Aminolevulinic Acid
drug drugOn this page
Also known as .delta.-aminolevulinic acidSID56322917delta-aminolevulinic acidACIDE_AMINOLEVULINIQUE5 amino levulinic acidC0164595AMINOLEVULINIC ACID.HCL
Summary
Aminolevulinic Acid (CHEMBL601) is an approved small-molecule photosensitizing agent (ATC L01XD04); indicated across 24 conditions including neoplasm and actinic keratosis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01XD04
- Indications: 24 conditions
- Clinical trials: 48
- Chemistry: 131.13 Da · C5H9NO3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL601 |
| Name | Aminolevulinic Acid |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 137 |
| ChEBI | CHEBI:17549 |
| ATC | L01XD04 |
| Molecular formula | C5H9NO3 |
| Molecular weight | 131.13 |
| InChIKey | ZGXJTSGNIOSYLO-UHFFFAOYSA-N |
SMILES: C(CC(=O)O)C(=O)CN
IUPAC name: 5-amino-4-oxopentanoic acid
ChEBI definition: The simplest δ-amino acid in which the hydrogens at the γ position are replaced by an oxo group. It is metabolised to protoporphyrin IX, a photoactive compound which accumulates in the skin. Used (in the form of the hydrochloride salt)in combination with blue light illumination for the treatment of minimally to moderately thick actinic keratosis of the face or scalp.
Pharmacological roles (ChEBI): photosensitizing agent, antineoplastic agent, dermatologic drug, prodrug.
Other ChEBI roles (chemical / environmental): plant metabolite, human metabolite, Saccharomyces cerevisiae metabolite, Escherichia coli metabolite, mouse metabolite.
Also known as: .delta.-aminolevulinic acid, Aminolevulinic acid, SID56322917, aminolevulinic acid, delta-aminolevulinic acid, delta-Aminolevulinic acid, ACIDE_AMINOLEVULINIQUE, AMINOLEVULINIC ACID, 5 amino levulinic acid, C0164595, AMINOLEVULINIC ACID.HCL
Parent form; salt/anhydrous children: CHEMBL18851, CHEMBL1200582, CHEMBL3350389, CHEMBL3350765
Patent coverage: 16,177 distinct patent families (53,584 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
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Beta-lactamase, Gamma-aminobutyric acid receptor subunit rho-1.
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
2 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).
| Indication | Phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| paraganglioma | 3 | MONDO:0000448 | EFO:1000453 |
17 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| actinic keratosis | 3 | MONDO:0005173 | EFO:0002496 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| brain neoplasm | 2 | MONDO:0021211 | EFO:0003833 |
| brain cancer | 2 | MONDO:0001657 | MONDO:0001657 |
| basal cell carcinoma | 2 | MONDO:0020804 | EFO:0004193 |
| desmoid tumor | 2 | MONDO:0007608 | EFO:0009907 |
| nevoid basal cell carcinoma syndrome | 2 | MONDO:0007187 | MONDO:0007187 |
| neurofibromatosis type 1 | 2 | MONDO:0018975 | MONDO:0018975 |
| anaplastic astrocytoma | 1 | MONDO:0016684 | EFO:0002499 |
| anaplastic oligodendroglioma | 1 | MONDO:0016696 | EFO:0002501 |
| acne | 1 | MONDO:0011438 | EFO:0003894 |
| gliosarcoma | 1 | MONDO:0016681 | EFO:1001465 |
| Crohn disease | 1 | MONDO:0005011 | EFO:0000384 |
| glioma | 1 | MONDO:0021042 | MONDO:0003268 |
| colonic neoplasm | 1 | MONDO:0005401 | MONDO:0021063 |
| colorectal adenocarcinoma | 1 | MONDO:0005008 | EFO:0000365 |
| soft tissue sarcoma | 1 | MONDO:0018078 | EFO:1001968 |
4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 48.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 18 |
| Not specified | 12 |
| PHASE1 | 9 |
| PHASE4 | 3 |
| PHASE1/PHASE2 | 3 |
| PHASE3 | 2 |
| EARLY_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) |
| NCT03327831 | PHASE4 | COMPLETED | Study of Daylight Photodynamic Therapy With Aminolevulinic Acid for Actinic Keratoses |
| NCT05359419 | PHASE4 | UNKNOWN | Comparison of Two Modes of Photodynamic Therapy for the Treatment of Actinic Keratosis on the Upper Extremities |
| NCT06160492 | PHASE3 | RECRUITING | Phase III Clinical Trial Evaluating the Resection Efficacy of 5-Aminolevulinic Acid Hydrochloride (5-ALA HCl) Fluorescence-Guided Microsurgery Versus Conventional White Light Microsurgery in Patients With Malignant Glioma (WHO Grade 3/4) |
| NCT00241670 | PHASE3 | COMPLETED | Fluorescence-guided Resection of Malignant Gliomas With 5-Aminolevulinic Acid |
| NCT01898416 | PHASE2 | RECRUITING | Safety and Efficacy Study Using 5-ALA Oral Administration as an Adjuvant Therapy on the Rate of Local Tumor Recurrence in Patients Who Have Desmoids Tumors |
| NCT02728388 | PHASE2 | RECRUITING | Photodynamic Therapy for Benign Dermal Neurofibromas- Phase II |
| NCT03897491 | PHASE2 | ACTIVE_NOT_RECRUITING | PD L 506 for Stereotactic Interstitial Photodynamic Therapy of Newly Diagnosed Supratentorial IDH Wild-type Glioblastoma |
| NCT06307548 | PHASE1/PHASE2 | RECRUITING | Fluorescence Image Guided Surgery Followed by Intraoperative Photodynamic Therapy for Improving Local Tumor Control in Patients With Locally Advanced or Recurrent Colorectal Cancer |
| NCT06577311 | PHASE2 | RECRUITING | Evaluating the Use of Photodynamic Therapy to Treat Facial Cutaneous Squamous Cell Carcinoma in Situ (SCCis) |
| NCT06948552 | PHASE2 | RECRUITING | Photodynamic Diagnosis of Upper Tract Urothelial Carcinoma Using Fluorescence Endoscopy and Oral 5-ALA |
| NCT00002975 | PHASE2 | COMPLETED | Photodynamic Therapy in Treating Patients With Skin Cancer |
| NCT00706433 | PHASE2 | COMPLETED | Light Dose Ranging Study of Photodynamic Therapy (PDT) With Levulan + Blue Light Versus Vehicle + Blue Light in Severe Facial Acne |
| NCT00752323 | PHASE2 | COMPLETED | Imaging Procedure Using ALA in Finding Residual Tumor in Grade IV Malignant Astrocytoma |
| NCT00865878 | PHASE2 | TERMINATED | ALA-PDT Versus Vehicle PDT for Treatment of AK and Reduction of New NMSC in Solid Organ Transplant Recipients |
| NCT00961090 | PHASE2 | COMPLETED | Safety Study of Aminolevulinic Acid (ALA) to Improve Visibility of Brain Tumors During Surgery |
| NCT00977795 | PHASE1/PHASE2 | WITHDRAWN | A Study of the Specificity and Sensitivity of 5-ALA Fluorescence in Malignant Brain Tumors |
| NCT01351519 | PHASE2 | TERMINATED | A Study of Aminolevulinic Acid Used to Enhance Visualization and Surgical Removal of Brain Tumors |
| NCT01556009 | PHASE2 | COMPLETED | Trial Comparing the Effects of Intermittent Vismodegib vs. PDT in Patients With Multiple Basal Cell Carcinomas |
| NCT01575275 | PHASE2 | TERMINATED | Aminolevulinic Acid in Visualizing a Tumor During Surgery in Patients With Glioblastoma Multiforme |
| NCT02239679 | PHASE2 | COMPLETED | Controlled Study of the Occurrence of Actinic Keratosis on the Face After Cryotherapy + Aminolevulinic Acid (ALA) Photodynamic Therapy |
| NCT04164849 | PHASE1/PHASE2 | COMPLETED | Extracorporeal Photopheresis of Patients With Crohn’s Disease Using 5-aminolevulinic Acid |
| NCT04738162 | PHASE2 | COMPLETED | Clinical Safety Study on 5-Aminolevulinic Acid (5-ALA) in Children and Adolescents With Brain Tumors |
| NCT04845919 | PHASE2 | COMPLETED | Sonodynamic Therapy With ExAblate System in Glioblastoma Patients |
| NCT06159842 | PHASE2 | COMPLETED | Evaluating the Use of Photodynamic Therapy to Treat Facial Cutaneous Squamous Cell Carcinoma in Situ (isSCC) |
| NCT07027670 | PHASE2 | COMPLETED | Treatment With 5-AminoLEvuliNic Acid Before Cardiac Surgery |
| NCT02191488 | PHASE1 | ACTIVE_NOT_RECRUITING | ALA-induced PpIX Fluorescence During Brain Tumor Resection |
| NCT06623201 | PHASE1 | RECRUITING | Blue-Light Photodynamic Therapy and Sonidegib for Multiple Basal Cell Carcinomas |
| NCT00671710 | PHASE1 | COMPLETED | Study of Aminolevulinic Acid to Enhance Visualization and Resection of Malignant Glial Tumors of the Brain |
| NCT00870779 | PHASE1 | COMPLETED | Fluorescence Guided Resection of Brain Tumors |
| NCT01148966 | PHASE1 | TERMINATED | Aminolevulinic Acid During Surgery in Treating Patients With Malignant Brain Tumors |
| NCT01502605 | PHASE1 | TERMINATED | Phase I Study of Orally Administered Aminolevulinic Acid for Resection of Malignant Astrocytomas |
| NCT03322293 | PHASE1 | COMPLETED | Daylight Photodynamic Therapy for Actinic Keratosis |
| NCT06252727 | PHASE1 | WITHDRAWN | Fluorescent Aided Resection and Evaluation of Soft Tissue Sarcomas (FLARES) |
| NCT06665724 | PHASE1 | COMPLETED | Clinical Trial Evaluating Safety of 5-Aminolevulinic Acid (5-ALA) Combined With CV01 Delivery of Ultrasound for Sonodynamic Therapy (SDT) in Patients With Newly Diagnosed High-Grade Glioma (HGG) Prior to Resection and Standard Adjuvant Therapy (ALA SDT GLIOMA 401) |
| NCT00663910 | EARLY_PHASE1 | TERMINATED | Topical Aminolevulinic Acid in Patients With Nonmelanoma Skin Cancer |
| NCT05850377 | Not specified | NOT_YET_RECRUITING | 5-Aminolevulinic Acid (5-ALA) Gliolan®: Usage Increase Proposal for Neurosurgical Procedures in High-Grade Gliomas |
| NCT06777511 | Not specified | NOT_YET_RECRUITING | Advancing Antimicrobial Photodynamic Therapy to Prevent Infection in Osseointegrated Prosthesis Patients |
| NCT00524485 | Not specified | TERMINATED | Photodynamic Therapy Using Topical Aminolevulinic Acid in Treating Patients With Actinic Keratosis |
| NCT01508741 | Not specified | COMPLETED | Use Of The Dietary Supplement 5-ALA And Its Relationship With Sleep And Mood |
| NCT01610778 | Not specified | COMPLETED | Effects of 5-Aminolevulinic Acid on Glucose Metabolism |
| NCT01812837 | Not specified | COMPLETED | The Use of Microneedles in Photodynamic Therapy |
| NCT02594644 | Not specified | COMPLETED | The Use of Microneedles to Expedite Treatment Time in Photodynamic Therapy |
| NCT02644187 | Not specified | COMPLETED | Pain Relief During Photodynamic Therapy for Actinic Keratoses With a New Irradiation Protocol |
| NCT04055688 | Not specified | COMPLETED | Novel Exoscope System for 5-ALA Fluorescence-Guided Surgery for Gliomas |
| NCT04390802 | Not specified | UNKNOWN | A Pilot Study of 5-Aminolevulinic Acid (5-ALA) to Enhance Visualization of Pituitary Adenomas |
| NCT04709289 | Not specified | COMPLETED | Adverse Effects of ALA-PDT for the Treatment of Moderate to Severe Acne Vulgaris: a Prospective Study |
| NCT05228483 | Not specified | UNKNOWN | Carbon Dioxide（CO2）Fractional Laser Plus Photodynamic Therapy in Female Patients With Vulvar Lichen Sclerosus |
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).
Related Atlas pages
- Indicated for: neoplasm, paraganglioma
- In clinical trials for: actinic keratosis, glioblastoma, brain neoplasm, brain cancer, basal cell carcinoma, desmoid tumor, nevoid basal cell carcinoma syndrome, neurofibromatosis type 1