The Interactions of Anti-Cancer Drugs Approved in the Last Decade in the United States with Membrane Transporters

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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The Interactions of Anti-Cancer Drugs Approved in the Last Decade in the United States with Membrane Transporters

Anti-Cancer Agents in Medicinal Chemistry, 10(8): 601-616.

Author(s): Lokesh Jain, Sophia Abraham and Stacy S Shord.

Affiliation: FDA/CDER/OTS/OCP/DCP2, 10903 New Hampshire Avenue, Building 51, Room 2219, Silver Spring MD 20993 USA.


Membrane transporters play a role in determining the absorption, distribution, metabolism and excretion of small molecule anticancer drugs and mediating chemosensitivity and resistance of tumor cells to these drugs. Our understanding of the influence of these transporters on the pharmacokinetics, clinical effectiveness and tolerability has considerably increased in the last decade. We reviewed the interaction of the small molecule anticancer drugs approved in the last decade with the more common membranes transporters, such as ABCB1, ABCG2, and OATP. The drugs were divided into three categories: targeted therapies, cytotoxic agents and hormonal therapies. The literature appears to focus on the interaction of the targeted therapies compared to the remaining two categories. Furthermore, most data stemmed from nonclinical studies with only a few clinical examples where transporters corresponded with systemic exposure, clinical effectiveness, or tolerability. More nonclinical and clinical studies are needed to improve the ability to use the findings from these nonclinical studies to predict clinical outcomes, but the literature appears to be rapidly expanding as our understanding of these transporters grows. Therefore, determining the interaction of membrane transporters with small molecule anticancer drugs can facilitate the development of effective and safe treatments.


Cytotoxic agents, drug resistance, drug-drug interactions, hormonal therapies, pharmacokinetics, targeted anticancer therapies, transporters.

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Article Details

Volume: 10
Issue Number: 8
First Page: 601
Last Page: 616
Page Count: 16
DOI: 10.2174/187152010794473966
Price: $58

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