Name: | irinotecan |
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PubChem Compound ID: | 104842 |
Molecular formula: | C22H20N2O5 |
Molecular weight: | 392.405 g/mol |
Synonyms: |
EHC; SN-38; 7-Ethyl-10-hydroxy-camptothecin; 1H-Pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4H,12H)-dione, 4,7-diethyl-4,10-dihydroxy-; 86639-52-3; SN38; NCI60_026056; AIDS-058635; AIDS058635; Captothecin, 7-ethyl-10-hydroxy-.
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Name: | irinotecan |
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Name (isomeric): | DB00762 |
Drug Type: | small molecule |
Synonyms: |
Irinotecanum [INN-Latin]; Irinotecan Hydrochloride Trihydrate; Irinotecan Hcl; Irinotecan Hydrochloride
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Brand: | IRINOTECAN, CPT-11, Camptosar, CP0 |
Category: | Parasympathomimetics, Prodrugs, Radiation-Sensitizing Agents, Antineoplastic Agents, Enzyme Inhibitors, Antineoplastic Agents, Phytogenic |
CAS number: | 100286-90-6 |
Indication: | For the treatment of metastatic colorectal cancer (first-line therapy when administered with 5-fluorouracil and leucovorin). Also used in combination with cisplatin for the treatment of extensive small cell lung cancer. Irinotecan is currently under investigation for the treatment of metastatic or recurrent cervical cancer. |
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Pharmacology: |
Irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. Irinotecan is a semisynthetic derivative of camptothecin. Camptothecins interact specifically with topoisomerase I, an enzyme in the cell nucleus that regulates DNA topology and facilitates nuclear processes such as DNA replication, recombination,...
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Mechanism of Action: |
Irinotecan inhibits the action of topoisomerase I. Irinotecan prevents religation of the DNA strand by binding to topoisomerase I-DNA complex. The formation of this ternary complex interferes with the moving replication fork, which induces replication arrest and lethal double-stranded breaks in DNA. As a result, DNA damage is not efficiently repair...
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Absorption: | 100% |
Protein binding: | 30%-68% |
Biotransformation: | Hepatic |
Route of elimination: | The cumulative biliary and urinary excretion of irinotecan and its metabolites (SN-38 and SN-38 glucuronide) over a period of 48 hours following administration of irinotecan in two patients ranged from approximately 25% (100 mg/m2) to 50% (300 mg/m2). |
Half Life: | 6-12 hours |
Toxicity: | Gastrointestinal complications, such as nausea, vomiting, abdominal cramping, diarrhea, and infection. |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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