药品详细
Methyl aminolevulinate (甲基氨基乙酰丙酸 )
化学结构式图
中文名
甲基氨基乙酰丙酸
英文名
Methyl aminolevulinate
分子式
Not Available
化学名
methyl 5-amino-4-oxopentanoate
分子量
Average: 145.1564
Monoisotopic: 145.073893223
Monoisotopic: 145.073893223
CAS号
33320-16-0
ATC分类
L01X 其它抗肿瘤药
药物类型
small molecule
阶段
商品名
Metvix;
同义名
5-Aminolevulinic acid methyl ester;Aminolevulinic acid methyl ester;
基本介绍
Methyl aminolevulinate is a prodrug that is metabolised to Protoporphyrin IX (a photosensitizer) used in photodynamic therapy.
生产厂家
- Galderma laboratories lp
封装厂家
参考
剂型
规格
| Unit description | Cost | Unit |
|---|---|---|
| Metvixia 16.8% cream | 82.2 USD | g |
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 topical use, in combination with 570 to 670 nm wavelength red light illumination, in the treatment of non-hyperkeratotic actinic keratoses of the face and scalp in immunocompetent patients when used in conjunction with lesion preparation (debridement using a sharp dermal curette). |
| Pharmacodynamics | After topical application of methyl aminolevulinate, porphyrins will accumulate intracellularly in the treated skin lesions. The intracellular porphyrins (including PpIX) are photoactive, fluorescing compounds and, upon light activation in the presence of oxygen, singlet oxygen is formed which causes damage to cellular compartments, in particular the mitochondria. Light activation of accumulated porphyrins leads to a photochemical reaction and thereby phototoxicity to the light-exposed target cells. |
| Mechanism of action | Photosensitization following application of methyl aminolevulinate cream occurs through the metabolic conversion of methyl aminolevulinate (prodrug) to photoactive porphyrins (PAP), which accumulates in the skin lesions to which the cream has been applied. When exposed to light of appropriate wavelength and energy, the accumulated photoactive porphyrins produce a photodynamic reaction, resulting in a cytotoxic process dependent upon the simultaneous presence of oxygen. The absorption of light results in an excited state of porphyrin molecules, and subsequent spin transfer from photoactive porphyrins to molecular oxygen generates singlet oxygen, which can further react to form superoxide and hydroxyl radicals. |
| Absorption | In vitro, after 24 hours the mean cumulative absorption through human skin was 0.26% of the administered dose. |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism | |
| Route of elimination | Not Available |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | The severity of local phototoxic reactions such as erythema, pain and burning sensation may increase in case of prolonged application time or very high light intensity. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
食物相互作用
Not Available
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