Evaluation of in vivo P-glycoprotein phenotyping probes: a need for validation.
Clin Pharmacokinet
; 49(4): 223-37, 2010 Apr.
Article
em En
| MEDLINE
| ID: mdl-20214407
ABSTRACT
Drug transporters are involved in clinically relevant drug-drug interactions. P-glycoprotein (P-gp) is an efflux transporter that displays genetic polymorphism. Phenotyping permits evaluation of real-time, in vivo P-gp activity and P-gp-mediated drug-drug interactions. Digoxin, fexofenadine, talinolol and quinidine are commonly used probe drugs for P-gp phenotyping. Although current regulatory guidance documents highlight methodologies for evaluating transporter-based drug-drug interactions, whether current probe drugs are suitable for phenotyping has not been established, and validation criteria are lacking. This review proposes validation criteria and evaluates P-gp probes to determine probe suitability. Based on these criteria, digoxin, fexofenadine, talinolol and quinidine have limitations to their use and are not recommended for P-gp phenotyping.
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Base de dados:
MEDLINE
Assunto principal:
Membro 1 da Subfamília B de Cassetes de Ligação de ATP
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Interações Medicamentosas
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Medicamentos sob Prescrição
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article