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.
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.

Diseases for which it is used

• Carcinoma of unknown primary
• Anaplastic glioma
• Cervical cancer
• Colorectal cancer
  • Rectal cancer
• Esophageal cancer
  • Esophageal adenocarcinoma
  • Esophageal squamous cell carcinoma
• Ewing sarcoma
• Gallbladder cancer
• Gastric cancer
• Glioblastoma
• Neuroblastoma
• Non-small cell lung cancer
• Pancreatic cancer
• Penile cancer
• Rhabdomyosarcoma
• Small cell lung cancer

Patient drug information

• Irinotecan (Camptosar) package insert
• Irinotecan (Camptosar) patient drug information (Chemocare)
• Irinotecan (Camptosar) patient drug information (UpToDate)

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