Irinotecan (Camptosar)

General information

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.^[1]^[2]
Route: IV
Extravasation: irritant

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.^[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

1996-06-14: Initial accelerated 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. (Based on Rothenberg et al. 1996, Pitot et al. 1997, Rougier et al. 1997, and Rothenberg et al. 1999)
- 1998-10-22: Converted to regular 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. (Based on V301 & V302)
2000-04-20: 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. (Based on Douillard et al. 2000 & Saltz et al. 2000)

History of changes in EMA indication

1995-05-05: EURD

History of changes in PMDA indication

2013-03-25: New additional indication and a new dosage for the treatment of pediatric malignant solid tumor.
2013-12-20: New additional indication and a new dosage for the treatment of unresectable pancreatic cancer.

Also known as

Generic name: irinotecan hydrochloride trihydrote
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, Satigene, Tecnotecan, Tekamen, Toptecin, Trinotecan, Winol

References

[insert-1] 1.0 ^1.1 ^1.2 Irinotecan (Camptosar) package insert

[2] Irinotecan (Camptosar) package insert (locally hosted backup)

[3] Irinotecan (Camptosar) patient drug information (Chemocare)

[4] Irinotecan (Camptosar) patient drug information (UpToDate)

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