Guo

Wendling

et al. 2017

Pharmacogenetics and Genomics

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Aim(s): Ethnicity has a modulating role in atorvastatin pharmacokinetics, with Asian subjects reported to have higher exposure compared to Caucasians. Therefore, it is difficult to safely extrapolate atorvastatin pharmacokinetic data and models across ethnic groups. This work aims to develop a population pharmacokinetic model for atorvastatin and its pharmacologically active metabolites specifically for the Japanese population. Subsequently it is aimed to identify genetic polymorphisms affecting atorvastatin pharmacokinetics in this population. Methods:Atorvastatin acid and o-OH-atorvastatin acid plasma concentrations, clinical/ demographic characteristics and genotypes for 18 genetic polymorphisms (3, 3, 1, 1, 7, 2 and 1 in the ABCB1, ABCG2, CYP3A4, CYP3A5, SLCO1B1, SLCO2B1 and PPARA genes respectively) were collected from 27 Japanese individuals (taking 10mg atorvastatin once daily) and analysed using a population pharmacokinetics modelling approach. Results:The developed population pharmacokinetic model (one-compartment for atorvastatin acid linked through metabolite formation to an additional compartment describing the disposition of o-OH-atorvastatin acid) accurately described the observed data and the associated population variability. Our analysis suggested that subjects carrying one variant allele for the rs2622604 polymorphism (ABCG2) exhibit a 55% (95%CI: 16%-131%) increase in atorvastatin oral bioavailability relatively to the value in individuals without the variant allele. Conclusion:The current work reports the identification in the Japanese population of a BCRP polymorphism, not previously associated with the pharmacokinetics of any statin, that substantially increases atorvastatin acid and o-OH-atorvastatin acid exposure. The developed model may be of clinical importance in order to guide dosing recommendations tailored specifically for the Japanese.

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“…This specific ethnic effect has been also observed with regard to other statin acid forms such as rosuvastatin [16,17] and simvastatin acid [16,18].…”

Section: Introductionmentioning

confidence: 78%

Section: Introductionmentioning

confidence: 99%

Modelling of atorvastatin pharmacokinetics and the identification of the effect of a BCRP polymorphism in the Japanese population

Tsamandouras

Guo

Wendling

et al. 2017

Pharmacogenetics and Genomics

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show abstract

“…This is consistent with similar safety findings reported in other studies on rosuvastatin 16,18,[21][22][23] . There have been concerns that increased plasma levels of rosuvastatin in Asians, as shown in single-dose pharmacokinetic studies, may lead to increased adverse drug effects 10) . However, our study did not reveal any increased adverse effects in our patients and the safety and lipid-lowering efficacy was shown to be similar to other studies predominantly using Caucasians.…”

Section: Discussionmentioning

confidence: 99%

Effects of Rosuvastatin on Low-Density Lipoprotein Cholesterol and Plasma Lipids in Asian Patients with Hypercholesterolemia

Tan

Low

Lim

et al. 2009

JAT

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Aims:Rosuvastatin is more efficacious than other statins in lowering low-density lipoprotein cholesterol (LDL-C). Studies showing higher blood levels in Asians have resulted in concerns regarding increased adverse drug reactions. This study aimed to evaluate the efficacy and safety of rosuvastatin in hypercholesterolemic Asian patients. Methods: This retrospective observational study was conducted on statin-naive patients and statinswitch patients. Patients were treated with rosuvastatin for ≥ 8 weeks. Primary outcomes were changes in LDL-C levels and proportions of patients achieving their goals (primary prevention, LDL-C ≤ 130 mg/dL; secondary prevention, LDL-C ≤ 100 mg/dL). Results: Of 1007 hypercholesterolemic patients, 483 were statin-naive (LDL-C 161 40.8 mg/dL) and 524 were statin-switch patients (LDL-C 132.7 36.9 mg/dL). In statin-naive patients, rosuvastatin significantly reduced LDL-C, total cholesterol, and triglycerides by 39.9%, 28.8%, and 9.2%, respectively (p 0.001). Eighty-one percent of these patients achieved LDL-C goals. In the statinswitch cohort, LDL-C, total cholesterol, and triglycerides levels were significantly reduced by 24.5%, 16.6%, and 3.8%, respectively (p 0.001). Achievement of target LDL-C levels increased from 29% to 72.9%. There was no significant adverse drug reaction. Conclusion

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“…In fact, a recent study indicates clear population differences in rosuvastatin sensitivity between subjects of Caucasian, Chinese, Malaysian, and Indian decent all residing in Singapore that could not be accounted for by non-genetic factors. 6 This review will summarize studies examining genetic influences on statin efficacy and toxicity, and discuss the potential for this information to guide the optimal clinical use of these compounds.…”

Section: B-hydroxy-b-methylglutarylmentioning

confidence: 99%

Clinical implications of pharmacogenomics of statin treatment

Mangravite¹,

Thorn

Krauss³

2006

Pharmacogenomics J

148

132

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Rosuvastatin pharmacokinetics and pharmacogenetics in white and Asian subjects residing in the same environment

Abstract: Plasma exposure to rosuvastatin and its metabolites was significantly higher in Chinese, Malay, and Asian-Indian subjects compared with white subjects living in the same environment.

Cited by 428 publications

References 18 publications

Modelling of atorvastatin pharmacokinetics and the identification of the effect of a BCRP polymorphism in the Japanese population

Modelling of atorvastatin pharmacokinetics and the identification of the effect of a BCRP polymorphism in the Japanese population

Effects of Rosuvastatin on Low-Density Lipoprotein Cholesterol and Plasma Lipids in Asian Patients with Hypercholesterolemia

Clinical implications of pharmacogenomics of statin treatment

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