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Current Drug Metabolism


ISSN (Print): 1389-2002
ISSN (Online): 1875-5453

PepT1, ASBT-Linked Prodrug Strategy to Improve Oral Bioavailability and Tissue Targeting Distribution

Author(s): Xiaopeng Han, Jin Sun, Yongjun Wang and Zhonggui He

Volume 16 , Issue 1 , 2015

Page: [71 - 83] Pages: 13

DOI: 10.2174/1389200216666150401110754

Price: $65


With the rapid development of molecular biology, various of drug transporters have been discovered in several important organs of the body, which determine intracellular exposure and pharmacokinetic performances of drugs by modulating cellular entry and exit. This article focuses on the design of transporter-linked prodrug to enhance oral bioavailability and to acquire tissue-specific distribution pattern, especially paying attention to peptide transporter 1 (PepT1) and apical sodium dependent bile acid transporter (ASBT). Conjugation of the native promotety to active drug was one of the effective methods to improve membrane permeability and distribution profiles of drugs. In this review, we highlight the transporter-linked prodrug design modality based on PepT1 and ASBT. The biology of transporters, structure-transport relationship, key features of natural substrates and successful examples of transporter-linked prodrugs are overviewed in detail.

Keywords: PepT1, ASBT, prodrug, oral bioavailability, tissue targeting.

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