物质信息
ID:4538
名称和标识
IUPAC传统名
lucanthone
商标名
NilodinMiracil DTixantoneScapurenMiracol
别名
Lucanthonum [inn-latin]Lucanthone hydrochloridelucanthone1-((2-(Diethylamino)ethyl)amino)-4-methylthioxanthen-9-oneLucanthoneLucantona [inn-spanish]Lucanthone monohydrochlorideLucanthon1-[[2-(Diethylamino)ethyl]amino]-4-methylthioxanthone
IUPAC标准名
1-{[2-(diethylamino)ethyl]amino}-4-methyl-9H-thioxanthen-9-one
化合物性质
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描述信息
Drug Groups
approved; investigational
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.
Indication
Intended for use as a radiation sensitizer in the treatment of brain cancer.
Pharmacology
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.
Affected Organisms
Humans and other mammals
Absorption
Orally available
References
•
Luo M, Kelley MR: Inhibition of the human apurinic/apyrimidinic endonuclease (APE1) repair activity and sensitization of breast cancer cells to DNA alkylating agents with lucanthone. Anticancer Res. 2004 Jul-Aug;24(4):2127-34.
[Pubmed]
•
Del Rowe JD, Bello J, Mitnick R, Sood B, Filippi C, Moran J, Freeman K, Mendez F, Bases R: Accelerated regression of brain metastases in patients receiving whole brain radiation and the topoisomerase II inhibitor, lucanthone. Int J Radiat Oncol Biol Phys. 1999 Jan 1;43(1):89-93.
[Pubmed]
External Links
分子图谱
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参考文献
• Luo M, Kelley MR: Inhibition of the human apurinic/apyrimidinic endonuclease (APE1) repair activity and sensitization of breast cancer cells to DNA alkylating agents with lucanthone. Anticancer Res. 2004 Jul-Aug;24(4):2127-34. Pubmed
• Del Rowe JD, Bello J, Mitnick R, Sood B, Filippi C, Moran J, Freeman K, Mendez F, Bases R: Accelerated regression of brain metastases in patients receiving whole brain radiation and the topoisomerase II inhibitor, lucanthone. Int J Radiat Oncol Biol Phys. 1999 Jan 1;43(1):89-93. Pubmed