药品详细
Lomustine (洛莫司汀 )
化学结构式图
中文名
洛莫司汀
英文名
Lomustine
分子式
Not Available
化学名
3-(2-chloroethyl)-1-cyclohexyl-3-nitrosourea
分子量
Average: 233.695
Monoisotopic: 233.093104478
Monoisotopic: 233.093104478
CAS号
13010-47-4
ATC分类
L01A 烷化剂
药物类型
small molecule
阶段
商品名
Belustine;Cecenu;CeeNU;CINU;
同义名
CCNU;Chloroethylcyclohexylnitrosourea;Lomustina [INN-Spanish];Lomustinum [INN-Latin];
基本介绍
An alkylating agent of value against both hematologic malignancies and solid tumors. [PubChem]
生产厂家
- Bristol myers squibb co
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Capsule | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Ceenu 100 mg capsule | 60.61 USD | capsule |
| Ceenu 40 mg capsule | 31.88 USD | capsule |
| CeeNU 300 mg capsule | 31.69 USD | capsule |
| Ceenu dose pack | 30.47 USD | each |
| Ceenu 10 mg capsule | 10.77 USD | capsule |
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
Cancer 癌症;
药理
| Indication | For the treatment of primary and metastatic brain tumors as a component of combination chemotherapy in addition to appropriate surgical and/or radiotherapeutic procedures. Also used in combination with other agents as secondary therapy for the treatment of refractory or relapsed Hodgkin's disease. |
| Pharmacodynamics | Lomustine is an alkylating agent of the nitrosourea type. Lomustine and its metabolites interferes with the function of DNA and RNA. It is cell cycle–phase nonspecific. Cancers form when some cells within the body multiply uncontrollably and abnormally. These cells then spread and destroy nearby tissues. Lomustine acts by slowing this process down. It kills cancer cells by damaging the DNA (the genetic material inside the cells) and stops them from dividing. |
| Mechanism of action | Lomustine is a highly lipophilic nitrosourea compound which undergoes hydrolysis in vivo to form reactive metabolites. These metabolites cause alkylation and cross-linking of DNA (at the O6 position of guanine-containing bases) and RNA, thus inducing cytotoxicity. Other biologic effects include inhibition of DNA synthesis and some cell cycle phase specificity. Nitrosureas generally lack cross-resistance with other alkylating agents. As lomustine is a nitrosurea, it may also inhibit several key processes such as carbamoylation and modification of cellular proteins. |
| Absorption | Well and rapidly absorbed from the gastrointestinal tract. |
| Volume of distribution | Not Available |
| Protein binding | 50% |
| Metabolism |
Hepatic. Rapid and complete, with active metabolites. |
| Route of elimination | Following oral administration of radioactive CeeNU at doses ranging from 30 mg/m2 to 100 mg/m2, about half of the radioactivity given was excreted in the urine in the form of degradation products within 24 hours. |
| Half life | Approximately 94 minutes, however the metabolites have a serum half-life of 16 to 48 hours. |
| Clearance | Not Available |
| Toxicity | Oral, rat: LD50 = 70 mg/kg. Pulmonary toxicity has been reported at cumulative doses usually greater than 1,100 mg/m2. There is one report of pulmonary toxicity at a cumulative dose of only 600 mg. The onset of toxicity has varied from 6 months after initiation of therapy, to as late as 15 years after. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 88-90 oC | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Atomoxetine | The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine |
| Terbinafine | Terbinafine may reduce the metabolism and clearance of Lomustine. Consider alternate therapy or monitor for therapeutic/adverse effects of Lomustine if Terbinafine is initiated, discontinued or dose changed. |
| Trastuzumab | Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. |
食物相互作用
Not Available
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