CYP3A5 genotype does not influence everolimus metabolism and in vitro clinical pharmacokinetics in renal transplant recipients

نویسندگان

  • Nicolas Picard
  • Nassim Kamar
  • Lionel Rostaing
  • Pierre Marquet
چکیده

Background genotyping might be useful to guide tacrolimus and sirolimus dosing. The aim of this study was to assess the influence of CYP3A5 polymorphism on everolimus metabolism and pharmacokinetics. CYP3A5

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منابع مشابه

CYP3A5 genotype does not influence everolimus in vitro metabolism and clinical pharmacokinetics in renal transplant recipients.

BACKGROUND CYP3A5 genotyping might be useful to guide tacrolimus and sirolimus dosing. The aim of this study was to assess the influence of CYP3A5 polymorphism on everolimus metabolism and pharmacokinetics. METHODS We investigated the effect of CYP3A5 6986A>G polymorphism (CYP3A5*1/*3 alleles) on the pharmacokinetics of everolimus in 28 renal transplant patients and on its in vitro hepatic me...

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بررسی پلی مورفیسم ژن های CYP3A5، MDR1 و ارتباط آن با غلظت خونی سیکلوسپورین در مراحل اولیه بعد از پیوند کلیه در بیماران شیراز

  Background & Aims: The immunosuppressive drug cyclosporine with a narrow therapeutic range and variable pharmacokinetic characteristics among individuals is a substrate for cytochrome P450 (CYP) 3A and P-glycoprotein, the product of the multidrug resistance 1 (MDR1) gene. Some of the single nucleotide polymorphisms (SNPs) in these genes are associated with deficient protein expression and red...

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بررسی پلی مورفیسم ژن های CYP3A5، MDR1 و ارتباط آن با غلظت خونی سیکلوسپورین در مراحل اولیه بعد از پیوند کلیه در بیماران شیراز

  Background & Aims: The immunosuppressive drug cyclosporine with a narrow therapeutic range and variable pharmacokinetic characteristics among individuals is a substrate for cytochrome P450 (CYP) 3A and P-glycoprotein, the product of the multidrug resistance 1 (MDR1) gene. Some of the single nucleotide polymorphisms (SNPs) in these genes are associated with deficient protein expression and red...

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Prediction of Tacrolimus Exposure by CYP3A5 Genotype and Exposure of Co-Administered Everolimus in Japanese Renal Transplant Recipients

While tacrolimus and everolimus have common metabolic pathways through CYP3A4/5, tacrolimus is metabolized solely by CYP3A4 in recipients with the CYP3A5*3/*3. The purpose of this study was to evaluate how the area under the blood concentration-time curves (AUC) of tacrolimus could be predicted based on CYP3A5 genotype and the AUC of everolimus in renal transplant patients taking both drugs. Th...

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Effect of CYP3A4*22, CYP3A5*3, and CYP3A Combined Genotypes on Cyclosporine, Everolimus, and Tacrolimus Pharmacokinetics in Renal Transplantation

Cyclosporine, everolimus, and tacrolimus are the cornerstone of immunosuppressive therapy in renal transplantation. These drugs are characterized by narrow therapeutic windows, highly variable pharmacokinetics (PK), and metabolism by CYP3A enzymes. Recently, the decreased activity allele, CYP3A4*22, was described as a potential predictive marker for CYP3A4 activity. This study investigated the ...

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تاریخ انتشار 2012