Details
Stereochemistry | ACHIRAL |
Molecular Formula | C29H33NO4 |
Molecular Weight | 459.5766 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(C)C1=CC(=CC=C1N2CCCC2)C3=CC(=CC=C3OCCO)C4=CC=C(C=C4)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)
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.
Originator
Approval Year
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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) Sources: 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, 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... |
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... |
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%) Sources: 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%) |
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%) Sources: 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%) |
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 Health Status: healthy Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211527Orig1s000MultidisclipineR.pdf#page=171 Page: 171.0 |
no | |||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211527Orig1s000MultidisclipineR.pdf#page=171 Page: 171.0 |
no | |||
no | ||||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211527Orig1s000MultidisclipineR.pdf#page=171 Page: 171.0 |
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) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211527Orig1s000MultidisclipineR.pdf#page=171 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) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211527Orig1s000MultidisclipineR.pdf#page=171 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) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211527Orig1s000MultidisclipineR.pdf#page=171 Page: 171.0 |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211527Orig1s000MultidisclipineR.pdf#page=59 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211527Orig1s000MultidisclipineR.pdf#page=59 Page: 59.0 |
|||
no | ||||
no | ||||
no | ||||
no | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
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 |
|
Randomized phase 3 evaluation of trifarotene 50 μg/g cream treatment of moderate facial and truncal acne. | 2019 Jun |
|
Long-term safety and efficacy of trifarotene 50 μg/g cream, a first-in-class RAR-γ selective topical retinoid, in patients with moderate facial and truncal acne. | 2020 Jan |
Patents
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
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Code | English | ||
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Systematic Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Systematic Name | English |
Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
431014
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
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WHO-ATC |
D10AD06
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
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Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
895542-09-3
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
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PRIMARY | |||
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C118577
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
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PRIMARY | |||
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0J8RN2W0HK
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
|
PRIMARY | |||
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m12163
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
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PRIMARY | |||
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9582
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
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PRIMARY | |||
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5350
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
|
PRIMARY | |||
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100000170499
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
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PRIMARY | |||
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CHEMBL3707313
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
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PRIMARY | |||
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DTXSID30237781
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
|
PRIMARY | |||
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SUB184480
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
|
PRIMARY | |||
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11518241
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
|
PRIMARY | |||
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0J8RN2W0HK
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
|
PRIMARY | |||
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2205637
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
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PRIMARY | |||
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DE-16
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
|
PRIMARY | |||
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DB12808
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
|
PRIMARY | |||
|
Trifarotene
Created by
admin on Sat Dec 16 01:45:45 GMT 2023 , Edited by admin on Sat Dec 16 01:45:45 GMT 2023
|
PRIMARY |
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