Methyl 5-aminolevulinate
Methyl 5-aminolevulinate Uses, Dosage, Side Effects, Food Interaction and all others data.
Methyl 5-aminolevulinate is a prodrug that is metabolised to Protoporphyrin IX (a photosensitizer) used in photodynamic therapy.
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.
| Trade Name | Methyl 5-aminolevulinate |
| Generic | Methyl aminolevulinate |
| Methyl aminolevulinate Other Names | Aminolevulinato de metilo, Aminolevulinic acid methyl ester, methyl 5-aminolevulinate, Methyl aminolevulinate, Methyl delta-aminolevulinate |
| Type | |
| Formula | C6H11NO3 |
| Weight | Average: 145.1564 Monoisotopic: 145.073893223 |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Methyl 5-aminolevulinate is a porphyrin precursor used to treat non-hyperkeratotic, non-pigmented actinic keratosis of the face and scalp.
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).
Methyl 5-aminolevulinate is also used to associated treatment for these conditions: Actinic Keratosis (AK)
How Methyl 5-aminolevulinate works
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.
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.
Food Interaction
No interactions found.Elimination Route
In vitro, after 24 hours the mean cumulative absorption through human skin was 0.26% of the administered dose.
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