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Irinotecan is a hydrophilic compound with a large volume of distribution (400 L/m 2). [20] [21] At physiological pH, irinotecan and its active metabolite ethyl-10-hydroxy-camptothecin (SN-38) are present in two pH-dependent equilibrium isoforms; the anti tumor active lactone ring which hydrolyzed to the carboxylate isoform. [21]
It is the active metabolite of irinotecan (an analog of camptothecin - a topoisomerase I inhibitor) but has 1000 times more activity than irinotecan itself. In vitro cytotoxicity assays show that the potency of SN-38 relative to irinotecan varies from 2- to 2000-fold.
The regimen consists of: irinotecan (180 mg/m 2 IV over 90 minutes) concurrently with folinic acid (400 mg/m 2 [or 2 x 250 mg/m 2] IV over 120 minutes); followed by fluorouracil (400–500 mg/m 2 IV bolus) then fluorouracil (2400–3000 mg/m 2 intravenous infusion over 46 hours).
Synthetic lethality with the topoisomerase inhibitor irinotecan appears to occur when given to cancer patients with deficient expression of the DNA repair gene WRN. [ citation needed ] The analysis of 630 human primary tumors in 11 tissues shows that hypermethylation of the WRN CpG island promoter (with loss of expression of WRN protein) is a ...
Also, the doses (Day 1: irinotecan 165 mg/m2 IV, plus oxaliplatin 85 mg/m2 IV; Day 1: leucovorin 400 mg/m2; Days 1–3: fluorouracil 1,600 mg/m2/day × 2 days (total 3,200 mg/m2 over 48 hours) continuous infusion starting on day 1; Day 1: bevacizumab 5 mg/kg IV; repeat cycle every 2 weeks) [1] [8] [9] are slightly dissimilar to FOLFIRINOX.
Camptothecin (CPT) is a topoisomerase inhibitor.It was discovered in 1966 by M. E. Wall and M. C. Wani in systematic screening of natural products for anticancer drugs.It was isolated from the bark and stem of Camptotheca acuminata (Camptotheca, Happy tree), a tree native to China used in traditional Chinese medicine.
Irinotecan is a prodrug [6] used in the treatment of many solid tumours, including colorectal, pancreatic, and lung cancer. [41] Irinotecan is metabolized into its active compound SN-38, which inhibits the enzyme topoisomerase-1 , involved in DNA replication. [ 42 ]
In 1996 a more stable analogue, irinotecan, won Food and Drug Administration (FDA) approval for the treatment of colon cancer. Later, this agent would also be used to treat lung and ovarian cancers. Later, this agent would also be used to treat lung and ovarian cancers.