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What Is Irinotecan's Mechanism of Action?

Available by prescription only, irinotecan (Camptosar®) is a medication that belongs to a group of drugs called topoisomerase I inhibitors. It is used in the treatment of colon or rectal cancer that has spread to other areas of the body.
What is the drug's mechanism of action? Irinotecan works by blocking topoisomerase I, an enzyme that helps relax DNA that has been overwound (such as when DNA is duplicating so it can divide). This enzyme normally helps break the DNA strand to relieve the strain, and then helps put the strand back together. Irinotecan binds to topoisomerase I, preventing the enzyme from repairing the broken DNA strand -- as a result, the cell is unable to divide and the cell dies.
(To learn more, click Irinotecan. This article offers a closer look at how this medicine works, possible side effects, and what to discuss with your healthcare provider before starting treatment.)
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