trifarotene
Trade name: Aklief
Approved
Oct 4, 2019
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. — NCATS
Clinical trial activity
14 trials · 7 clinical orgs · 2 marketing orgs
Earliest trial started Jun 1, 2012 (NCT01616654)
Timeline
Indications
Approved for
Mechanism of action
- Retinoic acid receptorAGONIST
Retinoic acid receptor agonist
- Retinoic acid receptor gammaAGONIST
Retinoic acid receptor gamma agonist
Activation of RAR has downstream effects including anti-inflammatory effects. However, the precise role in alleviating acne is unknown. The gamma subtype is most relevant to acne.
Most active at the gamma subtype, > 20-fold selectivity over RAR alpha and RAR beta.
Approval history
- approvedOct 4, 2019
Chemistry & pharmacology
SMILES
CC(C)(C)c1cc(-c2cc(-c3ccc(C(=O)O)cc3)ccc2OCCO)ccc1N1CCCC1- Mol. weight
- 459.59 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Topical
- Availability
- Prescription Only
Oral
No
Parenteral
No
Topical
Yes
Sources
- ChEMBLCHEMBL3707313 ↗
- WikipediaTrifarotene ↗
- NCATS0J8RN2W0HK ↗
Also known as
- cd5789
- cd5789
- trifarotene
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07186413 | Phase 3 | Sep 23, 2025 | Galderma |
| NCT06733402 | Phase 1 | Jun 20, 2024 | Taro Pharmaceuticals |
| NCT06063473 | Phase 1 | Feb 22, 2023 | Taro Pharmaceuticals |
| NCT05550337 | Phase 3 | Sep 19, 2022 | Teva |
| NCT05089708 | Phase 4 | Dec 31, 2021 | Galderma |
| NCT04856904 | Phase 4 | May 28, 2021 | Galderma |
| NCT04451330 | Phase 4 | Jul 28, 2020 | Galderma |
| NCT03915860 | Phase 3 | Apr 8, 2019 | Galderma |
| NCT03738800 | Phase 2 | Feb 21, 2019 | Mayne Pharma, Yale University |
| NCT02566369 | Phase 3 | Nov 30, 2015 | Galderma, Windsor Clinical Research |
| NCT02556788 | Phase 3 | Nov 1, 2015 | Galderma |
| NCT02189629 | Phase 3 | Feb 23, 2015 | Galderma |
| NCT01804335 | Phase 1 | Feb 1, 2013 | Galderma, University of Texas at Houston |
| NCT01616654 | Phase 2 | Jun 1, 2012 | Galderma |
Organizations
Research & Development (7)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Galderma | For profit | 10 | 9 | 4 | 2012 |
| Taro Pharmaceuticals | For profit | 2 | 2 | 1 | 2023 |
| Mayne Pharma | For profit | 1 | 1 | 1 | 2019 |
| Teva | For profit | 1 | 1 | 1 | 2022 |
| University of Texas at Houston | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Windsor Clinical Research | For profit | 1 | 0 | 1 | 2015 |
| Yale University | Academic/Hospital | 1 | 0 | 1 | 2019 |