Methyl Aminolevulinate

Summary

Methyl Aminolevulinate (CHEMBL1096562) is an approved small-molecule antineoplastic agent (ATC L01XD03); indicated across 8 conditions including neoplasm and basal cell carcinoma.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01XD03
• Indications: 8 conditions
• Clinical trials: 12
• Chemistry: 145.16 Da · C6H11NO3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1096562
Name	Methyl Aminolevulinate
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	157922
ChEBI	CHEBI:724125
ATC	L01XD03
Molecular formula	C6H11NO3
Molecular weight	145.16
InChIKey	YUUAYBAIHCDHHD-UHFFFAOYSA-N

SMILES: COC(=O)CCC(=O)CN

IUPAC name: methyl 5-amino-4-oxopentanoate

ChEBI definition: The methyl ester of 5-aminolevulinic acid. A prodrug, it is metabolised to protoporphyrin IX, a photosensitizer, and is used in the photodynamic treatment of non-melanoma skin cancer (including basal cell carcinoma). Topical application (often as the hydrochloride salt) results in an accumulation of protoporphyrin IX in the skin lesions to which the cream has been applied. Subsequent illumination with red light results in the generation of toxic singlet oxygen that destroys cell membranes and thereby kills the tumour cells.

Pharmacological roles (ChEBI): antineoplastic agent, photosensitizing agent, prodrug, dermatologic drug.

Also known as: Methyl aminolaevulinate, Methyl aminolevulinate, Methylaminolevulinate, Metvix, SID104171381, metvix, methyl aminolevulinate, METHYL AMINOLEVULINATE, Methyl Aminolevulinate_HCL

Parent form; salt/anhydrous children: CHEMBL1201093

Patent coverage: 1,340 distinct patent families (5,076 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

8 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
neoplasm	4	MONDO:0005070	EFO:0000616
basal cell carcinoma	3	MONDO:0020804	EFO:0004193
actinic keratosis	3	MONDO:0005173	EFO:0002496
acne	2	MONDO:0011438	EFO:0003894
squamous cell carcinoma	1	MONDO:0005096	EFO:0000707
dysplasia of cervix	1	MONDO:0006736	EFO:1000910
cheilitis	1	MONDO:0002102	MONDO:0002102

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 12.

Phase distribution

Phase	Trials
Not specified	4
PHASE4	3
PHASE3	3
PHASE1/PHASE2	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02464709	PHASE4	COMPLETED	Daylight PDT for Actinic Keratoses: a Multicentre Study Comparing Two Photosensitizers (BF-200 ALA Versus MAL)
NCT02647151	PHASE4	UNKNOWN	Efficacy and Safety of Treatment of Actinic Keratoses With Photodynamic Therapy Between MAL Cream and ALA Gel
NCT03511326	PHASE4	COMPLETED	PRO With Luxerm® in the Field Treatment of Thin and Non-hyperkeratotic Non-pigmented AK
NCT00472108	PHASE3	COMPLETED	Photodynamic Therapy (PDT) With Metvix Cream 160 mg/g Versus PDT With Placebo Cream in Participants With Primary Nodular Basal Cell Carcinoma
NCT00629317	PHASE3	COMPLETED	Trial of Methyl Aminolevulinate Plus Aktilite in Facial Photodamage
NCT01475071	PHASE3	COMPLETED	Intra-individual Comparison of Efficacy and Safety of Metvix® Natural Daylight Photodynamic Therapy Versus Conventional Metvix® Photodynamic Therapy in Subject With Mild Actinic Keratoses
NCT02367547	PHASE1/PHASE2	UNKNOWN	Superficial Basal Cell Cancer’s Photodynamic Therapy: Comparing Three Photosensitizers: HAL and BF-200 ALA Versus MAL
NCT01292668	PHASE1	COMPLETED	Photodynamic Therapy Using Methyl-5-Aminolevulinate Hydrochloride Cream in Determining Pain Threshold in Patients With Skin Cancer
NCT02674048	Not specified	COMPLETED	Metvix Daylight PDT in Actinic Keratosis
NCT03013647	Not specified	UNKNOWN	Daylight Photodynamic Therapy for Actinic Keratosis and Skin Field Cancerization
NCT05456334	Not specified	UNKNOWN	New Treatments for Actinic Keratoses of the Scalp
NCT05522036	Not specified	COMPLETED	Clinical Evaluation of a Short Illumination Duration (35 Minutes) When Performing PDT of AK Using the Dermaris ®

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).