Drug intelligence / Profile preview

adapalene

Development stage
Approved
Lead developer
Galderma
Modality
Small Molecules
Administration
Topical
01

Overview

Adapalene is a third-generation topical retinoid used primarily for the treatment of mild to severe acne vulgaris in adolescents and adults. It is a synthetic naphthoic acid derivative with retinoid activity that acts as an agonist at nuclear retinoic acid receptor beta and retinoic acid receptor gamma, which then form complexes with retinoid X receptors (RXRs) to modulate gene transcription. This leads to normalization of keratinocyte differentiation and decreased microcomedone formation. Adapalene also exhibits anti-inflammatory effects by inhibiting lipoxygenase activity and the oxidative metabolism of arachidonic acid into prostaglandins, as well as downregulating toll-like receptor 2 (TLR-2) expression and inhibiting activator protein 1 (AP-1). Its chemical stability allows it to be used alongside benzoyl peroxide without significant degradation. Adapalene is approved for use in patients aged 12 years or older[1][2][3][5][7][8].

Brand names
DifferinEpiduoCabtreoPanoxylTactupumpPlixda
Other names
adapalene
02

Targets

RARB (Retinoic acid receptor beta)RARG (Retinoic acid receptor gamma)FOS (Activator Protein 1)15-LOX (Lysyl Oxidase)TLR2 (Toll-like Receptor 2)

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