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Lucanthone


ACCESSION NB: DB04967


TYPE: small molecule


GROUP: approved


DESCRIPTION:
One of the schistosomicides, it has been replaced largely by hycanthone and more recently praziquantel. (From Martindale The Extrapharmacopoeia, 30th ed., p46). It is currently being tested as a radiation sensitizer.

VOLUME OF DISTRIBUTION: Not Available

CATEGORIES:
Radiation-Sensitizing Agents Anticancer Agents Schistosomicides

ABSORPTION: Orally available

INDICATION:
Intended for use as a radiation sensitizer in the treatment of brain cancer.

PHARMACODYNAMICS:
Although lucanthone has structural and biochemical similarities to Actinomycin D, it has no hematological or gastro-intestinal toxicity at clinically tolerated doses. In trials, Lucanthone was found to be safe, practical and effective and was proposed for use in clinical protocols for the treatment of cancer. The specificity of lucanthone in combination with radiation for the treatment of brain tumors arises from the fact that lucanthone acts preferentially on cycling cells (most of the normal brain cells are non-cycling) and the fact that lucanthone crosses the blood brain barrier efficiently.

MECHANISM OF ACTION:
Recent data suggests that lucanthone inhibits post-radiation DNA repair in tumor cells. The ability of lucanthone to inhibit AP endonuclease and topoisomerase II probably account for the specific DNA repair inhibition in irradiated cells.

PROTEIN BINDING:
Not Available

TOXICITY:
Not Available

AFECTED ORGANISMS:
Humans and other mammals