alexa In vitro and In vivo Relevance of the P-glycoprotein Probe Substrates in Drug Discovery and Development: Focus on Rhodamine 123, Digoxin and Talinolol
ISSN: 0975-0851

Journal of Bioequivalence & Bioavailability
Open Access

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Research Article

In vitro and In vivo Relevance of the P-glycoprotein Probe Substrates in Drug Discovery and Development: Focus on Rhodamine 123, Digoxin and Talinolol

Ana Fortuna1,2, Gilberto Alves2,3 and Amílcar Falcão1,2*

1Laboratory of Pharmacology, Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal

2Centre for Neurosciences and Cell Biology, University of Coimbra, 3004-517 Coimbra, Portugal

3CICS-UBI – Health Sciences Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, Portugal

*Corresponding Author:
Amílcar Falcão, PharmD, Ph.D.
Laboratory of Pharmacology
Faculty of Pharmacy, University of Coimbra
Pólo das Ciências da Saúde
Azinhaga de Santa Comba 3000-548 Coimbra, Portugal
Phone: +351 239488400
Fax: +351 239 827126
E-mail: [email protected]

Received Date: August 01, 2011; Accepted Date: August 18, 2011; Published Date: August 20, 2011

Citation: Fortuna A, Alves G, Falcão A (2011) In vitro and In vivo Relevance of the P-glycoprotein Probe Substrates in Drug Discovery and Development: Focus on Rhodamine 123, Digoxin and Talinolol. J Bioequiv Availab S2. doi: 10.4172/jbb.S2-001

Copyright: © 2011 Fortuna A, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.



P-glycoprotein (P-gp), an efflux transporter expressed in tumour and normal tissues, may significantly affect pharmacodynamics and pharmacokinetics of the drug, compromising its pharmacological effect. During drug discovery and development (DDD) programs, identification of compounds that are substrates, inhibitors or inducers of P-gp can aid drug candidate selection and optimization and eventually develop drugs with ideal pharmacological profiles and low potential for drug-drug interactions mediated by P-gp. Toward this end, rhodamine 123 (Rho 123), digoxin and talinolol are commonly used as P-gp substrates probes in several in vitro and in vivo models.

This article summarized the significant role of P-gp in drug disposition and the impact of its modulation in the current DDD. Furthermore, an overview of several examples from literature where Rho 123, digoxin and talinolol were used as P-gp substrate probes during different stages of DDD was also herein described. While Rho 123 seemed to be successfully used in early drug discovery and non-clinical development stages, digoxin and talinolol are more frequently applied as clinical in vivo probe drugs for P-gp. However for regulatory submission, Rho 123 cannot be used neither in in vitro investigations and therefore digoxin is preferred since its advantages over talinolol.

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