dexrazoxane

Dexrazoxane is a cardioprotective agent and iron chelator used in oncology to mitigate damage from anthracycline chemotherapy, most notably doxorubicin. It is a prodrug that is converted to active metabolites which chelate intracellular iron and can inhibit topoisomerase II, particularly the cardiac isoform TOP2B. By reducing iron-catalyzed free radical formation and DNA damage in heart cells, dexrazoxane helps lower the risk of anthracycline-induced cardiomyopathy while aiming to preserve anticancer activity in tumor cells.

Medical uses include prevention of doxorubicin- or daunorubicin-induced cardiomyopathy in patients anticipated to receive high cumulative anthracycline doses. It is marketed under the brand names Zinecard for cardioprotection and Totect for the treatment of anthracycline extravasation injuries, the latter used after an accidental leakage of the drug into surrounding tissue.

Administration and pharmacology: dexrazoxane is given by intravenous infusion, typically in a regimen coordinated with anthracycline administration according to approved guidelines. It is a water-soluble bis(dioxopiperazine) prodrug that is rapidly hydrolyzed to active chelating forms and excreted primarily by the kidneys. Its TOP2B-inhibitory action in cardiac tissue is thought to contribute to tissue protection, while many tumor cells relying on TOP2A may retain sensitivity to anthracyclines.

Adverse effects and safety: possible infusion-related reactions, nausea, mucositis, and hematologic suppression (neutropenia, thrombocytopenia) can occur. Hypersensitivity is possible. Dexrazoxane should be used with caution in patients with renal impairment and are contraindicated in those with hypersensitivity to the drug.