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Brand names,
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Analogs
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Brand Names Mixture
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Chemical_Formula
C33H38N4O6
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RX_link
http://www.rxlist.com/cgi/generic2/irinot.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
T. Miyasaka et al., U.S. pat. 4,604,463 (1985, 1986 both to Yakult Honsha)
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Molecular Weight
586.678 g/mol
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Melting Point
222-223 oC
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H2O Solubility
Soluble
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State
Solid
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LogP
4.372
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Dosage Forms
Solution for IM injection
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Indication
For the treatment of metastatic colorectal cancer (first-line therapy when administered with 5-fluorouracil and leucovorin).
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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).
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Absorption
100%
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side effects and Toxicity
Gastrointestinal complications, such as nausea, vomiting, abdominal cramping, diarrhea, and infection.
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Patient Information
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Organisms Affected
Humans and other mammals