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外観
うすい黄赤色～黄色～緑色粉末～結晶
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用途
抗新生物薬、抗悪性腫瘍薬
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用途
ニトロソウレア系化合物です。
DNA 合成阻害作用を示します。
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効能
抗悪性腫瘍薬, アルキル化剤
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化学的特性
Lomustine is a pale yellow powder.
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使用
CCNU is an oral anticancer drug that was approved by the U.S. Food and Drug Administration in 1976 for marketing, as lomustine (FDA 2009a). CCNU is used alone or in combination with other antineoplastic agents, including procarbazine and vincristine, etoposide and prednimustine, and other combinations (IARC 1981, HSDB 2009). It is used primarily in the treatment of Hodgkin’s disease and brain tumors, but it has also been used to treat other cancer, includ-ing lung cancer, non-Hodgkin’s lymphoma, malignant melanoma, breast cancer, kidney cancer, and cancer of the gastrointestinal tract (MedlinePlus 2009). It has also been applied to the skin to treat mycosis fungoides and psoriasis.
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定義
ChEBI: An N-nitrosourea that is urea in which one of the nitrogens is substituted by a 2-chloroethyl group and by a nitroso group, while the other nitrogen is substituted by a cyclohexyl group. An alkylating antineoplastic agent, it is used in
he treatment of brain tumours, lung cancer, malignant melanoma and other solid tumours.
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一般的な説明
Lomustine is available in 10-, 40-, and 100-mg capsules fororal administration in the treatment of primary and metastaticbrain cancers and Hodgkin’s lymphoma. This lipophilicagent is well absorbed, widely distributed, and crosses theblood-brain barrier. Lomustine undergoes extensive hepaticmetabolism, which is mediated by CYP3A4 to give severalhydroxylated metabolites, which arise as a result of oxidationof the cyclohexyl ring. Several of these are more activethan the parent compound. Denitrosation and dechlorinationhave also been demonstrated to occur for lomustine as well.The intact drug was not found in plasma when the agent wasadministered orally. Elimination occurs primarily in theurine with an elimination half-life of 16 to 72 hours.Myelosuppression is dose limiting and presents in a mannersimilar to that seen with carmustine. Other toxicities includenausea, vomiting, anorexia, impotence, sterility, amenorrhea,and infertility. Pulmonary and renal toxicity are rarelyseen during standard-dose therapy but increase during highdosetherapy.
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作用機序
Like other nitrosoureas, lomustine acts as a DNA-alkylating agent, and it also inhibits various key enzymatic reactions by carbamoylating proteins.
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安全性プロファイル
Confirmed carcinogen
with experimental carcinogenic and
tumorigenic data. Poison by ingestion,
intraperitoneal, subcutaneous, intravenous,
and possibly other routes. Human systemic
effects by ingestion: anorexia, nausea or
vomiting, leukopenia (decrease in the white
blood cell count), and thrombocytopenia
(decrease in the number of blood platelets).
Experimental teratogenic and reproductive
effects. Human mutation data reported.
When heated to decomposition it emits very
toxic fumes of Cland NOx. See also NNITROSO COMPOUNDS.
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職業ばく露
A potential danger to those involved
in the manufacture, administration or consumption of this
antineoplastic (anti-cancer) agent
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発がん性
1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU) is reasonably
anticipated to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in experimental animals.
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輸送方法
UN2811 Toxic solids, organic, n.o.s., Hazard
Class: 6.1; Labels: 6.1-Poisonous materials, Technical
Name Required. UN3249 Medicine, solid, toxic, n.o.s.,
Hazard Class: 6.1; Labels: 6.1-Poisonous materials
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廃棄物の処理
It is inappropriate and possibly
dangerous to the environment to dispose of expired or waste
drugs and pharmaceuticals by flushing them down the toilet
or discarding them to the trash. Household quantities of
expired or waste pharmaceuticals may be mixed with wet
cat litter or coffee grounds, double-bagged in plastic, discard
in trash. Larger quantities shall carefully take into consideration applicable DEA, EPA, and FDA regulations. If possible return the pharmaceutical to the manufacturer for proper
disposal being careful to properly label and securely package
the material. Alternatively, the waste pharmaceutical shall be
labeled, securely packaged and transported by a state
licensed medical waste contractor to dispose by burial in a
licensed hazardous or toxic waste landfill or incinerator.
