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Description: Irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. Irinotecan is a derivative of camptothecin. Irinotecan inhibits the action of topoisomerase I. Irinotecan prevents religation of the DNA strand by binding to topoisomerase I-DNA complex, and causes double-strand DNA breakage and cell death.
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. Irinotecan is a derivative of camptothecin. Camptothecins interact specifically with the enzyme topoisomerase I which relieves torsional strain in DNA by inducing reversible single-strand breaks. Irinotecan and its active metabolite SN-38 bind to the topoisomerase I-DNA complex and prevent religation of these single-strand breaks. Current research suggests that the cytotoxicity of Irinotecan is due to double-strand DNA damage produced during DNA synthesis when replication enzymes interact with the ternary complex formed by topoisomerase I, DNA, and either Irinotecan or SN-38. Mammalian cells cannot efficiently repair these double-strand breaks. The precise contribution of SN-38 to the activity of Irinotecan in humans is not known. Irinotecan is cell cycle phase-specific (S-phase).
Mechanism of Action: Irinotecan inhibits the action of topoisomerase I. Irinotecan prevents religation of the DNA strand by binding to topoisomerase I-DNA complex, and causes double-strand DNA breakage and cell death.
Indication: For the treatment of metastatic colorectal cancer (first-line therapy when administered with 5-fluorouracil and leucovorin).
Half Life: 6-12 hours
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Data Correlations | 2 studies

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Genes category icon Genes
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TOP1MT 100 100
Ly6f 96 96
GEM 96 96
Mcpt2 92 92
FKBP5 88 88
EEF1A1 87 87
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Biogroups category icon Biogroups
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Speract/scavenger receptor 100 100
Activation of cAMP-dependent Protei… 99 99
RECK Pathway - Inhibition of Matrix… 98 98
Blood Group Glycolipid Biosynthesis… 97 97
Glycosphingolipid Biosynthesis Lact… 97 97
Blood Group Glycolipid Biosynthesis… 97 97
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Individual Studies

  • Drug target sets for approved compounds

    Homo sapiens Homo sapiens | Therapeutic   Therapeutic

    The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information.

    Authors: David S Wishart, Craig Knox, An Chi Guo et al.

    Organization: Department of Computing Science, Univers…

  • Irinotecan-induced gene expression changes in the rat intestine

    Rattus norvegicus Rattus norvegicus | RNA Expression   RNA Expression

    The aim of the study was therefore to determine the early time course of gene expression changes along the gastrointestinal tract (GIT) of the DA rat following irinotecan treatment, so as to provide an insight into the genetic component of mucositis.

    Authors: Bowen M Joanne, Gibson J Rachel, Tsykin Anna et al.

    Organization: Royal Adelaide Hospital Medical Oncology…
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Associated Researchers

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Thought leaders and organizations working on research involving irinotecan.

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  • A Falcone
  • John W Park
  • Wei Duan
  • R Danesi
  • Ron H J Mathijssen
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  • Pfizer
  • Gachon University Gil Medical Center
  • USC/Norris Comprehensive Cancer Center
  • Amgen
  • National Cancer Institute (NCI)
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  • Stanford University
  • University of North Carolina
  • Duke University Medical Center
  • National University of Singapore
  • University of Pisa

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