Part I: Biochemistry, Pharmacology, and Chemistry Mechanism of Action of Topoisomerase 1 Poisons Leroy F. Liu and Shyamal D. Desai Crystallographic Insight Into the Mechanism of Drug-Induced Topoisomerase I DNA Damage Alex B. Burgin, Jr., Michael D. Feese, Bart L. Staker, and Lance Stewart Inhibitors of Topoisomerase I Function Sidney M. Hecht Cytotoxic Mechanisms of the Topoisomerase 1 Inhibitors Yves G. Pommier, Juana Barcelo, Takahisa Furuta, Haruyuki Takemura, Olivier Sordet, and ZhiYong Liao Biochemical and Genetic Analyses of DNA Topoisomerase 1-Mediated DNA Damage Robert C. A. M. van Waardenburg and Mary-Ann Bjornsti Preclinical Models for Evaluating Topoisomerase I-Targeted Drugs Aarti S. Juvekar, Joyce Thompson, Clinton F. Stewart, and Peter J. Houghton Mechanisms of Resistance to Camptothecins Zeshaan A. Rasheed and Eric H. Rubin Recent Advances in Camptothecin Drug Design and Delivery Strategies Thomas G. Burke, Tian-Xiang Xiang, Bradley D. Anderson, and Lori J. Latus Part II: Clinical Perspectives Clinical Experience With 9-Aminocamptothecin: Lessons for New Drug Development Chris H. Takimoto Clinical Studies of Rubitecan (9-Nitro 20(S) Camptothecin) Hilary Hewes, Judith A. Smith, and Claire Verschraegen Irinotecan: Current Clinical Status and Pharmacological Aspects Laurent P. Rivory Clinical Experience With Topotecan Aimee K. Bence and Val R. Adams The Clinical Development of Lurtotecan: Experience With Water-Soluble and Liposomal Forms Keith T. Flaherty, James P. Stevenson, Christopher J. Twelves, and Peter J. O'Dwyer Preclinical and Clinical Development of Exatecan (DX-8951f): A Hexacyclic Camptothecin Analog Eric K. Rowinsky Camptothecins in the Treatment of Primary Brain Tumors Clinton F. Stewart,Markos Leggas, and Henry S. Friedman Camptothecins in the Treatment of Lung Cancer Pankaj Kumar, Missak Haigentz, Jr., Jorge Gomez, and Roman Perez-Soler Use of Camptothecins in the Treatment of Leukemia and Related Disorders Benjamin M. F. Mow and Scott H. Kaufmann Index