November 1st 1997
The article by Drs. Takimoto and Arbuck reviews the chemistry, mechanism of action, pharmacology and clinical trials of topotecan (Hycamtin), one of two topoisomerase I inhibitors approved recently by the FDA. Topotecan was approved for refractory ovarian cancer and irinotecan (Camptosar) for advanced colorectal cancer. These drugs represent a new drug class designed to inhibit topoisomerase I, an enzyme involved in relaxation of torsional strain in supercoiled DNA allowing replication and translation. The authors’ overview is informative and unbiased.