Topotecan-d6 is intended for use as an internal standard for the quantification of topotecan by GC- or LC-MS. Topotecan is an inhibitor of DNA topoisomerase I and a derivative of the DNA topoisomerase I inhibitor camptothecin .1,2,3 Topotecan inhibits DNA topoisomerase I in human MCF-7 breast and DU145 prostate cancer cells with IC50 values of 13 and 2 nM, respectively, in a cell-based luciferase reporter assay.4 Topotecan induces cytotoxicity and DNA damage in HT-29 human colon adenocarcinoma cells (IC50s = 33 and 280 nM, respectively).1 Formulations containing topotecan have been used in the treatment of small-cell lung cancer.
|1. Rothenberg, M.L. Topoisomerase I inhibitors: Review and update. Ann. Oncol. 8(9), 837-855 (1997).|2. Dancey, J., and Eisenhauer, E.A. Current perspectives on camptothecins in cancer treatment. Br. J. Cancer 74(3), 327-338 (1996).|3. Schellens, J.H., Creemers, G.J., Beijnen, J.H., et al. Bioavailability and pharmacokinetics of oral topotecan: A new topoisomerase I inhibitor. Br. J. Cancer 73(10), 1268-1271 (1996).|4. Caceres, G., Zankina, R., Zhu, X., et al. Determination of chemotherapeutic activity in vivo by luminescent imaging of luciferase-transfected human tumors. Anticancer Drugs 14(7), 569-574 (2003).