Razoxane
Razoxane - General Information
An antimitotic agent with immunosuppressive properties. Razoxane, the (+)-enantiomorph of razoxane, provides cardioprotection against anthracycline toxicity. It appears to inhibit formation of a toxic iron-anthracycline complex. [PubChem]
Pharmacology of Razoxane
Razoxane is a cardioprotective agent for use in conjunction with doxorubicin indicated for reducing the incidence and severity of cardiomyopathy associated with doxorubicin administration in women with metastatic breast cancer who have received a cumulative doxorubicin dose.
Razoxane for patients
Razoxane Interactions
ZINECARD does not influence the pharmacokinetics of doxorubicin.
Carcinogenesis, Mutagenesis, Impairment of Fertility No long-term carcinogenicity studies have been carried out with dexrazoxane in animals. Dexrazoxane was not mutagenic in the Ames test but was found to be clastogenic to human lymphocytes in vitro and to mouse bone marrow erythrocytes in vivo (micronucleus test).
The possible adverse effects of ZINECARD on the fertility of humans and experimental animals, male or female, have not been adequately studied. Testicular atrophy was seen with dexrazoxane administration at doses as low as 30 mg/kg weekly for 6 weeks in rats (1/3 the human dose on a mg/m 2 basis) and as low as 20 mg/kg weekly for 13 weeks in dogs (approximately equal to the human dose on a mg/m 2 basis).
Razoxane Contraindications
ZINECARD should not be used with chemotherapy regimens that do not contain an anthracycline.
Additional information about Razoxane
Razoxane Indication: For reducing the incidence and severity of cardiomyopathy associated with doxorubicin administration in women with metastatic breast cancer.
Mechanism Of Action: The mechanism by which dexrazoxane exerts its cardioprotective activity is not fully understood. Razoxane is a cyclic derivative of EDTA that readily penetrates cell membranes. Results of laboratory studies suggest that dexrazoxane is converted intracellularly to a ring-opened chelating agent that interferes with iron-mediated free radical generation thought to be responsible, in part, for anthracycline-induced cardiomyopathy.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Dexrazoxane
Synonyms: Dexrazoxano [Inn-Spanish]; Dexrazoxanum [Inn-Latin]; Dextrorazoxane; Desrazoxane; Razoxana [Inn-Spanish]; Razoxanum [Inn-Latin]
Drug Category: Immunosuppressive Agents; Chelating Agents; Cardiovascular Agents; Antineoplastic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Dexrazoxane: Cardioxane; Dyzoxane; Eucardion; Razoxane; Razoxin; Tepirone; Troxozone; Zinecard;
Absorption: IV administration results in complete bioavailability.
Toxicity (Overdose): Intraperitoneal, mouse LD10 = 500 mg/kg. Intravenous, dog LD10 = 2 gm/kg.
Protein Binding: Very low (< 2%)
Biotransformation: Dexrazoxane is hydrolysed by the enzyme dihydropyrimidine amidohydrolase in the liver and kidney to active metabolites that are capable of binding to metal ions.
Half Life: 2.5 hours
Dosage Forms of Razoxane: Powder, for solution Intravenous
Chemical IUPAC Name: 4-[(2S)-1-(3,5-dioxopiperazin-1-yl)propan-2-yl]piperazine-2,6-dione
Chemical Formula: C11H16N4O4
Dexrazoxane on Wikipedia: https://en.wikipedia.org/wiki/Dexrazoxane
Organisms Affected: Humans and other mammals
