RT Journal Article SR Electronic T1 CANCER CHEMOTHERAPY AND DRUG METABOLISM JF Drug Metabolism and Disposition JO Drug Metab Dispos FD American Society for Pharmacology and Experimental Therapeutics SP 1083 OP 1096 DO 10.1124/dmd.105.004374 VO 33 IS 8 A1 David S. Riddick A1 Chunja Lee A1 Shairoz Ramji A1 Edwin C. Chinje A1 Rachel L. Cowen A1 Kaye J. Williams A1 Adam V. Patterson A1 Ian J. Stratford A1 Charles S. Morrow A1 Alan J. Townsend A1 Youssef Jounaidi A1 Chong-Sheng Chen A1 Ting Su A1 Hong Lu A1 Pamela S. Schwartz A1 David J. Waxman YR 2005 UL http://dmd.aspetjournals.org/content/33/8/1083.abstract AB Drug-metabolizing enzymes and drug transporters are key determinants of the pharmacokinetics and pharmacodynamics of many antineoplastic agents. Metabolism and transport influence the cytotoxic effects of antineoplastic agents in target tumor cells and normal host tissues. This article summarizes several state-of-the-art approaches to enhancing the effectiveness and safety of cancer therapy based on recent developments in our understanding of antineoplastic drug metabolism and transport. Advances in four interrelated research areas presented at a recent symposium sponsored by the Division for Drug Metabolism of the American Society for Pharmacology and Experimental Therapeutics (Experimental Biology 2004; Washington D.C., April 17–21, 2004) are discussed: 1) interactions of anthracyclines with drug-metabolizing enzymes; 2) use of hypoxia-selective gene-directed enzyme prodrug therapy (GDEPT) in combination with bioreductive prodrugs; 3) synergy between glutathione conjugation and conjugate efflux in conferring resistance to electrophilic toxins; and 4) use of cytochromes P450 as prodrug-activating enzymes in GDEPT strategies. A clear theme emerged from this symposium: drug metabolism and transport processes can be modulated and exploited in ways that may offer distinct therapeutic advantages in the management of patients with cancer. The American Society for Pharmacology and Experimental Therapeutics