trifarotene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| arotinoid derivatives | 5350 | 895542-09-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
AKLIEF Cream for topical administration contains 0.005% (50 mcg/g) trifarotene. Trifarotene is a terphenyl acid derivative and is a retinoid. Trifarotene is an agonist of retinoic acid receptors (RAR), with particular activity at the gamma subtype of RAR. Stimulation of RAR results in modulation of target genes which are associated with various processes, including cell differentiation and mediation of inflammation. The exact process by which trifarotene ameliorates acne is unknown.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 4, 2019 | FDA | GALDERMA R AND D |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | D10AD06 | DERMATOLOGICALS ANTI-ACNE PREPARATIONS ANTI-ACNE PREPARATIONS FOR TOPICAL USE Retinoids for topical use in acne |
| MeSH PA | D003879 | Dermatologic Agents |
| FDA CS | M0018962 | Retinoids |
| FDA EPC | N0000175607 | Retinoid |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acne vulgaris | indication | 88616000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.05 | acidic |
| pKa2 | 4.95 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 0.005% | AKLIEF | GALDERMA LABS LP | N211527 | Oct. 4, 2019 | RX | CREAM | TOPICAL | 8227507 | Dec. 21, 2025 | TOPICAL TREATMENT OF ACNE VULGARIS |
| 0.005% | AKLIEF | GALDERMA LABS LP | N211527 | Oct. 4, 2019 | RX | CREAM | TOPICAL | 8470871 | Dec. 21, 2025 | METHOD OF ACTIVATING RARGAMMA RECEPTOR |
| 0.005% | AKLIEF | GALDERMA LABS LP | N211527 | Oct. 4, 2019 | RX | CREAM | TOPICAL | 9084778 | May 30, 2033 | TREATMENT OF ACNE VULGARIS |
| 0.005% | AKLIEF | GALDERMA LABS LP | N211527 | Oct. 4, 2019 | RX | CREAM | TOPICAL | 9498465 | May 30, 2033 | TOPICAL TREATMENT OF ACNE VULGARIS |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 0.005% | AKLIEF | GALDERMA LABS LP | N211527 | Oct. 4, 2019 | RX | CREAM | TOPICAL | Oct. 4, 2024 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Retinoic acid receptor gamma | Nuclear hormone receptor | AGONIST | EC50 | 8.11 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Retinoic acid receptor alpha | Nuclear hormone receptor | AGONIST | EC50 | 6.30 | SCIENTIFIC LITERATURE | ||||
| Retinoic acid receptor beta | Nuclear hormone receptor | AGONIST | EC50 | 6.90 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| 0J8RN2W0HK | UNII |
| C4519213 | UMLSCUI |
| CHEMBL3707313 | ChEMBL_ID |
| 11518241 | PUBCHEM_CID |
| DB12808 | DRUGBANK_ID |
| D11225 | KEGG_DRUG |
| 9582 | INN_ID |
| 9962 | IUPHAR_LIGAND_ID |
| 018160 | NDDF |
| 818968008 | SNOMEDCT_US |
| 818975009 | SNOMEDCT_US |
| 4038777 | VANDF |
| 2205637 | RXNORM |
| 324748 | MMSL |
| 37492 | MMSL |
| C000629420 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| AKLIEF | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0299-5935 | CREAM | 50 ug | TOPICAL | NDA | 23 sections |
| AKLIEF | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0299-5935 | CREAM | 50 ug | TOPICAL | NDA | 23 sections |
| AKLIEF | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0299-5935 | CREAM | 50 ug | TOPICAL | NDA | 23 sections |