Drug intelligence / Profile preview

methyl aminolevulinate

Development stage
Phase 4
Lead developer
Galderma
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Topical
01

Overview

Methyl aminolevulinate is a small molecule prodrug and porphyrin precursor used topically in photodynamic therapy (PDT) for the treatment of non-hyperkeratotic, non-pigmented actinic keratosis of the face and scalp, as well as superficial basal cell carcinoma in some regions[1][2][4][5]. After topical application, it is metabolized to protoporphyrin IX (PpIX), a photoactive compound that accumulates in treated skin lesions. Upon exposure to red light or daylight, PpIX generates singlet oxygen and other reactive oxygen species that induce local cytotoxicity by damaging cellular compartments—particularly mitochondria—leading to destruction of diseased cells[2][4][6]. Methyl aminolevulinate is functionally related to 5‑aminolevulinic acid and acts as an antineoplastic agent, photosensitizer, prodrug, and dermatologic drug. It is primarily indicated for actinic keratosis but may also be used for superficial basal cell carcinoma when other therapies are less appropriate[1][4][5].

Brand names
MetvixMetvixia
Other names
methyl aminolevulinatemethyl 5-aminolevulinatemethyl5-aminolevulinatemethyl-5-aminolevulinateaminolevulinic acid methyl estermethyl 5-amino-4-oxopentanoatemethyl5-amino-4-oxopentanoatemethyl-5-amino-4-oxopentanoate
02

Targets

FECH (Ferrochelatase)

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