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QuickView for Irinotecan (compound)

Name: irinotecan
PubChem Compound ID: 104842
Molecular formula: C22H20N2O5
Molecular weight: 392.405 g/mol
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
Name (isomeric): DB00762
Drug Type: small molecule
Irinotecanum [INN-Latin]; Irinotecan Hydrochloride Trihydrate; Irinotecan Hcl; Irinotecan Hydrochloride
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.
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:
TelithromycinTelithromycin may reduce clearance of Irinotecan. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Irinotecan if Telithromycin is initiated, discontinued or dose changed.
AprepitantAprepitant may change levels of the chemotherapy agent, irinotecan.
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of irinotecan by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of irinotecan if voriconazole is initiated, discontinued or dose changed.
TrastuzumabTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
ThiotepaThiotepa, a strong CYP2B6 inhibitor, may decrease the metabolism and clearance of Irinotecan, a CYP2B6 substrate. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Irinotecan if Thiotepa is initiated, discontinued or dose changed.
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