Irinotecan medac

Active Ingredient

Irinotecan hydrochloride trihydrate

Mode of Action

Irinotecan is a semisynthetic derivative of camptothecin. It is an antineoplastic agent that acts as a specific inhibitor of DNA topoisomerase-I. In most tissues, irinotecan is metabolised by carboxylesterase to SN-38, which was found to be more active than irinotecan in purified topoisomerase-I and more cytotoxic than irinotecan for several mouse and human tumour cell lines. Inhibition of DNA topoisomerase-I by irinotecan or SN-38 causes single-stranded DNA lesions that block the DNA replication fork and are responsible for cytotoxicity. The cytotoxic effect was found to be time-dependent and specific to S-phase. Besides antitumour activity, the most significant pharmacological effect of irinotecan is the inhibition of acetylcholinesterase.

Indication

• Advanced colorectal cancer in combination with 5-FU and folinic acid in patients without prior chemotherapy for advanced disease; as single agent in patients who have failed an established 5-FU containing treatment regimen
• EGFR-expressing, KRAS wild-type metastatic colorectal cancer in combination with cetuximab without prior treatment for metastatic disease or after failure of irinotecan-including cytotoxic therapy
• First-line treatment of metastatic carcinoma of the colon or rectum in combination with 5-fluorouracil, folinic acid and bevacizumab
• First-line treatment of metastatic colorectal carcinom in combination with capecitabine with or without bevacizumab

Dosage

Concentrate for solution for infusion:

• 40 mg (2 ml)
• 100 mg (5 ml)
• 300 mg (15 ml)
• 500 mg (25 ml)
• 1000 mg (50 ml)

Not all pack sizes may be marketed.