Drug Information for Totect Kit (dexrazoxane) for injection, for intravenous infusion onlyInitial U.S. Approval: 2007 (TopoTarget USA): 11 DESCRIPTION

Totect^® (dexrazoxane for injection) is a sterile, pyrogen-free lyophilizate intended for intravenous (IV) administration. Totect^® is packaged as a kit for single patient use. Each kit contains 10 vials of Totect^® (dexrazoxane for injection) 500 mg and 10 vials of 50 mL diluent, which provides a complete three day treatment

Chemically, dexrazoxane is 2,6-piperazinedione,4,4'-(1-methyl-1,2-ethanediyl) bis-,(S)- or (S)-(+)-1,2-bis(3,5-dioxopiperazin-1-yl) propane. The following diagram shows the chemical structure:

The molecular formula is C₁₁H₁₆N₄O₄; the molecular weight is 268.3. Dexrazoxane is a white to off-white powder, with a melting point of 194 ± 3 °C. It is soluble in dioxane and 0.1 N HCl, sparingly soluble in water, tetrahydrofuran, citrate buffer at pH 4.0, phosphate buffer at pH 7.0, and borate-potassium chloride sodium hydroxide buffer at pH 9.0. The acid dissociation constants, pKa, are 2.5 (for the tertiary piperazine nitrogen) and 9.7 (for the nitrogen imide). Log P is -2.135.

The finished product is supplied in a sterile form for intravenous infusion only following mixing and diluting.

Each kit contains twenty 50 mL Type I glass vials. Ten vials each contains dexrazoxane hydrochloride equivalent to 500 mg dexrazoxane and 10 vials each contains diluent (0.167M Sodium Lactate Injection, USP). Each vial of dexrazoxane for injection is closed with an aluminum flip-off cap covered with a dark red overcap. Each vial of diluent is closed with an aluminum flip-off cap covered with a white overcap.

When reconstituted as directed, the admixture contains dexrazoxane and the following excipients: hydrochloric acid, sodium lactate, water for injection, sodium hydroxide and lactic acid [see Dosage and Administration (2.4)]. The admixture should be further diluted in 0.9 % NaCl prior to administration to patients.