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Pegylated doxorubicin hydrochloride (also known as pegylated liposomal doxorubicin) is a liposomal formulation of the anthracycline antineoplastic antibiotic doxorubicin hydrochloride. Originally developed by Liposome Technology (later Sequus Pharmaceuticals, Alza, and Johnson & Johnson), the drug consists of doxorubicin HCl encapsulated in pegylated liposomes coated with methoxypolyethylene glycol (MPEG). This pegylation shields the liposomes from detection by the mononuclear phagocyte system, significantly extending blood circulation time and enhancing drug accumulation in tumor tissues via the enhanced permeability and retention (EPR) effect, while reducing cardiotoxicity compared to conventional doxorubicin. Doxorubicin exerts its cytotoxic effects by intercalating into DNA and inhibiting topoisomerase II, thereby blocking DNA replication and RNA synthesis. It is widely approved for the treatment of various malignancies, including metastatic breast cancer, advanced ovarian cancer, multiple myeloma (in combination with bortezomib), and AIDS-related Kaposi's sarcoma.
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