Drug intelligence / Profile preview

DaunoXome (NeXstar Pharmaceuticals, b3db14)

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

DaunoXome is a liposomal formulation of the anthracycline chemotherapy agent daunorubicin, specifically developed to treat advanced HIV-associated Kaposi's sarcoma. Developed by NeXstar Pharmaceuticals (later acquired by Gilead Sciences), the drug consists of daunorubicin citrate encapsulated in small unilamellar liposomes composed of distearoylphosphatidylcholine and cholesterol. This delivery system enhances the drug's therapeutic index by allowing preferential accumulation in tumor tissues with increased vascular permeability, such as Kaposi's sarcoma lesions, while simultaneously reducing the risk of cardiotoxicity associated with conventional daunorubicin. Its primary mechanism of action involves the intercalation of daunorubicin into DNA and the inhibition of topoisomerase II, which prevents DNA replication and transcription, ultimately leading to apoptosis in rapidly dividing malignant cells. It was approved by the FDA as a first-line cytotoxic therapy for advanced HIV-related Kaposi's sarcoma.

Brand names
DaunoXome
Other names
liposomal daunorubicindaunorubicin citrate liposome injectionliposomal daunorubicin citrate
02

Targets

DNATOP2A (DNA topoisomerase II)ND1 (Mitochondrial electron transport chain complex I)POR (NADPH-cytochrome P450 oxidoreductase)XO (Xanthine Oxidoreductase)

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