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Genetic polymorphisms of the CYP3A4, CYP3A5, and MDR-1 genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus

Clinical Pharmacology & Therapeutics · 2003 · Vol. 74(3) · pp. 245–254
Dennis A. Hesselink

Abstract

As a group, patients with the CYP3A5*3/*3 genotype require less tacrolimus to reach target predose concentrations compared with CYP3A5*1 allele carriers, whereas CYP3A4*1B carriers require more tacrolimus to reach target trough concentrations compared with CYP3A4*1 homozygotes.

Renal Transplantation Outcomes and TreatmentsPharmacological Effects and Toxicity StudiesDrug Transport and Resistance MechanismsTacrolimusCalcineurinPharmacokineticsCYP3A5PharmacologyCYP3A4CiclosporinMedicineTrough levelGenotype

MeSH terms

Cytochrome P-450 Enzyme SystemDNADose-Response Relationship, DrugFemaleHumansImmunosuppressive AgentsMalePolymorphism, GeneticKidney TransplantationTacrolimusCyclosporineGenes, MDRReverse Transcriptase Polymerase Chain ReactionCytochrome P-450 CYP3ACalcineurin Inhibitors
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Genetic polymorphisms of the CYP3A4, CYP3A5, and MDR-1 genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus · Scinovex