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Irinotecan
drug data and news
Irinotecan drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Irinotecan | ||
| Brand Names/Synonyms | CP0; Camptosar; IRINOTECAN, CPT-11; Irinotecan; Irinotecan Hcl; Irinotecan Hydrochloride; Irinotecan Hydrochloride Trihydrate; Irinotecanum [Inn-Latin] | ||
| Indication | For the treatment of metastatic colorectal cancer (first-line therapy when administered with 5-fluorouracil and leucovorin) | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Irinotecan News (When available) |
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| Dosage Forms | IV Solution | ||
| Drug_Category | Radiation-Sensitizing Agents; Prodrugs; Parasympathomimetics; Antineoplastic Agents; Enzyme Inhibitors; ATC:L01XX19 | ||
| Absorption | 100% | ||
| Interactions |
-->Interactions for Irinotecan: The adverse effects of CAMPTOSAR, such as myelosuppression and diarrhea, would be expected to be exacerbated by other antineoplastic agents having similar adverse effects. Patients who have previously received pelvic/ abdominal irradiation are at increased risk of severe myelosuppression following the administration of CAMPTOSAR. The concurrent administration of CAMPTOSAR with irradiation has not been adequately studied and is not recommended. Lymphocytopenia has been reported in patients receiving CAMPTOSAR, and it is possible that the administration of dexamethasone as antiemetic prophylaxis may have enhanced the likelihood of this effect. However, serious opportunistic infections have not been observed, and no complications have specifically been attributed to lymphocytopenia. Hyperglycemia has also been reported in patients receiving CAMPTOSAR. Usually, this has been observed in patients with a history of diabetes mellitus or evidence of glucose intolerance prior to administration of CAMPTOSAR. It is probable that dexamethasone, given as antiemetic prophylaxis, contributed to hyperglycemia in some patients. The incidence of akathisia in clinical trials of the weekly dosage schedule was greater (8.5%, 4/47 patients) when prochlorperazine was administered on the same day as CAMPTOSAR than when these drugs were given on separate days (1.3%, 1/80 patients). The 8.5% incidence of akathisia, however, is within the range reported for use of prochlorperazine when given as a premedication for other chemotherapies. It would be expected that laxative use during therapy with CAMPTOSAR would worsen the incidence or severity of diarrhea, but this has not been studied. In view of the potential risk of dehydration secondary to vomiting and/or diarrhea induced by CAMPTOSAR, the physician may wish to withhold diuretics during dosing with CAMPTOSAR and, certainly, during periods of active vomiting or diarrhea. Drug-Laboratory Test Interactions There are no known interactions between CAMPTOSAR and laboratory tests. | ||
| Toxicity | gastrointestinal complications, such as nausea, vomiting, abdominal cramping, diarrhea, and infection | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | irinotecan hydrochloride | ||
| Chemical Formula | C33H38N4O6 | ||
| Molecular Weight | 586.678 g/mol | ||
| Smiles String | CCC1=C2C=C(C=CC2=NC3=C1CN4C3=CC5=C(C4=O)COC(=O)C5(CC)O)OC(=O)N6CCC(CC6)N7CCCCC7 | ||
| Melting Point | 222-223 °C | ||
| Water Solubility | Soluble | ||
| State | pale yellow to yellow crystalline powder | ||
| LogP/Hphobicity | 4.372 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 6-12 hours | ||
| Protein Binding [%] | 30%-68% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Irinotecan.html http://www.rxlist.com/cgi/generic2/irinot.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00579 | ||
| CAS Registry Number | 100286-90-6 | ||
| KEGG Compound ID | Not Available | ||
| PubChem ID | SID:217212 | ||
| PharmGKB ID | PA450085 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2231622 |
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