trifarotene 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: 6.31
  • 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

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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acne vulgaris indication 88616000

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)

None

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
4038777 VANDF
C5209982 UMLSCUI
CHEMBL3707313 ChEMBL_ID
D11225 KEGG_DRUG
11518241 PUBCHEM_CID
C000629420 MESH_SUPPLEMENTAL_RECORD_UI
9582 INN_ID
DB12808 DRUGBANK_ID
0J8RN2W0HK UNII
9962 IUPHAR_LIGAND_ID
2205637 RXNORM
324748 MMSL
37492 MMSL
018160 NDDF
818968008 SNOMEDCT_US
818975009 SNOMEDCT_US

Pharmaceutical products:

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