trifarotene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
arotinoid derivatives 5350 895542-09-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • trifarotene
  • CD5789
  • aklief
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.
  • Molecular weight: 459.59
  • Formula: C29H33NO4
  • CLOGP: 6.67
  • LIPINSKI: 1
  • HAC: 5
  • HDO: 2
  • TPSA: 70
  • ALOGS: -5.69
  • ROTB: 8

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
ATC D10AD06 DERMATOLOGICALS
ANTI-ACNE PREPARATIONS
ANTI-ACNE PREPARATIONS FOR TOPICAL USE
Retinoids for topical use in acne
MeSH PA D003879 Dermatologic Agents

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Acne vulgaris indication 88616000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.05 acidic
pKa2 4.95 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.005% AKLIEF GALDERMA LABS LP N211527 Oct. 4, 2019 RX CREAM TOPICAL Oct. 4, 2024 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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:

IDSource
0J8RN2W0HK UNII
C4519213 UMLSCUI
CHEMBL3707313 ChEMBL_ID
11518241 PUBCHEM_CID
DB12808 DRUGBANK_ID
D11225 KEGG_DRUG
9962 IUPHAR_LIGAND_ID
2205637 RXNORM
324748 MMSL
37492 MMSL
818968008 SNOMEDCT_US
818975009 SNOMEDCT_US
4038777 VANDF
018160 NDDF
C000629420 MESH_SUPPLEMENTAL_RECORD_UI
9582 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
AKLIEF HUMAN PRESCRIPTION DRUG LABEL 1 0299-5935 CREAM 50 ug TOPICAL NDA 23 sections