药品详细
Valrubicin(戊柔比星)
化学结构式图
中文名
戊柔比星
英文名
Valrubicin
分子式
C34H36F3NO13
化学名
2-oxo-2-[(2S,4S)-2,5,12-trihydroxy-4-{[5-hydroxy-6-methyl-4-(trifluoroacetamido)oxan-2-yl]oxy}-7-methoxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-2-yl]ethyl pentanoate
分子量
Average: 723.6437
Monoisotopic: 723.213874858
Monoisotopic: 723.213874858
CAS号
56124-62-0
ATC分类
L01D 细胞毒素抗生素及相关物质
药物类型
small molecule
阶段
approved
商品名
Valstar;Valstar Preservative Free;
同义名
Antibiotic Ad 32;
基本介绍
Valrubicin (N-trifluoroacetyladriamycin-14-valerate, Valstar®) is a chemotherapy drug used to treat bladder cancer. Valrubicin is a semisynthetic analog of the anthracycline doxorubicin, and is administered by infusion directly into the bladder. [Wikipedia]
生产厂家
- Endo pharmaceutical solutions inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
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 the treatment of cancer of the bladder. | ||||||||||||
| Pharmacodynamics | Valrubicin is a semisynthetic analog of the anthracycline doxorubicin, and is administered by infusion directly into the bladder. | ||||||||||||
| Mechanism of action | Valrubicin is an anthracycline that affects a variety of inter-related biological functions, most of which involve nucleic acid metabolism. It readily penetrates into cells, where after DNA intercalation, it inhibits the incorporation of nucleosides into nucleic acids, causes extensive chromosomal damage, and arrests cell cycle in G2. Although valrubicin does not bind strongly to DNA, a principal mechanism of its action, mediated by valrubicin metabolites, is interference with the normal DNA breaking-resealing action of DNA topoisomerase II. | ||||||||||||
| Absorption | Not Available | ||||||||||||
| Volume of distribution | Not Available | ||||||||||||
| Protein binding | >99% | ||||||||||||
| Metabolism |
Valrubicin is metabolized to two primary metabolites: N-trifluoroacetyladriamycin and N-trifluoroacetyladriamycinol.
Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.
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| Route of elimination | Not Available | ||||||||||||
| Half life | Not Available | ||||||||||||
| Clearance | Not Available | ||||||||||||
| Toxicity | The primary anticipated complications of overdosage associated with intravesical administration would be consistent with irritable bladder symptoms. Myelosuppression is possible if valrubicin is inadvertently administered systemically or if significant systemic exposure occurs following intravesical administration (e.g., in patients with bladder/rupture perforation). The maximum tolerated dose in humans by either intraperitoneal or intravenous administration is 600 mg/m2. | ||||||||||||
| Affected organisms |
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| Pathways | Not Available | ||||||||||||
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||||||||
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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 |
|---|---|
| Docetaxel | The taxane derivative, Docetaxel, may increase Valrubicin toxicity. Consider alternate therapy or monitor for toxic effects. |
| Natalizumab | Valrubicin may increase Natalizumab toxicity. Concurrent therapy should be avoided. |
| Paclitaxel | The taxane derivative, Paclitaxel, may increase Valrubicin toxicity. Consider alternate therapy or monitor for toxic effects. |
| Trastuzumab | Trastuzumab may increase the cardiotoxicity of Valrubicin. Signs and symptoms of cardiac dysfunction should be monitored for frequently. Increased risk of heart failure. 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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