Dexrazoxane: how it works in cardiac and tumor cells. Is it a prodrug or is it a drug?
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Hasinoff BB, Herman EH
Dexrazoxane: how it works in cardiac and tumor cells. Is it a prodrug or is it a drug?
Cardiovasc Toxicol. 2007;7(2):140-4.
- PubMed ID
- 17652819 [ View in PubMed]
- Abstract
Dexrazoxane is highly effective in reducing anthracycline-induced cardiotoxicity and extravasation injury and is used clinically for these indications. Dexrazoxane has two biological activities: it is a prodrug that is hydrolyzed to an iron chelating EDTA-type structure and it is also a strong inhibitor of topoisomerase II. Doxorubicin is able to be reductively activated to produce damaging reactive oxygen species. Iron-dependent cellular damage is thought to be responsible for its cardiotoxicity. The available experimental evidence supports the conclusion that dexrazoxane reduces doxorubicin cardiotoxicity by binding free iron and preventing site-specific oxidative stress on cardiac tissue. However, it cannot be ruled out that dexrazoxane may also be protective through its ability to inhibit topoisomerase II.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Dexrazoxane DNA topoisomerase 2-alpha Protein Humans YesInhibitorDetails