Dexrazoxane - CAS 24584-09-6
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Not Intended for Therapeutic Use. For research use only.
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Dexrazoxane is a cardioprotective compound against anthracyclines. It is highly protective in reducing anthracycline-induced cardiotoxicity and extravasation injury. It functions by inhibiting topoisomerase II without inducing DNA strand breaks. Dexrazoxane is a + enantiomer of razoxane.
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Cardioxane; ICRF187; NSC169780; Zinecard; Totect; Savene
1.The doxorubicin-cardioprotective drug dexrazoxane undergoes metabolism in the rat to its metal ion-chelating form ADR-925
Patricia E. Schroeder, Brian B. Hasinoff. Cancer Chemother Pharmacol (2002) 50: 509–513
The rats (male Sprague-Dawley, 300–350 g) were allowed food and water ad libitum before the study. The rats were anesthetized i.p. with a combination of ketamine (90 mg/ml) and xylazine (10 mg/kg) and the left jugular vein was cannulated. The dexrazoxane hydrochloride solution (freshly prepared, 10 mg/ml in sterile saline) was administered at a dose of 40 mg/kg as an i.v. infusion (1 ml/min) into the tail vein. Blood samples (0.5 ml) were removed from the left jugular vein from a group of six rats before dexrazoxane infusion and at 5, 30, 60, 120, and 180 min after dexrazoxane infusion, and at 60, 80, 100, 120, and 140 min after dexrazoxane infusion from a second group of six rats. The blood removed was replaced with an equal volume of sterile saline. The animal protocol was approved by the University of Manitoba Animal Care Committee. The blood samples were added to heparin (10 ll of 1000 U/ml) and centrifuged for 5 min at 500 g. The plasma was removed, 20 llof5 M HCl per ml of plasma was added, and the samples were stored at –80 ℃ to prevent further hydrolysis. To precipitate plasma proteins, acetonitrile (Fisher) was added in a 2:1 ratio (v/v). The sample was mixed, allowed to settle for 5 min and centrifuged at 8000 g for 10 min. The supernatant was removed, acidified to pH 3 with HCl and evaporated to dryness under N2. The samples for the ADR-925 analysis were reconstituted in water to their original volume just before analysis. Samples for dexrazoxane, B and C analysis were reconstituted in 10 mM HCl/500 lM Na2EDTA to their original volume just prior to analysis. The dexrazoxane hydrochloride that was injected was found to contain less than 0.05% B, 0.02% C, and 0.001% ADR-925 (mol%). Because only very small quantities (nanomoles) of B and C were isolatable after the HPLC separation, pharmacokinetic or plasma studies could not be carried out on these intermediates.
2.Metabolism of dexrazoxane (ICRF-187) used as a rescue agent in cancer patients treated with high-dose etoposide
Patricia E. Schroeder, Peter Buhl Jensen. Cancer Chemother Pharmacol (2003) 52: 167–174
Our previous spectrophotometric and HPLC studies have shown that under physiological conditions dexrazoxane is only slowly hydrolyzed to B and C (t1/2 9.3 h at 37℃ and pH 7.4) and the final hydrolysis product ADR-925 (t1/2 23 h), according to the kinetic scheme shown in Fig. 1. Given the slow rate at which hydrolysis-activation occurs in vitro it is unclear how sufficient amounts of ADR-925 could be present in heart tissue to chelate iron and prevent oxygen radical damage before dexrazoxane is eliminated (t1/2 b 4.2±2.9 h in humans). Our previous in vitro tissue homogenate, isolated hepatocyte, and purified enzyme studies and our in vivo rat studies have shown that dexrazoxane, but not B or C, are metabolized by DHPase (EC that is present in the liver and kidney, but not in the heart. However, B and C, but not dexrazoxane, are both enzymatically hydrolyzed by purified DHOase (EC which is present in the heart, liver, kidney and blood.
3.Dexrazoxane’s protection of jejunal crypt cells in the jejunum of C3Hf/Kam mice from doxorubicin-induced toxicity
Michael Pearlman, David Jendiroba. Cancer Chemother Pharmacol (2003) 52: 477–481
One drug with potential as a mucositis preventative is dexrazoxane (DEX). In one clinical study, Basser et al. observed that stomatitis and vomiting are less common when DEX is also administered. Elimination half-life, maximum plasma concentration, and volume of distribution were not significantly affected by DEX. Hence pharmacokinetic differences could not explain the observations reported. In a preclinical investigation, Wang et al. found that razoxane (RZ), DEX’s racemate, protects animals receiving ordinarily lethal doses of daunorubicin and that this protection is probably due to RZ’s ability to protect the mucosa of the small bowel. Inhibition of anthracycline-induced nephrotoxicity by RZ has also been reported.
4.Dexrazoxane: how it works in cardiac and tumor cells. Is it a prodrug or is it a drug?
Brian B. Hasinoff, Eugene H. Herman. Cardiovasc Toxicol (2007) 7:140–144
Dexrazoxane is currently licenced in the USA, Canada (ZinecardTM), Europe (CardioxaneTM), and in other countries as a cardioprotective agent to reduce doxorubicin-induced cardiotoxicity. In the USA dexrazoxane is labeled for use with women with metastatic breast cancer who have already received 300 mg/m2 of doxorubicin. Dexrazoxane is also licenced to prevent anthracycline extravasation injury in Europe (SaveneTM) and has orphan drug status for this use in the USA (TotectTM). The bisdioxopiperazine dexrazoxane, has been shown in both extensive animal studies and in clinical trials to be highly effective in adults and children in reducing doxorubicin-induced cardiotoxicity, without affecting the antitumor activity of doxorubicin.
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CAS 24584-09-6 Dexrazoxane

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