药品详细
Aminolevulinic acid(氨基乙酰丙酸)
化学结构式图
中文名
氨基乙酰丙酸
英文名
Aminolevulinic acid
分子式
C5H9NO3
化学名
5-amino-4-oxopentanoic acid
分子量
Average: 131.1299
Monoisotopic: 131.058243159
Monoisotopic: 131.058243159
CAS号
106-60-5
ATC分类
L01X 其它抗肿瘤药
药物类型
small molecule
阶段
approved
商品名
Aladerm;Kerastick;Levulan;Levulan Kerastick;
同义名
ALA;Aminolevulinate;delta-Aminolevulinic acid;
基本介绍
A compound produced from succinyl-CoA and glycine as an intermediate in heme synthesis. It is used as a photochemotherapy for actinic keratosis. [PubChem]
生产厂家
- Dusa pharmaceuticals inc
封装厂家
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 | Aminolevulinic acid plus blue light illumination using a blue light photodynamic therapy illuminator is indicated for the treatment of minimally to moderately thick actinic keratoses of the face or scalp. |
| Pharmacodynamics | The metabolism of aminolevulinic acid (ALA) is the first step in the biochemical pathway resulting in heme synthesis. Aminolevulinic acid is not a photosensitizer, but rather a metabolic precursor of protoporphyrin IX (PpIX), which is a photosensitizer. The synthesis of ALA is normally tightly controlled by feedback inhibition of the enzyme, ALA synthetase, presumably by intracellular heme levels. ALA, when provided to the cell, bypasses this control point and results in the accumulation of PpIX, which is converted into heme by ferrochelatase through the addition of iron to the PpIX nucleus. |
| Mechanism of action | According to the presumed mechanism of action, photosensitization following application of aminolevulinic acid (ALA) topical solution occurs through the metabolic conversion of ALA to protoporphyrin IX (PpIX), which accumulates in the skin to which aminolevulinic acid has been applied. When exposed to light of appropriate wavelength and energy, the accumulated PpIX produces a photodynamic reaction, a cytotoxic process dependent upon the simultaneous presence of light and oxygen. The absorption of light results in an excited state of the porphyrin molecule, and subsequent spin transfer from PpIX to molecular oxygen generates singlet oxygen, which can further react to form superoxide and hydroxyl radicals. Photosensitization of actinic (solar) keratosis lesions using aminolevulinic acid, plus illumination with the BLU-UTM Blue Light Photodynamic Therapy Illuminator (BLU-U), is the basis for aminolevulinic acid photodynamic therapy (PDT). |
| Absorption | Oral bioavailability is 50-60%. |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism |
Following topical administration, synthesis into protoporphyrin IX takes place in situ in the skin.
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| Route of elimination | Not Available |
| Half life | Mean half-life is 0.70 ± 0.18 h after the oral dose and 0.83 ± 0.05 h after the intravenous dose. |
| Clearance | Not Available |
| Toxicity | Solution overdose have not been reported. |
| 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
食物相互作用
Not Available
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