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Intestinal Transporter-Associated Drug Absorption and Toxicity

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Drug Transporters in Drug Disposition, Effects and Toxicity

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 1141))

Abstract

Oral drug administration is the most favorable route of drug administration in the clinic. Intestinal transporters have been shown to play a significant role in the rate and extent of drug absorption of some, but not all, drug molecules. Due to the heterogeneous expression of multiple transporters along the intestine, the preferential absorption sites for drugs may vary significantly. In this chapter, we aim to summarize the current research on the expression, localization, function, and regulation of human intestinal transporters implicated in altering the absorption of low to medium molecular weight drug molecules. The role played by bile acid transport proteins (e.g., ASBT and OST-α/β) is included in the discussion. The synergistic action of intestinal drug metabolism and transport is also discussed. Despite the complicated regulatory factors, the biopharmaceutics drug disposition classification system (BDDCS) put forward by Wu and Benet may help us better predict the effect of transporters on drug absorption. The drug-induced toxicity in the intestine, which may result from drug-drug interaction, gut microbiota, and bile salt toxicity, is also discussed.

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Acknowledgments

This chapter was completed with the help of Xin Luo and Chen Ma.

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Authors and Affiliations

  1. Shanghai Institute of Materia Medica, Shanghai, China

    Yaru Xue, Chenhui Ma & Guoyu Pan

  2. Novartis Institutes for Biomedical Research, East Hanover, NJ, USA

    Imad Hanna

  3. University of Chinese Academy of Science, Beijing, China

    Yaru Xue, Chenhui Ma & Guoyu Pan

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  1. Yaru Xue
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  1. School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu, China

    Xiaodong Liu

  2. Shanghai Institute of Materia Medica, Chinese Academy of Science, Shanghai, Shanghai, China

    Guoyu Pan

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Xue, Y., Ma, C., Hanna, I., Pan, G. (2019). Intestinal Transporter-Associated Drug Absorption and Toxicity. In: Liu, X., Pan, G. (eds) Drug Transporters in Drug Disposition, Effects and Toxicity. Advances in Experimental Medicine and Biology, vol 1141. Springer, Singapore. https://doi.org/10.1007/978-981-13-7647-4_8

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