药品详细
Altretamine(六甲蜜胺)
化学结构式图
中文名
六甲蜜胺
英文名
Altretamine
分子式
C9H18N6
化学名
2-N,2-N,4-N,4-N,6-N,6-N-hexamethyl-1,3,5-triazine-2,4,6-triamine
分子量
Average: 210.2794
Monoisotopic: 210.159294606
Monoisotopic: 210.159294606
CAS号
645-05-6
ATC分类
L01X 其它抗肿瘤药
药物类型
small molecule
阶段
approved
商品名
Hemel;Hexalen;Hexastat;
同义名
Altretaminum [INN-Latin];HEXAMETHYLMELAMINE;HMM;HTM;HXM;
基本介绍
An alkylating agent proposed as an antineoplastic. It also acts as a chemosterilant for male houseflies and other insects. [PubChem]
生产厂家
- Eisai inc
封装厂家
- AAIPharma Inc.
- Eisai Inc.
- Excella GmbH
- MGI Pharma
参考
| Synthesis Reference | Not Available |
| General Reference |
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剂型
规格
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 use as a single agent in the palliative treatment of patients with persistent or recurrent ovarian cancer following first-line therapy with a cisplatin and/or alkylating agent-based combination. |
| Pharmacodynamics | Altretamine is a novel antineoplastic agent. The precise mechanism by which altretamine exerts its cytotoxic effect is unknown, although a number of theoretical possibilities have been studied. Structurally, altretamine resembles the alkylating agent triethylenemelamine, yet in vitro tests for alkylating activity of altretamine and its metabolitics have been negative. Altretamine has been demonstrated to be efficacious for certain ovarian tumors resistant to classical alkylating agents. Metabolism of altretamine is a requirement of cytotoxicity. Synthetic monohydroxymethylmelamines, and products of altretamine metabolism, in vitro and in vivo, can form covalent adducts with tissue macromolecules including DNA, but the relevance of these reactions to antitumor activity is unknown. |
| Mechanism of action | The precise mechanism by which altretamine exerts its cytotoxic effect is unknown although it is classified as an alkylating anti-neoplastic agent. Through this mechanism, the drug is metabolized into alkylating agents by N-demethylation. These alkylating species consequently damage tumor cells. |
| Absorption | Not Available |
| Volume of distribution | Not Available |
| Protein binding | 94% |
| Metabolism |
Not Available
|
| Route of elimination | Human urinary metabolites were Ndemethylated homologues of altretamine with <1% unmetabolized altretamine excreted at 24 hours. |
| Half life | 4.7-10.2 hours |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Amitriptyline | Risk of severe hypotension |
| Amoxapine | Risk of severe hypotension |
| Clomipramine | Risk of severe hypotension |
| Desipramine | Risk of severe hypotension |
| Doxepin | Risk of severe hypotension |
| Imipramine | Risk of severe hypotension |
| Isocarboxazid | Risk of severe hypotension |
| Nortriptyline | Risk of hypotension |
| Phenelzine | Risk of severe hypotension |
| Rasagiline | Risk of severe hypotension |
| 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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