Trifarotene

Highest phase reached
Approved
www.ebi.ac.uk
Drug type
Small molecule
www.ebi.ac.uk
First approval year
2019
www.ebi.ac.uk

First approval year
2019
www.ebi.ac.uk
Listing at source
Listed
Highest phase reached
Approved
www.ebi.ac.uk

Drug type
Small molecule
www.ebi.ac.uk
Drug name
Trifarotene
www.ebi.ac.uk
Molecular weight
459.59
www.ebi.ac.uk
Structure (SMILES)
CC(C)(C)c1cc(-c2cc(-c3ccc(C(=O)O)cc3)ccc2OCCO)ccc1N1CCCC1
www.ebi.ac.uk

  • aklief
  • Aklief

  • aklief
  • AKLIEF®
  • cd 5789
  • CD-5789
  • cd5789
  • CD5789
  • CD5789 (trifarotene)
  • trifarotene
  • Trifarotene
  • trifarotene [INN]
  • TRIFAROTENE [MI]
  • TRIFAROTENE [ORANGE BOOK]
  • TRIFAROTENE [USAN]
  • Trifarotene [WHO-DD]
  • Trifarotene cream
  • Trifarotene Cream
  • trifarotene inn
  • trifarotene mi
  • trifarotene orange book
  • trifarotene usan
  • trifarotene who dd
  • trifaroteno
  • Trifaroteno

ATC classification codes
  • D10AD06
Sources for recorded values
www.ebi.ac.uk
CAS registry numbers
  • 895542-09-3
ChEMBL ID
CHEMBL3707313
www.ebi.ac.uk
InChIKey
MFBCDACCJCDGBA-UHFFFAOYSA-N
www.ebi.ac.uk
PubChem compound IDs
  • 11518241
RxNorm IDs (RxCUI)
  • 2205637
FDA ingredient codes (UNII)
  • 0J8RN2W0HK

Applicant
GALDERMA LABS LP
Approval date
4 Oct 2019
Application number
NDA211527

Patents
3
Designations
1
Earliest recorded loss of exclusivity
30 May 2033
First in class
No
Fast track
No
Breakthrough designation
No
Orphan designation
No
Priority review
No
Orphan exclusivity
No
Accelerated approval
No
Availability
Prescription only

Pharmacology name
trifarotene
Type
Synthetic organic
Drug name stem
-arotene
Approval recorded by Guide to Pharmacology
Yes

Administration routes

  • topical

  • Action
    Agonist
    Action type
    Agonist
    Target
    Retinoic acid receptor-α
    Gene symbol
    RARA
    Protein identifier
    P10276
    Median affinity
    6.3
    Affinity units
    pEC50
  • Action
    Agonist
    Action type
    Agonist
    Target
    Retinoic acid receptor-β
    Gene symbol
    RARB
    Protein identifier
    P10826
    Median affinity
    6.9
    Affinity units
    pEC50
  • Action
    Agonist
    Action type
    Agonist
    Target
    Retinoic acid receptor-γ
    Gene symbol
    RARG
    Protein identifier
    P13631
    Median affinity
    8.11
    Affinity units
    pEC50
    Primary target
    Yes
  • Mechanism
    Retinoic acid receptor gamma agonist
    Action type
    Agonist
    Target
    Retinoic acid receptor gamma
    Protein identifier
    P13631

Open Targets mechanisms

  • Mechanism
    Retinoic acid receptor gamma agonist
    Action type
    Agonist
    Target
    Retinoic acid receptor gamma

  • Action type
    Agonist
    Gene symbol
    RARA
    Protein identifier
    P10276
    Organism
    Homo sapiens
    Target development level
    Clinical
  • Action type
    Agonist
    Gene symbol
    RARB
    Protein identifier
    P10826
    Organism
    Homo sapiens
    Target development level
    Clinical
  • Action type
    Agonist
    Gene symbol
    RARG
    Protein identifier
    P13631
    Organism
    Homo sapiens
    Target development level
    Clinical

  • Condition
    Lymphoma
    Highest recorded phase
    1
    Condition identifier
    EFO:0000574
    Subject identifier
    D008223
  • Condition
    Acne Vulgaris
    Highest recorded phase
    4
    Condition identifier
    EFO:0003894
    Subject identifier
    D000152
  • Condition
    Ichthyosis, Lamellar
    Highest recorded phase
    2
    Condition identifier
    MONDO:0017778
    Subject identifier
    D017490

  • Condition identifier
    EFO_0000574
    Highest recorded phase
    1
  • Condition identifier
    EFO_0003894
  • Condition identifier
    MONDO_0000607
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0011438
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0017778
    Highest recorded phase
    2

Dose
One pump actuation for face, two actuations for upper trunk, optionally one more for back if acne present
Route
Topical
How often
Once daily

  • Apply in the evening
  • Apply to affected areas of face and/or trunk
  • Avoid contact with eyes, lips, creases, mucous membranes
  • On clean and dry skin

Hydrogen bond acceptors
4
Hydrogen bond donors
2
Polar surface area
70
Calculated partition coefficient (ALogP)
5.99
Calculated partition coefficient (XLogP)
6.3
Prodrug
No
Chirality
Achiral
Inorganic
No
Rule-of-five violations
1
Rotatable bonds
7
Heavy atoms
34
Molecular formula
C29H33NO4
Monoisotopic mass
459.24095853
Natural product
Yes

  • 0299-5935

Recorded assays
12
Active assays
6

Active assay types

  • Confirmatory

Distribution coefficient (LogD)

Median
3.5
Mean
3.5
Minimum
3.5
Maximum
3.5
Unit
unitless
Assays
1
Standard deviation
0
Summary method
median
Censored results excluded
0
Other units excluded
0
Unknown units excluded
0

Measurement types

  • LogD

Related records

Trials (14)

Approved for (1)

In development for (2)

Targets (1)