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Mitoxantrone


ACCESSION NB: DB01204 (APRD00371)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
An anthracenedione-derived antineoplastic agent. [PubChem]

VOLUME OF DISTRIBUTION: 1000 L/m2

CATEGORIES:
Antineoplastic Agents Analgesics

ABSORPTION: Poorly absorbed following oral administration

INDICATION:
For the treatment of secondary (chronic) progressive, progressive relapsing, or worsening relapsing-remitting multiple sclerosis

PHARMACODYNAMICS:
Mitoxantrone has been shown in vitro to inhibit B cell, T cell, and macrophage proliferation and impair antigen presentation, as well as the secretion of interferon gamma, TNFa, and IL-2.

MECHANISM OF ACTION:
Mitoxantrone, a DNA-reactive agent that intercalates into deoxyribonucleic acid (DNA) through hydrogen bonding, causes crosslinks and strand breaks. Mitoxantrone also interferes with ribonucleic acid (RNA) and is a potent inhibitor of topoisomerase II, an enzyme responsible for uncoiling and repairing damaged DNA. It has a cytocidal effect on both proliferating and nonproliferating cultured human cells, suggesting lack of cell cycle phase specificity.

PROTEIN BINDING:
78%

METABOLISM:
Hepatic

TOXICITY:
Severe leukopenia with infection.

AFECTED ORGANISMS:
Humans and other mammals