Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ∼65-fold and ∼16-fold selectivitiy for the RARγ ( EC 50 =7.7 nM) over RARα ( EC 50 =500 nM) and RARβ ( EC 50 =125 nM), respectively.
In Vitro
Trifarotene (CD5789) (3.3 μL 0.33 cm 2 ; 24 hours) involves in keratinization, desquamation, cornification and cell adhesion in reconstructed human epidermis (RHE). The mean EC 50 on the combined target genes is 0.0048% for Trifarotene. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Trifarotene (0.001%-0.01% in a cream at 25 mg/mouse) shows dose-dependent comedolytic activity, being fully efficacious at 0.01% (98% reduction). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Rhino miceDosage: 0.001%, 0.0025%, 0.005% and 0.01% in a cream at 25 mg/mouse (5 cm 2 surface on the back skin on a 5 mg/cm 2 basis) Administration: Topical application; once a day; 11 days Result: Increased the epidermis thickness by 275% (66 μm) and the transepidermal water\nloss (TEWL) by 285% (26 g/h/m 2 ).
