Rosuvastatin pharmacokinetics and pharmacogenetics in Caucasian and Asian subjects residing in the United States.

Purpose: Systemic exposure to rosuvastatin in Asian subjects living in Japan or Singapore is approximately twice that observed in Caucasian subjects in Western countries or in Singapore. This study was conducted to determine whether pharmacokinetic differences exist among the most populous Asian sub...

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Publicado en:European Journal of Clinical Pharmacology Vol. 71; no. 3; pp. 329 - 341
Autores principales: Birmingham, Bruce, Bujac, Sarah, Elsby, Robert, Azumaya, Connie, Zalikowski, Julie, Chen, Yusong, Kim, Kenneth, Ambrose, Helen
Formato: research tables/charts Journal Article
Publicado: Springer Nature Mar2015
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Mar2015
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      pub: Springer Nature
      place: New York, New York
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        atl: Rosuvastatin pharmacokinetics and pharmacogenetics in Caucasian and Asian subjects residing in the United States.
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          Birmingham, Bruce
          Bujac, Sarah
          Elsby, Robert
          Azumaya, Connie
          Zalikowski, Julie
          Chen, Yusong
          Kim, Kenneth
          Ambrose, Helen
        affil: AstraZeneca, Macclesfield, Cheshire UK
      sug:
        subj:
          Rosuvastatin Pharmacokinetics
          Pharmacogenetics
          White Persons
          Asians
          Race Factors
          Human
          United States
          Rosuvastatin Therapeutic Use
          Rosuvastatin Metabolism
          Polymorphism, Genetic
          Descriptive Statistics
          Hyperlipidemia Drug Therapy
          Male
          Female
          Analysis of Variance
          Confidence Intervals
          Genotype
          Food Intake
          Data Analysis Software
          Male
          Female
      ab: Purpose: Systemic exposure to rosuvastatin in Asian subjects living in Japan or Singapore is approximately twice that observed in Caucasian subjects in Western countries or in Singapore. This study was conducted to determine whether pharmacokinetic differences exist among the most populous Asian subgroups and Caucasian subjects in the USA. Method: Rosuvastatin pharmacokinetics was studied in Chinese, Filipino, Asian-Indian, Korean, Vietnamese, Japanese and Caucasian subjects residing in California. Plasma concentrations of rosuvastatin and metabolites after a single 20-mg dose were determined by mass spectrometric detection. The influence of polymorphisms in SLCO1B1 (T521>C [Val174Ala] and A388>G [Asn130Asp]) and in ABCG2 (C421>A [Gln141Lys]) on exposure to rosuvastatin was also assessed. Results: The average rosuvastatin area under the curve from time zero to time of last quantifiable concentration was between 64 and 84 % higher, and maximum drug concentration was between 70 and 98 % higher in East Asian subgroups compared with Caucasians. Data for Asian-Indians was intermediate to these two ethnic groups at 26 and 29 %, respectively. Similar increases in exposure to N-desmethyl rosuvastatin and rosuvastatin lactone were observed. Rosuvastatin exposure was higher in subjects carrying the SLCO1B1 521C allele compared with that in non-carriers of this allele. Similarly, exposure was higher in subjects carrying the ABCG2 421A allele compared with that in non-carriers. Conclusion: Plasma exposure to rosuvastatin and its metabolites was significantly higher in Asian populations residing in the USA compared with Caucasian subjects living in the same environment. This study suggests that polymorphisms in the SLCO1B1 and ABCG2 genes contribute to the variability in rosuvastatin exposure.
      pubtype: Academic Journal
      doctype:
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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