药品详细
Everolimus (依维莫 )
化学结构式图
中文名
依维莫
英文名
Everolimus
分子式
Not Available
化学名
(1S,9R,15R,16E,18R,19R,21S,23R,24E,26E,28E,30S,32R,35S)-1,18-dihydroxy-12-[(2S)-1-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0^{4,9}]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
分子量
Average: 958.2244
Monoisotopic: 957.581356369
Monoisotopic: 957.581356369
CAS号
159351-69-6
ATC分类
L04A 未知
药物类型
small molecule
阶段
商品名
Certican;
同义名
everolimus;
基本介绍
Everolimus is a derivative of Rapamycin (sirolimus), and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor. It is currently used as an immunosuppressant to prevent rejection of organ transplants. In a similar fashion to other mTOR inhibitors Everolimus’ effect is solely on the mTORC1 protein and not on the mTORC2 protein.
生产厂家
- Novartis pharmaceuticals corp
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
|
剂型
规格
| Unit description | Cost | Unit |
|---|---|---|
| Afinitor 10 mg tablet | 247.58 USD | tablet |
| Afinitor 5 mg tablet | 234.75 USD | tablet |
| Vesicare 10 mg tablet | 6.98 USD | tablet |
| Vesicare 5 mg tablet | 6.98 USD | tablet |
化合物类型
| Type | small molecule |
| Classes | Not Available |
| Substructures | Not Available |
适应症
IMMUNOSUPPRESSIVE 免疫抑制;
药理
| Indication | Investigated for use/treatment in transplant (rejection) and renal cell carcinoma. |
| Pharmacodynamics | Not Available |
| Mechanism of action | Everolimus is a mTOR inhibitor that binds with high affinity to the FK506 binding protein-12 (FKBP-12), thereby forming a drug complex that inhibits the activation of mTOR. This inhibition reduces the activity of effectors downstream, which leads to a blockage in the progression of cells from G1 into S phase, and subsequently inducing cell growth arrest and apoptosis. Everolimus also inhibits the expression of hypoxia-inducible factor, leading to a decrease in the expression of vascular endothelial growth factor. The result of everolimus inhibition of mTOR is a reduction in cell proliferation, angiogenesis, and glucose uptake. |
| Absorption | Not Available |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism | |
| Route of elimination | After a single dose of radiolabeled everolimus was given to transplant patients receiving cyclosporine, the majority (80%) of radioactivity was recovered from the feces and only a minor amount (5%) was excreted in urine. |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms | Not Available |
| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties | Not Available | ||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Clarithromycin | The macrolide, clarithromycin, may increase the serum concentration and toxicity of everolimus. |
| Erythromycin | The macrolide, erythromycin, may increase the serum concentration and toxicity of everolimus. |
| Fluconazole | Fluconazole may increase everolimus levels/toxicity. |
| Itraconazole | Itraconazole may increase everolimus levels/toxicity. |
| Ketoconazole | Ketoconazole may increase everolimus levels/toxicity. |
| Verapamil | Concomitant administration may increase the serum concentrations of both agents. Concurrent use should be avoided. |
| Voriconazole | Voriconzole, a strong CYP3A4 inhibitor, may increase the serum concentration of everolimus by decreasing its metabolism. Concurrent therapy should be avoided. |
食物相互作用
Not Available
收藏