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

Dexrazoxane

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Dexrazoxane	DNA topoisomerase 2-alpha	Protein	Humans	Yes	Inhibitor	Details