ミトタン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H351：発がんのおそれの疑い

• 注意書き

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

ミトタン 価格

MSDS Information

• 2,2-(2-Chlorophenyl)-2-(4-chlorophenyl)-1,1-dichloroethane

ミトタン 化学特性,用途語,生産方法

• 外観

  白色～ほとんど白色粉末～結晶

• 用途

  医薬(副腎皮質ホルモン合成阻害剤)

• 効能

  抗悪性腫瘍薬, ステロイド合成阻害薬

• 商品名

  オペプリム (ヤクルト本社)

• 説明

  Mitotane is an inhibitor of steroidogenesis that suppresses the growth of adrenocortical cells. It blocks the expression of several genes that encode proteins involved in steroidogenesis and disrupts mitochondrial respiratory chain activity in human adrenocortical cells. Mitotane has anti-neoplastic actions, alone or in combination with other compounds, and suppresses cortisol synthesis, although it also has significant toxicity in the gastrointestinal tract and nervous system. It is effective against adrenocortical carcinoma and Cushing’s Syndrome in clinical trials.

• 化学的特性

  Crystalline Solid

• 使用

  Mitotane is an inhibitor of steroidogenesis that suppresses the growth of adrenocortical cells. It blocks the expression of several genes that encode proteins involved in steroidogenesis and disrupts mitochondrial respiratory chain activity in human adrenocortical cells. Mitotane has anti-neoplastic actions, alone or in combination with other compounds, and suppresses cortisol synthesis, although it also has significant toxicity in the gastrointestinal tract and nervous system. It is effective against adrenocortical carcinoma and Cushing’s Syndrome in clinical trials.

• 適応症

  Mitotane (Lysodren) produces selective atrophy of the zona fasciculata and zona reticularis, which results in a decrease in the secretion of 17-hydroxycorticosteroids. Direct inhibition of cholesterol side-chain cleavage and 11/18-hydroxylase activities has also been demonstrated.

• 一般的な説明

  Colorless powder.

• 空気と水の反応

  Insoluble in water.

• 反応プロフィール

  Mitotan dehydrohalogenates with strong alkalis. Simple aromatic halogenated organic compounds are very unreactive; halogenated aliphatic compounds are moderately or very reactive. For both subgroups, reactivity generally decreases with increased degree of substitution of halogen for hydrogen atoms. Materials in this group are incompatible with strong oxidizing and reducing agents. Also, they are incompatible with many amines, nitrides, azo/diazo compounds, alkali metals, and epoxides.

• 火災危険

  Flash point data for Mitotan are not available. Mitotan is probably combustible.

• 薬理学

  Mitotane, a derivative of the insecticide DDT, quickly lowers the level of corticosteroids, and is metabolized in the blood and urine and used on non-operable metastatic prostate carcinomas. Synonyms of this drug are lysodren and others.

• 臨床応用

  Mitotane is the drug of choice for the treatment of primary adrenal carcinoma when surgery or radiation therapy is not feasible. Its effectiveness in curtailing adrenal activity is due to an action on adrenocortical mitochondria to impair cytochrome P450 steps in steroid biosynthesis. Mitotane requires metabolic transformation to exert its therapeutic action, and the differential ability of tumors to metabolize the drug may determine its clinical effectiveness. It is advised to measure serum mitotane levels and urinary free cortisol excretion to ensure adequate therapeutic concentrations. Mitotane increases circulating cholesterol by inhibiting cytochrome P450–mediated reactions and therefore contributes to the cardiovascular events that are a significant cause of mortality in untreated Cushing’s syndrome.
  Mitotane, being closely related to the organochlorine insecticides, shares its inductive effects on the liver microsomal drug-metabolizing enzyme system, and its use may therefore alter the requirement for concomitantly administered drugs that are also metabolized by this pathway.

• 副作用

  Mitotane is capable of inducing remission of Cushing’s disease, but only after several weeks of therapy and at the price of severe gastrointestinal distress. Moreover, more than half of patients relapse following cessation of therapy. Other side effects include lethargy, mental confusion, skin rashes, and altered hepatic function. Being a lipid-soluble substance, mitotane remains stored in body tissues for extended periods. This may account for the marked patient-to-patient variability in its therapeutic and/or toxic effects.

• 純化方法

  Purify Mitotane by recrystallisation from pentane, MeOH or EtOH. It is soluble in isooctane and CCl4. [Haller et al. J Am Chem Soc 67 1600 1945, Beilstein 5 IV 1883.]

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