Products
Irinotecan is commercially available as an infusion concentrate (Campto, generic). It has been approved in many countries since 1998. In 2017, the nanoliposomal formulation irinotecan sucrosofate was released (Onivyde).
Structure and properties
Irinotecan (C33H38N4O6, Mr = 586.7 g/mol) is a semisynthetic derivative of camptothecin, a plant alkaloid derived from the tree. In the drug product, it is present as irinotecan hydrochloride trihydrate. Irinotecan has an active metabolite, SN-38 (7-ethyl-10-hydroxycamptothecin), which is formed by carboxylesterases. Because this is much more active, irinotecan can be considered a prodrug.
Effects
Irinotecan (ATC L01XX19) has cytotoxic and antitumor properties. The effects are due to selective inhibition of topoisomerase I. This causes single-strand breaks in DNA, ultimately leading to cancer cell death.
Indications
- For the treatment of advanced and metastatic carcinoma of the colon and rectum (colon cancer, combination therapy).
- Pancreatic cancer, see under irinotecansucrosofate.
Dosage
According to the professional information. The drug is administered as an intravenous infusion.
Contraindications
For complete precautions, see the drug label.
Interactions
Irinotecan is a substrate of CYP3A4 and the active metabolite is glucuronidated by UGT1A1. Corresponding drug-drug interactions with inhibitors and inducers are possible and must be considered during treatment.
Adverse effects
The most common possible adverse effects include nausea, vomiting, abdominal pain, diarrhea, constipation, poor appetite, neutropenia, leukopenia, anemia, weakness, fever, weight loss, and hair loss.
