Literature DB >> 21142914

SLCO1B1 genetic polymorphism influences mycophenolic acid tolerance in renal transplant recipients.

Hugues Michelon1, Jörg König, Antoine Durrbach, Lina Quteineh, Céline Verstuyft, Valérie Furlan, Sophie Ferlicot, Alexia Letierce, Bernard Charpentier, Martin F Fromm, Laurent Becquemont.   

Abstract

AIMS: This study aimed to determine the influence of gene candidates on mycophenolic acid (MPA) response during the first year of renal transplantation. MATERIALS &
METHODS: A total of 218 renal transplant recipients who received MPA from the first day of transplantation at a fixed dose of 2 g/day were genotyped for ABCB1, ABCC2, UGT2B7, UGT1A9, SLCO1B1, SLCO1B3 and IMPDH1 polymorphisms. Clinical end points were MPA-related adverse drug reactions (ADRs) and acute rejection episodes during the first year post-transplantation.
RESULTS: After correction for multiple statistical testing, SLCO1B1 (encoding the hepatic uptake transporter OATP1B1) was the only gene associated with MPA-related ADRs, showing a 75% risk reduction in favor of a protective effect of the SLCO1B1*5 allele (p = 0.002). In vitro experiments showed that MPA metabolites MPA-phenyl-glucuronide and MPA-acyl-glucuronide are substrates of OATP1B1. Their transport was decreased in the presence of the variant transporter (OATP1B1*5).
CONCLUSION: These results suggest for the first time that carriers of the SLCO1B1*5 allele seem to be protected from MPA-related ADRs.

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Year:  2010        PMID: 21142914     DOI: 10.2217/pgs.10.132

Source DB:  PubMed          Journal:  Pharmacogenomics        ISSN: 1462-2416            Impact factor:   2.533


  14 in total

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Review 10.  Plasma membrane transporters in modern liver pharmacology.

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