aminolevulinic acid 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 166 | 106-60-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A compound produced from succinyl-CoA and GLYCINE as an intermediate in heme synthesis. It is used as a PHOTOCHEMOTHERAPY for actinic KERATOSIS.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 60 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.12 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.88 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.88 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.83 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 34 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 3, 1999 | FDA | DUSA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Application site erythema | 150.04 | 126.55 | 26 | 379 | 4809 | 63483808 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Application site erythema | 142.31 | 109.97 | 23 | 249 | 2313 | 34954346 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Application site erythema | 289.19 | 93.80 | 47 | 551 | 5063 | 79738727 |
| Application site pain | 179.71 | 93.80 | 31 | 567 | 4716 | 79739074 |
| Erythema | 120.05 | 93.80 | 49 | 549 | 223241 | 79520549 |
| Application site swelling | 119.42 | 93.80 | 17 | 581 | 736 | 79743054 |
| Application site pustules | 105.57 | 93.80 | 11 | 587 | 26 | 79743764 |
| Oedema | 95.14 | 93.80 | 35 | 563 | 119545 | 79624245 |
| Off label use | 93.84 | 93.80 | 66 | 532 | 907149 | 78836641 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XD04 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Sensitizers used in photodynamic/radiation therapy |
| FDA CS | M0017335 | Porphyrinogens |
| MeSH PA | D003879 | Dermatologic Agents |
| MeSH PA | D017319 | Photosensitizing Agents |
| MeSH PA | D011838 | Radiation-Sensitizing Agents |
| FDA EPC | N0000175846 | Porphyrin Precursor |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:47868 | photosensitising agent |
| CHEBI has role | CHEBI:50177 | dermatologic agent |
| CHEBI has role | CHEBI:50266 | Prodrugs |
| CHEBI has role | CHEBI:75771 | Mus musculus metabolites |
| CHEBI has role | CHEBI:75772 | S. cerevisiae metabolites |
| CHEBI has role | CHEBI:76924 | plant metabolites |
| CHEBI has role | CHEBI:76971 | Escherichia coli metabolites |
| CHEBI has role | CHEBI:77746 | Homo sapiens metabolite |
| FDA MoA | N0000193981 | Fluorescence Contrast Activity |
| FDA EPC | N0000193983 | Optical Imaging Agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Fluorescent stain | indication | 35352008 | |
| Actinic keratosis | indication | 201101007 | DOID:8866 |
| Non-Hyperkeratotic Actinic Keratoses | indication | ||
| Photosensitivity | contraindication | 90128006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.82 | acidic |
| pKa2 | 9.59 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 20% | LEVULAN | DUSA | N020965 | Dec. 3, 1999 | RX | SOLUTION | TOPICAL | 10357567 | Jan. 12, 2038 | TREATMENT OF ACTINIC KERATOSES OF UPPER EXTREMITIES BY PHOTODYNAMIC THERAPY |
| 20% | LEVULAN | DUSA | N020965 | Dec. 3, 1999 | RX | SOLUTION | TOPICAL | 11077192 | Jan. 12, 2038 | TREATMENT OF ACTINIC KERATOSES OF UPPER EXTREMITIES BY PHOTODYNAMIC THERAPY |
| 20% | LEVULAN | DUSA | N020965 | Dec. 3, 1999 | RX | SOLUTION | TOPICAL | 11135293 | Jan. 12, 2038 | TREATMENT OF ACTINIC KERATOSES OF UPPER EXTREMITIES BY PHOTODYNAMIC THERAPY |
| 20% | LEVULAN | DUSA | N020965 | Dec. 3, 1999 | RX | SOLUTION | TOPICAL | 11571478 | Jan. 12, 2038 | TREATMENT OF ACTINIC KERATOSES OF UPPER EXTREMITIES BY PHOTODYNAMIC THERAPY |
| 20% | LEVULAN | DUSA | N020965 | Dec. 3, 1999 | RX | SOLUTION | TOPICAL | 11690914 | Jan. 12, 2038 | TREATMENT OF ACTINIC KERATOSES OF UPPER EXTREMITIES BY PHOTODYNAMIC THERAPY |
| 10% | AMELUZ | BIOFRONTERA | N208081 | May 10, 2016 | RX | GEL | TOPICAL | 11235169 | Oct. 15, 2040 | TOPICAL LESION-DIRECTED AND FIELD-DIRECTED TREATMENT OF ACTINIC KERATOSIS OF THE FACE AND SCALP WITH PHOTODYNAMIC THERAPY BY POSITIONING AN ILLUMINATION DEVICE IN AN APPROPRIATE DISTANCE AND ILLUMINATING THE TREATMENT AREA WITH NARROWBAND RED LIGHT |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 1.5GM/VIAL | GLEOLAN | NXDC | N208630 | June 6, 2017 | RX | FOR SOLUTION | ORAL | June 6, 2024 | OPTICAL IMAGING AGENT INDICATED IN PATIENTS WITH GLIOMA (SUSPECTED WORLD HEALTH ORGANIZATION GRADES III OR IV ON PREOPERATIVE IMAGING) AS AN ADJUNCT FOR THE VISUALIZATION OF MALIGNANT TISSUE DURING SURGERY |
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| 4025779 | VUID |
| N0000176068 | NUI |
| D02908 | KEGG_DRUG |
| 5451-09-2 | SECONDARY_CAS_RN |
| 1806646 | RXNORM |
| C0002563 | UMLSCUI |
| CHEBI:17549 | CHEBI |
| CHEMBL601 | ChEMBL_ID |
| 137 | PUBCHEM_CID |
| DB00855 | DRUGBANK_ID |
| CHEMBL1200582 | ChEMBL_ID |
| D000622 | MESH_DESCRIPTOR_UI |
| C000614854 | MESH_SUPPLEMENTAL_RECORD_UI |
| 4784 | IUPHAR_LIGAND_ID |
| 88755TAZ87 | UNII |
| 228491 | MMSL |
| 30525 | MMSL |
| 8581 | MMSL |
| d07530 | MMSL |
| 259496005 | SNOMEDCT_US |
| 409398000 | SNOMEDCT_US |
| 784354008 | SNOMEDCT_US |
| FVT | PDB_CHEM_ID |
| 4023632 | VANDF |
| 4025779 | VANDF |
| 009074 | NDDF |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| GLEOLAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59137-231 | POWDER, FOR SOLUTION | 1500 mg | ORAL | NDA | 30 sections |
| AMELUZ | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70621-101 | GEL | 100 mg | TOPICAL | NDA | 26 sections |
| AMELUZ | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70621-101 | GEL | 100 mg | TOPICAL | NDA | 26 sections |
| AMELUZ | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70621-101 | GEL | 100 mg | TOPICAL | NDA | 26 sections |
| GLEOLAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71469-231 | POWDER, FOR SOLUTION | 1500 mg | ORAL | NDA | 26 sections |