BCRP polymorphism

In conclusion, to date no in vivo effects of BCRP polymorphisms have been detected in relation to efficacy and toxicity of anticancer dmgs that are substrates for BCRP. 

For other efflux transporters such as BCRP (ABCG2), human pharmacokinetic and pharmacodynamic data are currently rare. However, an investigation of the influence of polymorphisms in ABC-transporter genes on the accumulation of nelfinavir in peripheral blood mononuclear cells (PBMCs) revealed no associations between the polymorphisms in the transporters analyzed and the accumulation of nelfinavir in the PBMCs [151], A second study in patients clearly demonstrated an increase in the AUC of the orally and intravenously administered BCRP substrate topotecan when it is given with GF120918, an inhibitor of P-glycoprotein and BCRP [152],... 

Kobayashi, D., leiri, I., Hirota, T., et al. (2005) Eunctional assessment of ABCG2 (BCRP) gene polymorphisms to protein expression in human placenta. Drug Metab. Dispos. 33, 94-101. 

Lapatinib had been shown ex vivo to be primarily metabolized by CYP3A4/5 with a minor contribution from CYP2C19, and to be a substrate of the transporters MDRl(ABCBl) and BCRP(ABCG2). A hypothesis was proposed whereby polymorphisms in these genes would be associated with a propensity to develop rash and/or diarrhea. 

Honjo Y, Morisaki K, Huff LM, Robey RW, Hung J, Dean M, Bates SE. Single-nucleotide polymorphism (SNP) analysis in the ABC half-transporter ABCG2 (MXR/BCRP/ABCP1). Cancer Biol Ther 2002 1 696-702. 

Choudhuri, S., and Klaassen, C. D. Structure, function, expression, genomic organization, and single nucleotide polymorphisms of human ABCB1 (MDR1), ABCC (MRP), and ABCG2 (BCRP) efflux transporters. Int. J. Toxicol. 25, 231-259, 2006. 

Generaux GT, Bonomo FM, Johnson M, Doan KM (2011) Impact of SLCOIBI (OATP1B1) and ABCG2 (BCRP) genetic polymorphisms and inhibition on LDL-C lowering and myopathy of statins. Xenobiotica 41 639-651... 

Y., Irie, S., Ware, J., Nakai, Y., Higuchi, S. and Sugiyama, Y. (2008) Pharmacogenetic characterization of sulfasalazine disposition based on NAT2 and ABCG2 BCRP) gene polymorphisms in humans. Clinical Pharmacology and Therapeutics 84, 95-103. 

Z. R., Fen, J., Huang, Y.F. and Zhou, H.H. (2006) Role of BCRP 421C>A polymorphism on rosuvastatin pharmacokinetics in healthy Chinese... 

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