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Irinotecan in the Treatment of Colorectal Cancer

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Colorectal Cancer

Part of the book series: Current Clinical Oncology ((CCO))

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Abstract

Irinotecan, also known as CPT-11, is a semisynthetic derivative of the plant alkaloid camptothecin. The antitumor activity of the camptothecin derivatives is accomplished via inhibition of the nuclear enzyme topoisomerase I (topo I).Topo I facilitates DNA uncoiling for replication and transcription by binding to DNA and causing reversible single-stranded DNA breaks (1). Under normal circumstances, these single-stranded breaks are transient and readily reversible. However, in the presence of irinotecan or its active metabolite, SN-38 (2), these single-stranded breaks are stabilized and potentiated. This stabilization is also reversible and nonlethal. However, if a replication fork collides with one of these stabilized single-stranded breaks, double-stranded breaks and DNA fragmentation occurs, leading to cell death (3).

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Authors
  1. Leonard B. Saltz
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Editors and Affiliations

  1. Gastrointestinal Oncology Division, Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, NY, USA

    Leonard B. Saltz MD

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© 2002 Springer Science+Business Media New York

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Saltz, L.B. (2002). Irinotecan in the Treatment of Colorectal Cancer. In: Saltz, L.B. (eds) Colorectal Cancer. Current Clinical Oncology. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-59259-160-2_28

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  • DOI: https://doi.org/10.1007/978-1-59259-160-2_28

  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-4684-9670-3

  • Online ISBN: 978-1-59259-160-2

  • eBook Packages: Springer Book Archive

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