Abstract
Irinotecan (CPT-11) is a potent anticancer agent approved for use in the treatment of advanced colorectal cancer, as either a first-line therapy in combination with 5-fluorouracil or in the treatment of 5-flurouracil refractory cases (Sawada et al., 1995; Saltz, 1997). Irinotecan is a prodrug designed to deliver the poorly soluble parent molecule SN-38, an analog of a highly potent plant alkaloid camptothecin (CPT). Camptothecin and its analogs inhibit the nuclear enzyme topoisomerase I, inhibiting replication and demonstrating antitumor activity as an S-phase-specific drug (Garcia-Carbonero and Supko, 2002). The structure and enzymatic bioconversion of CPT-11 to SN-38 is shown in Scheme 1.
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Hageman, M.J., Morozowich, W. (2007). Case Study: Irinotecan (CPT-11), A Water-soluble Prodrug of SN-38. In: Stella, V.J., Borchardt, R.T., Hageman, M.J., Oliyai, R., Maag, H., Tilley, J.W. (eds) Prodrugs. Biotechnology: Pharmaceutical Aspects, vol V. Springer, New York, NY. https://doi.org/10.1007/978-0-387-49785-3_44
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DOI: https://doi.org/10.1007/978-0-387-49785-3_44
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