Irinotecan
- Atc Codes:L01XX19
- CAS Codes:136572-09-3#97682-44-5
- PHARMGKB ID:136572-09-3#97682-44-5
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Arinotec, Campto, Irinotecan; Belgium: Campto, Irinotecan, Irinosin; Bulgaria: Campto, Irinotecan, Irinto; Czech Republic: Campto, Canri, Flamborin, Irinotecan, Irinoxin; Denmark: Campto, Irinotecan; Estonia: Campto, Irinotecan, Jovadolin; Finland: Campto, Irinotecan; France: Campto, Irinotecan; Germany: Axinotecan, Campto, Irinomedac, Irinotecan, Irinotecanhydrochorid, Irinotesin, Riboirino; Greece: Biotecan, Campto, Irinocan, Irinotecan, Santacil; Hungary: Campto, Irinotecan, Zetonec; Ireland: Campto, Irinotecan; Italy: Campto, Irinotecan; Latvia: Campto, Irinotecan, Irinotecion; Lithuania: Irinotecan; Luxembourg: Campto; Malta: Campto, Irinotecan; Netherlands: Campto, Irinotecan, Iritec, Irinotecanhydrochloridetrihydraat; Poland: Campto, Irinotecan, Irinotesin; Portugal: Campto, Faultenocan, Irinotecano, Iritec, Irkan; Romania: Campto, Irinotecan, Irinotesin, Jovadolin, Tekazol; Slovakia: Campto, Irinotecan, Irinoxin, Irenax; Slovenia: Campto, Irinotekan, Irinotekanijev; Spain: Campto, Irinotecan; Sweden: Campto, Irinotecan; UK: Campto, Irinotecan.
North America
Canada: Camptosar, Irinotecan; USA: Camptosar, Irinotecan.
Latin America
Argentina: Biotecan, C.P.T. 11, Camptosar, Efixano, Irenax, Irinogen, Irinotecan, Itoxaril, Kebirtecan, Pipetecan, Satigene, Sibudan, Trinotecan, Winol; Brazil: Biotecan, Camptosar, Irenax, Irinotecano, Tecnotecan; Mexico: Camptolem, Camptosar, Daritex-A.
Asia
Japan: Campto, Topotecin.
Drug combinations
Irinotecan, Bevacizumab, Fluorouracil, and Leucovorin
Chemistry
Irinotecan Hydrochloride: C~33~H~38~N~4~O~6~ HCl 3H~2~O. Mw: 677.18. (1) [1,4′-Bipiperidine]-1′-carboxylic acid, 4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinolin-9-yl ester, monohydrochloride, trihydrate, (S)-; (2)(+)-7-Ethyl-10-hydroxycamptothecine 10-[1,4′-bipiperidine]-1′-carboxylate, monohydrochloride, trihydrate. CAS-136572-09-3; CAS-97682-44-5 (irinotecan)(1995).
Pharmacologic Category
Other Antineoplastic Agents. Natural Source (Plant) Derivative, Camptothecin. (ATC-Code: L01XX19).
Mechanism of action
Irinotecan and its active metabolite (SN-38) bind reversibly to topoisomerase I-DNA complex preventing religation of cleaved DNA strand. This results in accumulation of cleavable complexes and double-strand DNA breaks. As mammalian cells cannot efficiently repair these breaks, cell death consistent with S-phase cell cycle specificity occurs, leading to termination of cellular replication.
Therapeutic use
Treatment of metastatic carcinoma of colon or rectum.
Pregnancy and lactiation implications
Teratogenic effects in animal studies. There are no adequate studies in pregnant women. Pregnancy should be avoided during treatment.
Unlabeled use
Lung cancer (small cell and non-small cell), cervical cancer, gastric cancer, pancreatic cancer, leukemia, lymphoma, breast cancer, brain tumors.
Contraindications
Hypersensitivity to irinotecan or any component of the formulation. Concurrent use of ketoconazole, St. John’s wort.
Warnings and precautions
Hazardous agent. May cause severe myelosuppression. Colitis, complicated by ulceration, bleeding, ileus, and infection reported. Two severe (life-threatening) forms of diarrhea might occur (early and late diarrhea). Severe hypersensitivity reactions occurred. Renal impairment and acute renal failure reported, possibly due to dehydration secondary to diarrhea. Patients with bowel obstruction should not be treated with irinotecan until resolution of obstruction. Use with caution in hepatic impairment. Patients with hyperbilirubinemia, or abnormal glucuronidation of bilirubin, may be at risk of myelosuppression when receiving therapy with irinotecan (use caution when treating known hepatic dysfunction or hyperbilirubinemia). Use with caution in elderly patients with comorbid conditions, or baseline performance status of 2. Patients homozygous for the UGT1A1*28 allele are at increased risk of neutropenia. Heterozygous carriers of the UGT1A1*28 allele may also be at increased risk. Use with caution in patients who have previously received pelvic/abdominal radiation. Product contains sorbitol.