♦Doxorubicin Hydrochloride Liposome
(dox-oh-roo’-bih-sin)
Doxil
Pregnancy Category D
Mechanism of Action
The active ingredient is doxorubicin hydrochloride, which exerts its cytotoxic effect by binding DNA and inhibiting nucleic acid synthesis. Doxorubicin hydrochloride is encapsulated in liposomal vesicles consisting of one or more concentric lipid bilayers surrounding aqueous compartments. This form allows slow release of the drug, decreases rapid exposure to sensitive organ systems, and provides specific target delivery. It is hypothesized that because of their small size and persistence in the circulation, the pegylated liposomes can penetrate tumor vasculature.
Indications
♦ AIDS-related Kaposi’s sarcoma in patients with disease that has progressed with prior combination chemotherapy or in patients who are intolerant to such therapy
♦ Metastatic carcinoma of the ovary refractory to both paclitaxel and platinum-based regimens.
Metabolism/Excretion
The major metabolite of doxorubicin, doxorubicinol, was detected at very low levels in the plasma of patients who were given a 10- or 20-mg/m2 dose. Terminal half-life: 55 hours.