Which of the following drugs is topoisomerase 1 inhibitor?
CAM PTOTHECIN ANALOGUES Topotecan and Irinotecan are two recently introduced semisynthetic analogues of camptothecin, an anti tumour principle obtained from a Chinese tree. They act in a manner similar to etoposide, but interact with a different enzyme (DNA topoisomerase I). Their binding to this nuclear enzyme allows single strand breaks in DNA, but not its resealing after the strand has untwisted. They damage DNA during replication; act in the S phase and arrest cell cycle at G2 phase. lrinotecan It is a prodrug; is decarboxylated in liver to the active metabolite. Cholinergic effects are produced in some patients because it inhibits AChE. These effects can be suppressed by prior atropinization. Irinotecan is indicated in metastatic/ advanced colorectal carcinoma, cancer lung/ cervix/ ovary, etc. Dose limiting toxicity is diarrhoea; neutropenia, thrombocytopenia, haemorrhage, bodyache and weakness are the other adverse effects. ESSENTIALS OF MEDICAL PHARMACOLOGY K.D.TRIPATHI SIXTH EDITION PAGE NO:825,826
Doxorubicin
Irinotecan
Etoposide
Vincristine
Chemotherapy