Role of BCRP 421C&gt;A polymorphism on rosuvastatin pharmacokinetics in healthy Chinese males

Zhang, Wei; Yu, Bangning; He, Yijing; Li, Fan; Li, Qing; Liu, Zhao‐Qian; Wang, An; Liu, Yali; Tan, Zhi‐Rong; Feng, Jiang; Huang, Yuan‐Fei; Zhou, Hong‐Hao

doi:10.1016/j.cca.2006.05.010

Cited by 230 publications

(182 citation statements)

References 15 publications

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“…Such a discrepancy cannot be explained from a pharmacokinetic viewpoint, and the effect of such a polymorphism on the plasma concentration should be theoretically clearer after oral administration. In another report, the area under the curve of the plasma concentration of rosuvastatin following a single oral administration was greater in the hetero-and homozygotes [89], but heterozygotes did not show any difference in the pharmacokinetic profile of irinotecan and its active metabolite SN-38 [15].…”

Section: Polymorphisms Of Abcg2mentioning

confidence: 88%

ATP-binding cassette, subfamily G (ABCG family)

Kusuhara

Sugiyama

2006

Pflugers Arch - Eur J Physiol

144

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This review summarizes the characteristics of the ATP-binding cassette, subfamily G (ABCG family), which has five members: ABCG1, ABCG2, ABCG4, ABCG5, and ABCG8. The members consist of a single ABC cassette in the amino terminal followed by six putative transmembrane domains, and to become functionally active, they form homo-or obligate heterodimers. Except for ABCG2, the members of the ABCG family play an important role in efflux transport of cholesterol. Mutations causing a loss of function of ABCG5 or ABCG8 are associated with sitosterolemia characterized by accumulation of phyto-and shellfish sterols. Unlike other members, ABCG2 is not involved in cholesterol efflux, but it exhibits broad substrate specificity to xenobiotic compounds. ABCG2 confers cancer cells resistance to anticancer drugs and plays a critical role in the pharmacokinetics of drugs in the clearance organs and tissue barriers. ABCG2 is also associated with a subpopulation phenotype of stem cells. Genetic polymorphisms of ABCG2 have been suggested to account for the interindividual differences in the pharmacokinetics of drugs.

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Section: Polymorphisms Of Abcg2mentioning

confidence: 88%

ATP-binding cassette, subfamily G (ABCG family)

Kusuhara

Sugiyama

2006

Pflugers Arch - Eur J Physiol

144

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“…3,[21][22][23] Similarly, in vitro studies of multidrug resistanceassociated protein 2 have shown that this protein transports a number of statins, 24 but in vivo pharmacogenomic evidence is inconclusive and limited to two small pharmacokinetic studies using pravastatin; these studies obtained contrasting results. 25,26 In contrast, the c.421C4A SNP in ABCG2 has been shown to alter the in vivo pharmacokinetics of both rosuvastatin 27,28 and atorvastatin, 27 although not pitavastatin 29 or pravastatin. 26 Both multidrug resistanceassociated protein 2 and breast cancer resistance protein are reviewed elsewhere by Ieiri et al 19 and although it is accepted that these and other transporters, both intestinal and hepatic, may play a role in statin disposition, this review will focus exclusively on OATP1B1, an hepatic influx transporter that is becoming increasing linked with differences in response to statin therapy.…”

Section: Hepatic Transportersmentioning

confidence: 97%

The influence of SLCO1B1 (OATP1B1) gene polymorphisms on response to statin therapy

et al. 2009

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Statins (3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors) are well established in the treatment of hypercholesterolaemia and the prevention of coronary artery disease. Despite this, there is wide interindividual variability in response to statin therapy, in terms of both lipidlowering and adverse drug reactions. The major site of statin action is within hepatocytes and recent interest has focussed on genetic variation in hepatic influx and efflux transporters for their potential to explain these differences. In this review we explore current literature regarding the pharmacokinetic and pharmacodynamic influence of the common c.388A4G and c.521T4C single-nucleotide polymorphisms (SNPs) within the solute carrier organic anion transporter 1B1 (SLCO1B1) gene, encoding the organic anion transporter polypeptide 1B1 (OATP1B1) influx transporter. We discuss their potential to predict the efficacy of statin therapy and the likelihood that patients will experience adverse effects.

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“…[12][13][14] BCRP also belongs to the ABC efflux transporter superfamily 26 and is widely expressed in the small intestine, liver and placenta, influencing the absorption and disposition of a variety of substrates. 27,28 It is noteworthy that Petain et al reported that IM clearance in patients carrying the ABCG2 421C/A genotype was significantly lower than in those with the 421C/C genotype. 29 To investigate the role of pharmacogenetic variation in IM metabolism and efficacy, SNPs within important IM exposure genes (ABCB1 (MDR1), ABCC2 (MRP2), ABCG2 (BCRP), CYP3A5, SLC22A1 (OCT1) and SLCO1B3 (OATP1B3)) were analyzed in IM-treated CML patients.…”

Section: Introductionmentioning

confidence: 99%

Influence of CYP3A5 and drug transporter polymorphisms on imatinib trough concentration and clinical response among patients with chronic phase chronic myeloid leukemia

et al. 2010

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Imatinib mesylate (IM) trough concentration varies among IM-treated chronic myeloid leukemia (CML) patients. Although IM pharmacokinetics is influenced by several enzymes and transporters, little is known about the role of pharmacogenetic variation in IM metabolism. In this study, associations between IM trough concentration, clinical response and 11 single-nucleotide polymorphisms in genes involved in IM pharmacokinetics (ABCB1, ABCC2, ABCG2 CYP3A5, SLC22A1 and SLCO1B3) were investigated among 67 Japanese chronic phase CML patients. IM trough concentration was significantly higher in patients with a major molecular response than in those without one (P¼0.010). No significant correlations between IM trough concentration and age, weight, body mass index or biochemical data were observed. However, the dose-adjusted IM trough concentration was significantly higher in patients with ABCG2 421A than in those with 421C/C (P=0.015). By multivariate regression analysis, only ABCG2 421A was independently predictive of a higher dose-adjusted IM trough concentration (P¼0.015). Moreover, previous studies have shown that the ABCG2 421C4A (p.Q141K) variant is prevalent among Japanese and Han Chinese individuals and less common among Africans and Caucasians. Together, these data indicate that plasma IM concentration monitoring and prospective ABCG2 421C4A genotyping may improve the efficacy of IM therapy, particularly among Asian CML patients.

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Role of BCRP 421C>A polymorphism on rosuvastatin pharmacokinetics in healthy Chinese males

Cited by 230 publications

References 15 publications

ATP-binding cassette, subfamily G (ABCG family)

ATP-binding cassette, subfamily G (ABCG family)

The influence of SLCO1B1 (OATP1B1) gene polymorphisms on response to statin therapy

Influence of CYP3A5 and drug transporter polymorphisms on imatinib trough concentration and clinical response among patients with chronic phase chronic myeloid leukemia

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