Class/mechanism: Topoisomerase I inhibitor; derivative of camptothecin, which interferes with topoisomerase I's normal action of relieving torsional strain in DNA by creating reversible
single-strand breaks. Irinotecan and its active metabolite SN-38 bind to the topoisomerase
I & DNA complex and interfere with ligation of these single-strand breaks. Failure to repair these breaks eventually leads to double-strand DNA damage, which disrupts cell proliferation and leads to cell death.
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.
Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 6/14/1996: Initial FDA approval for the treatment of patients with metastatic carcinoma of the colon or rectum whose disease has recurred or progressed following 5-FU-based therapy.
- 4/20/2000: Indicated as a component of first-line therapy in combination with 5-fluorouracil and leucovorin for patients with metastatic carcinoma of the colon or rectum.
- 4/20/2000: Also indicated for patients with metastatic carcinoma of the colon or rectum whose disease has recurred or progressed following initial fluorouracil-based therapy.
Also known as
- Code names: Camptothecin-11, CPT-11, U-101440E
- Brand names: Axinotecan, Biotecan, Biskam, Campto, Campostar, Camptosar, Elinatecan, Faultenocan, Irenax, Irinogen, Irinomedac, Irinotel, Irinotesin, Irnocam, Itoxaril, Linatecan, Onivyde, Satigene, Tecnotecan, Tekamen, Toptecin, Trinotecan, Winol