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Review

Pharmacogenetics of ATP-binding Cassette Transporters in Cancer and Chemotherapy¹

Departments of Medicine and Clinical Pharmacology, Vanderbilt University Medical Center, Nashville, Tennessee 37232

² To whom requests for reprints should be addressed, at 572 RRB, 23rd Avenue at Pierce Avenue, Division of Clinical Pharmacology, Vanderbilt University School of Medicine, Nashville, TN 37232-6602. Phone: (615) 343-1522; Fax: (615) 343-7605; E-mail: richard.kim{at}vanderbilt.edu

The ATP-binding cassette (ABC) transporters belong to the largest known transporter gene family and translocate a variety of substrates including chemotherapy agents. ABC multidrug transporter expression has been implicated in tumor cell resistance to anticancer therapy, altered disposition of chemotherapy drugs, and associated chemotherapy toxicity. More recently, genetic heterogeneity has been described in a number of the ABC transporter genes, including ABC transporters that contribute to the pharmacokinetics and/or pharmacodynamics of chemotherapy drugs. The role of these transporters and their naturally occurring genetic polymorphisms in cancer and chemotherapy is reviewed.