title: Suitability of digoxin as a P-glycoprotein probe: implications of other transporters on sensitivity and specificity.
abstract: The study of transporter-mediated drug-drug interactions (DDI) requires use of appropriate probes to reflect transporter function. Digoxin is often used as a probe in DDI studies involving P-glycoprotein (P-gp) and is recommended by FDA for this purpose, despite several lingering questions regarding suitability of digoxin as P-gp probe. This review aims to critically evaluate use of digoxin as a probe for P-gp-mediated clinical DDI studies, with focus on sensitivity and specificity of digoxin for P-gp. Although previous reviews have evaluated digoxin transport by P-gp, the purpose of the current review is to critically evaluate such literature in light of newly evolving literature suggesting digoxin transport by non-P-gp transporters.
authors.affiliation: Pharmaceutical Sciences Section, College of Pharmacy, Qatar University, Doha, Qatar.
authors.forename: Ahmed M
authors.initials: AM
authors.lastname: Nader
authors.forename: David R
authors.initials: DR
authors.lastname: Foster
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000235:genetics / Q000378:metabolism*; D000818:Animals; D002352:Carrier Proteins / Q000235:genetics / Q000378:metabolism*; D004077:Digoxin; D004347:Drug Interactions; D018565:Food-Drug Interactions; D006801:Humans; D004364:Pharmaceutical Preparations / Q000378:metabolism
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D002352:Carrier Proteins; D004364:Pharmaceutical Preparations; D004077:Digoxin
keywords: OATP; P-glycoprotein; digoxin; drug-drug interaction; transporter