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Details

Stereochemistry ACHIRAL
Molecular Formula C29H33NO4
Molecular Weight 459.5777
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TRIFAROTENE

SMILES

CC(C)(C)c1cc(ccc1N2CCCC2)-c3cc(ccc3OCCO)-c4ccc(cc4)C(=O)O

InChI

InChIKey=MFBCDACCJCDGBA-UHFFFAOYSA-N
InChI=1S/C29H33NO4/c1-29(2,3)25-19-23(10-12-26(25)30-14-4-5-15-30)24-18-22(11-13-27(24)34-17-16-31)20-6-8-21(9-7-20)28(32)33/h6-13,18-19,31H,4-5,14-17H2,1-3H3,(H,32,33)

HIDE SMILES / InChI

Molecular Formula C29H33NO4
Molecular Weight 459.5777
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Trifarotene is a novel first-in-class fourth-generation topical retinoid. It is a potent and selective RAR gamma-agonist. In multiple mouse models, trifarotene exhibited superior comedolytic, anti-inflammatory and depigmenting activity compared with other topical retinoids. In this 52-week study, trifarotene was safe, well-tolerated and effective in moderate facial and truncal acne. Trifarotene is in phase II clinical trial for the treatment of ichthyosis.

Approval Year

Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
12 pg/mL
200 mg 1 times / day steady-state, topical
dose: 200 mg
route of administration: Topical
experiment type: STEADY-STATE
co-administered:
TRIFAROTENE plasma
Homo sapiens
population: UNHEALTHY
age: ADOLESCENT
sex: UNKNOWN
food status: UNKNOWN
10.8 pg/mL
200 mg 1 times / day steady-state, topical
dose: 200 mg
route of administration: Topical
experiment type: STEADY-STATE
co-administered:
TRIFAROTENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
137 pg × h/mL
200 mg 1 times / day steady-state, topical
dose: 200 mg
route of administration: Topical
experiment type: STEADY-STATE
co-administered:
TRIFAROTENE plasma
Homo sapiens
population: UNHEALTHY
age: ADOLESCENT
sex: UNKNOWN
food status: UNKNOWN
118 pg × h/mL
200 mg 1 times / day steady-state, topical
dose: 200 mg
route of administration: Topical
experiment type: STEADY-STATE
co-administered:
TRIFAROTENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3 h
200 mg 1 times / day steady-state, topical
dose: 200 mg
route of administration: Topical
experiment type: STEADY-STATE
co-administered:
TRIFAROTENE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
0.01 % 1 times / day multiple, topical
Studied dose
Dose: 0.01 %, 1 times / day
Route: topical
Route: multiple
Dose: 0.01 %, 1 times / day
Sources:
unhealthy, 15 years (range: 12-17 years)
Health Status: unhealthy
Condition: acne vulgaris
Age Group: 15 years (range: 12-17 years)
Sex: M+F
Sources:
DLT: Skin irritation...
Other AEs: Skin exfoliation, Erythema...
Dose limiting toxicities:
Skin irritation (all grades, 8 patients)
Other AEs:
Skin exfoliation (all grades, 4 patients)
Erythema (all grades, 4 patients)
Sources:
0.01 % 1 times / day multiple, topical
Studied dose
Dose: 0.01 %, 1 times / day
Route: topical
Route: multiple
Dose: 0.01 %, 1 times / day
Sources:
unhealthy, 20 years (range: 18-34 years)
Health Status: unhealthy
Condition: acne vulgaris
Age Group: 20 years (range: 18-34 years)
Sex: M+F
Sources:
Other AEs: Skin irritation...
Other AEs:
Skin irritation (88.9%)
Sources:
0.01 % 1 times / day multiple, topical
Studied dose
Dose: 0.01 %, 1 times / day
Route: topical
Route: multiple
Dose: 0.01 %, 1 times / day
Sources:
unhealthy, 20 years (range: 18-34 years)
n = 18
Health Status: unhealthy
Condition: acne vulgaris
Age Group: 20 years (range: 18-34 years)
Sex: M+F
Population Size: 18
Sources:
Other AEs: Erythema...
Other AEs:
Erythema (88.9%)
Sources:
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Other AEs: Application site irritation, Application site pruritus...
Other AEs:
Application site irritation (7.5%)
Application site pruritus (2.4%)
Sunburn (2.6%)
Application site pain (< 1%)
Application site dryness (< 1%)
Application site discoloration (< 1%)
Application site rash (< 1%)
Application site swelling (< 1%)
Application site erosion (< 1%)
Erythema (< 1%)
Dermatitis allergic (< 1%)
Skin erythema (grade 1, 30.6%)
Scale (grade 1, 37.5%)
Dry skin face (grade 1, 39%)
Stinging skin (grade 1, 35.6%)
Skin erythema (grade 2, 28.4%)
Scale (grade 2, 27.1%)
Dry skin face (grade 2, 29.7%)
Stinging skin (grade 2, 20.6%)
Skin erythema (grade 3, 6.2%)
Scale (grade 3, 4.9%)
Dry skin face (grade 3, 4.8%)
Stinging skin (grade 3, 5.9%)
Skin erythema (grade 1, 26.5%)
Skin scarring (grade 1, 29.7%)
Dry skin (grade 1, 32.9%)
Stinging skin (grade 1, 26.1%)
Skin erythema (grade 2, 18.9%)
Skin scarring (grade 2, 13.7%)
Dry skin (grade 2, 16.1%)
Stinging skin (grade 2, 10.9%)
Skin erythema (grade 3, 5.2%)
Skin scarring (grade 3, 1.7%)
Dry skin (grade 3, 1.8%)
Stinging skin (grade 3, 4.3%)
Sources:
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Disc. AE: Application site irritation, Application site erosion...
AEs leading to
discontinuation/dose reduction:
Application site irritation (1.1%)
Application site erosion (0.1%)
Application site pain (0.1%)
Acne (0.2%)
Skin irritation (0.2%)
Dermatitis allergic (0.1%)
Bronchitis (0.1%)
Muscle rupture (0.1%)
Tibia fracture (0.1%)
Major depression (0.1%)
Suicide attempt (0.1%)
Sources:
0.02 % 2 times / week multiple, topical
Highest studied dose
Dose: 0.02 %, 2 times / week
Route: topical
Route: multiple
Dose: 0.02 %, 2 times / week
Sources:
unhealthy, adolescents; adults
Health Status: unhealthy
Condition: Lamellar Ichthyosis
Age Group: adolescents; adults
Sex: M+F
Sources:
12 g 2 times / week multiple, topical
Highest studied dose
Dose: 12 g, 2 times / week
Route: topical
Route: multiple
Dose: 12 g, 2 times / week
Sources:
healthy
AEs

AEs

AESignificanceDosePopulation
Erythema all grades, 4 patients
0.01 % 1 times / day multiple, topical
Studied dose
Dose: 0.01 %, 1 times / day
Route: topical
Route: multiple
Dose: 0.01 %, 1 times / day
Sources:
unhealthy, 15 years (range: 12-17 years)
Health Status: unhealthy
Condition: acne vulgaris
Age Group: 15 years (range: 12-17 years)
Sex: M+F
Sources:
Skin exfoliation all grades, 4 patients
0.01 % 1 times / day multiple, topical
Studied dose
Dose: 0.01 %, 1 times / day
Route: topical
Route: multiple
Dose: 0.01 %, 1 times / day
Sources:
unhealthy, 15 years (range: 12-17 years)
Health Status: unhealthy
Condition: acne vulgaris
Age Group: 15 years (range: 12-17 years)
Sex: M+F
Sources:
Skin irritation all grades, 8 patients
DLT
0.01 % 1 times / day multiple, topical
Studied dose
Dose: 0.01 %, 1 times / day
Route: topical
Route: multiple
Dose: 0.01 %, 1 times / day
Sources:
unhealthy, 15 years (range: 12-17 years)
Health Status: unhealthy
Condition: acne vulgaris
Age Group: 15 years (range: 12-17 years)
Sex: M+F
Sources:
Skin irritation 88.9%
0.01 % 1 times / day multiple, topical
Studied dose
Dose: 0.01 %, 1 times / day
Route: topical
Route: multiple
Dose: 0.01 %, 1 times / day
Sources:
unhealthy, 20 years (range: 18-34 years)
Health Status: unhealthy
Condition: acne vulgaris
Age Group: 20 years (range: 18-34 years)
Sex: M+F
Sources:
Erythema 88.9%
0.01 % 1 times / day multiple, topical
Studied dose
Dose: 0.01 %, 1 times / day
Route: topical
Route: multiple
Dose: 0.01 %, 1 times / day
Sources:
unhealthy, 20 years (range: 18-34 years)
n = 18
Health Status: unhealthy
Condition: acne vulgaris
Age Group: 20 years (range: 18-34 years)
Sex: M+F
Population Size: 18
Sources:
Application site pruritus 2.4%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Sunburn 2.6%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Application site irritation 7.5%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Application site discoloration < 1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Application site dryness < 1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Application site erosion < 1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Application site pain < 1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Application site rash < 1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Application site swelling < 1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Dermatitis allergic < 1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Erythema < 1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Stinging skin grade 1, 26.1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Skin erythema grade 1, 26.5%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Skin scarring grade 1, 29.7%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Skin erythema grade 1, 30.6%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Dry skin grade 1, 32.9%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Stinging skin grade 1, 35.6%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Scale grade 1, 37.5%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Dry skin face grade 1, 39%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Stinging skin grade 2, 10.9%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Skin scarring grade 2, 13.7%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Dry skin grade 2, 16.1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Skin erythema grade 2, 18.9%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Stinging skin grade 2, 20.6%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Scale grade 2, 27.1%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Skin erythema grade 2, 28.4%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Dry skin face grade 2, 29.7%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Skin scarring grade 3, 1.7%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Dry skin grade 3, 1.8%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Stinging skin grade 3, 4.3%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Dry skin face grade 3, 4.8%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Scale grade 3, 4.9%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Skin erythema grade 3, 5.2%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Stinging skin grade 3, 5.9%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Skin erythema grade 3, 6.2%
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Application site erosion 0.1%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Application site pain 0.1%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Bronchitis 0.1%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Dermatitis allergic 0.1%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Major depression 0.1%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Muscle rupture 0.1%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Suicide attempt 0.1%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Tibia fracture 0.1%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Acne 0.2%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Skin irritation 0.2%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
Application site irritation 1.1%
Disc. AE
2 g 1 times / day multiple, topical
Recommended
Dose: 2 g, 1 times / day
Route: topical
Route: multiple
Dose: 2 g, 1 times / day
Sources:
unhealthy, >= 9 years
n = 1220
Health Status: unhealthy
Condition: acne vulgaris
Age Group: >= 9 years
Sex: M+F
Population Size: 1220
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
yes [IC50 2.78 uM]
unlikely
Comment: approximately 140,000-fold higher than the Cmax of trifarotene (9.6 pg/mL equivalent to 0.00002µM)
Page: 171.0
yes [IC50 3.9 uM]
unlikely
Comment: approximately 140,000-fold higher than the Cmax of trifarotene (9.6 pg/mL equivalent to 0.00002µM)
Page: 171.0
yes [IC50 7.8 uM]
unlikely
Comment: approximately 300,000-fold higher than the Cmax of trifarotene (9.6 pg/mL equivalent to 0.00002µM)
Page: 171.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
unlikely
Comment: The PBPK modeling predicted that Cmax and AUC of trifarotene could increase by 2.3- and 2.9-fold, respectively, if co-administered with strong CYP2C9 and CYP3A4 inhibitor. The simulated highest Cmax of trifarotene was markedly lower than the safety margin of trifarotene cream 50 µg/g.
Page: 59.0
minor
minor
minor
minor
unlikely
Comment: The PBPK modeling predicted that Cmax and AUC of trifarotene could increase by 2.3- and 2.9-fold, respectively, if co-administered with strong CYP2C9 and CYP3A4 inhibitor. The simulated highest Cmax of trifarotene was markedly lower than the safety margin of trifarotene cream 50 µg/g.
Page: 59.0
no
no
no
no
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Topical trifarotene: a new retinoid.
2018 Aug
Nonclinical and human pharmacology of the potent and selective topical retinoic acid receptor-γ agonist trifarotene.
2018 Aug
Retinoids in Acne Management: Review of Current Understanding, Future Considerations, and Focus on Topical Treatments
2018 Dec 1
Retinoids in Acne Management: Review of Current Understanding, Future Considerations, and Focus on Topical Treatments
2018 Dec 1
Patents
Substance Class Chemical
Created
by admin
on Sat Jun 26 08:18:23 UTC 2021
Edited
by admin
on Sat Jun 26 08:18:23 UTC 2021
Record UNII
0J8RN2W0HK
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TRIFAROTENE
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
TRIFAROTENE [ORANGE BOOK]
Common Name English
CD-5789
Code English
(1,1':3',1''-TERPHENYL)-4-CARBOXYLIC ACID, 3''-(1,1-DIMETHYLETHYL)-4'-(2-HYDROXYETHOXY)-4''-(1-PYRROLIDINYL)-
Systematic Name English
CD5789
Code English
TRIFAROTENE [INN]
Common Name English
TRIFAROTENE [USAN]
Common Name English
TRIFAROTENE [WHO-DD]
Common Name English
3''-TERT-BUTYL-4'-(2-HYDROXYETHOXY)-4''-(PYRROLIDIN-1-YL)(1,1':3',1'')TERPHENYL-4-CARBOXYLIC ACID
Systematic Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 431014
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
WHO-ATC D10AD06
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
Code System Code Type Description
CAS
895542-09-3
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
NCI_THESAURUS
C118577
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
FDA UNII
0J8RN2W0HK
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
INN
9582
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
DRUG CENTRAL
5350
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
ChEMBL
CHEMBL3707313
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
EPA CompTox
895542-09-3
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
EVMPD
SUB184480
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
PUBCHEM
11518241
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
RXCUI
2205637
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
DRUG BANK
DB12808
Created by admin on Sat Jun 26 08:18:23 UTC 2021 , Edited by admin on Sat Jun 26 08:18:23 UTC 2021
PRIMARY
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REVERSIBLE
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ACTIVE MOIETY