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Trifarotene is a topical retinoid indicated for the treatment of acne vulgaris. Retinoids are a class of medications structurally and functionally analogous to vitamin A, though later generation retinoids such as trifarotene and adapalene bear little structural resemblance to vitamin A and are analogous only in function.
- Mechanism
- Curator reviewed · 3 references
Trifarotene is a potent and selective agonist of retinoic acid receptor-γ (RAR-γ). It has significantly less activity at RAR-β and RAR-α (16- and 65-fold lower than activity at RAR-γ, respectively), and has no activity at retinoid X receptors (RXRs). Agonism at retinoic acid receptors results in dimerization, and the resulting receptor-ligand dimer binds to specific DNA regulatory sequences (retinoic acid response elements, or RAREs) in the promotor regions of retinoid-responsible genes. Downstream alterations to gene expression induced by binding to these regions is the principle mechanism through which trifarotene exerts its comedolytic, anti-inflammatory, and depigmenting effects.
Like other retinoids, trifarotene influences the expression of a number of genes involved in retinoid metabolism, epidermal differentiation/proliferation, and epidermal response to stress. In addition, trifarotene appears to modulate retinoid-mediated pathways involved in proteolysis, skin hydration, and cell adhesion - modulation of these additional pathways has not been observed with other retinoids and may therefore be unique to trifarotene.
- Primary indication
- Trifarotene is indicated for the topical treatment of acne vulgaris in patients 9 years of age and older.Curator reviewed · 1 structured indication
- Formula / weight
- C29H33NO4 · 459.586 g/mol (avg)
- First approval
- Canada, 2019 · United States, 2019
- Code names
- CD-5789
- Brand names
- Aklief
Resolves to
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Which drugs share a target with Trifarotene, and which of those have an active Phase 3 trial?