methyl aminolevulinate
Trade name: metvixia
Approved
Jul 27, 2004
Methyl aminolevulinate is a prodrug that is metabolised to Protoporphyrin IX (a photosensitizer) used in photodynamic therapy. 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. Methyl aminolevulinate is used 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). — NCATS
Clinical trial activity
45 trials · 47 clinical orgs · 2 marketing orgs
Earliest trial started Sep 30, 2000 (NCT00473343)
Timeline
Indications
Approved for
Studied for
- Acne Vulgaris · Phase 2
- Basal Cell Carcinoma · Phase 4
- Bowen's Disease · Phase 4
- Carcinoma, Squamous Cell · Phase 1
- Cheilitis · Phase 1
- Dermatology · Phase 4
- Facial Injuries · Phase 2
- Healthy Volunteers · Phase 1
- Keratosis, Actinic · Phase 4
- Low-Level Light Therapy · Phase 4
- Neoplasms, Basal Cell · Phase 1/Phase 2
- Pain · Phase 1
- Photochemotherapy · Phase 1/Phase 2
- Photosensitizing Agents · Phase 1/Phase 2
- Skin Aging · Phase 3
- Skin Neoplasms · Phase 1
- Uterine Cervical Dysplasia · Phase 1/Phase 2
- Vulvar Neoplasms · Phase 2
Mechanism of action
- DNAINHIBITOR
DNA inhibitor
Photodynamic therapy
Approval history
- approvedJul 27, 2004
Chemistry & pharmacology
SMILES
COC(=O)CCC(=O)CN- Mol. weight
- 145.16 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Topical
- Availability
- Discontinued
Oral
No
Parenteral
No
Topical
Yes
Sources
- ChEMBLCHEMBL1096562 ↗
- WikipediaMethyl aminolevulinate ↗
- NCATS585NM85KYM ↗
- ChEMBLCHEMBL1201093 ↗
Also known as
- 5-amino-4-oxopentanoic acid methyl ester
- 5-aminolevulinic acid methyl ester
- 5-aminolevulinic acid methyl ester
- 5-aminolevulinic acid methyl ester
- aktilite
- ala-me
- aminolevulinic acid methyl ester
- aminolevulinic acid methyl ester
- aminolevulinic acid methyl ester
- aminolevulinic acid methyl ester
- aminolevulinic acid methyl ester
- aminolevulinic acid methyl ester
- delta-aminolevulinic acid methyl ester
- maop cpd
- methyl 5-aminolevulinate
- methyl-5-aminolevulinate
- methyl-5-aminolevulinate
- methyl aminolaevulinate
- methyl aminolaevulinate
- methylaminolevulinate
- methyl aminolevulinate
- methyl aminolevulinate
- methyl aminolevulinate
- methyl aminolevulinate
- methyl aminolevulinate
- methyl aminolevulinate
- methyl aminolevulinate
- methyl-aminolevulinate
- methyl-aminolevulinate
- methyl aminolevulinate hcl
- methyl aminolevulinate hcl
- methyl aminolevulinate hcl
- methyl aminolevulinate hydrochloride
- methyl aminolevulinate hydrochloride
- methyl aminolevulinate hydrochloride
- methyl aminolevulinate hydrochloride
- methyl delta-aminolevulinate
- methyl delta-aminolevulinate
- metvix
- metvix
- metvix
- metvix
- metvixia
- metvixia
- metvixia
- metvixia
- p-1202
- p-1202
- visonac
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05104099 | Phase 2 | Nov 1, 2021 | Institut de Cancérologie de Lorraine |
| NCT04085367 | Phase 3 | Sep 30, 2019 | Galderma |
| NCT03909646 | Phase 4 | May 31, 2019 | Maastricht University |
| NCT03013647 | N/A | Sep 1, 2016 | Hospital das Clinicas da USP, University of Sao Paulo |
| NCT05456334 | N/A | Mar 24, 2016 | University of Helsinki |
| NCT02736760 | Phase 4 | Mar 1, 2016 | University of Regensburg |
| NCT02647151 | Phase 4 | Dec 1, 2015 | University of Valencia |
| NCT02392390 | N/A | Oct 1, 2015 | Centre Hospitalier Universitaire de Nīmes |
| NCT02464709 | Phase 4 | Jun 1, 2015 | Government of Finland, Radiation and Nuclear Safety Authority, Finland, University of Helsinki, University of Tampere |
| NCT02367547 | Phase 1/Phase 2 (Phase 2) | Mar 1, 2015 | Government of Finland, University of Jyvaskyla, University of Tampere |
| NCT02373371 | Phase 3 | Mar 1, 2015 | Galderma, University of Limoges |
| NCT02354391 | Phase 2 | Jan 1, 2015 | Leo Pharma, Pacific Dermaesthetics |
| NCT02281682 | Phase 4 | Jan 1, 2015 | Maastricht University |
| NCT02372370 | Phase 1 | Dec 1, 2014 | University of Copenhagen |
| NCT03012009 | N/A | Sep 1, 2014 | Ghent University |
| NCT02670655 | Phase 1 | Jun 1, 2014 | Dong-A University |
| NCT02976727 | Phase 1 | May 1, 2014 | Dong-A University |
| NCT02149342 | Phase 1/Phase 2 (Phase 2) | May 1, 2014 | Government of Finland, University of Helsinki |
| NCT02139618 | Phase 2 | Apr 1, 2014 | Fundación Dermabase, Universidad de Antioquia |
| NCT02511145 | Phase 1 | Feb 1, 2014 | Galderma |
Organizations
Research & Development (47)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Galderma | For profit | 10 | 7 | 3 | 2000 |
| Dong-A University | Academic/Hospital | 7 | 7 | 1 | 2011 |
| Photocure | For profit | 7 | 7 | 1 | 2006 |
| Government of Finland | Government | 4 | 4 | 2 | 2013 |
| University of Helsinki | Academic/Hospital | 4 | 1 | 3 | 2013 |
| Maastricht University | Academic/Hospital | 3 | 3 | 1 | 2013 |
| Accovion GmbH | For profit | 2 | 0 | 1 | 2008 |
| Biofrontera Bioscience GmbH | For profit | 2 | 2 | 1 | 2008 |
| Innovaderm | For profit | 2 | 1 | 2 | 2007 |
| Universidad de Antioquia | Academic/Hospital | 2 | 1 | 2 | 2008 |
| University of Tampere | Academic/Hospital | 2 | 0 | 2 | 2015 |
| Centre Hospitalier Universitaire de Nīmes | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Dermatology Institute of DuPage Medical Group | Academic/Hospital | 1 | 0 | 1 | 2008 |
| Derm Research Incorporated | For profit | 1 | 0 | 1 | 2010 |
| Erasmus University Rotterdam | Academic/Hospital | 1 | 0 | 1 | 2013 |
| Fundación Dermabase | Academic/Hospital | 1 | 1 | 1 | 2014 |
| Ghent University | Academic/Hospital | 1 | 1 | 1 | 2014 |
| Gottfried Wilhelm Leibniz Universität Hannover | Academic/Hospital | 1 | 0 | 1 | 2006 |
| Hospital das Clinicas da USP | Academic/Hospital | 1 | 0 | 1 | 2016 |
| Hudlegekontoret Lillehammer | Academic/Hospital | 1 | 0 | 1 | 2012 |