|Trade names||Differin, Pimpal, Gallet, Adelene, Adeferin|
|Chemical and physical data|
|Molar mass||412.52 g/mol|
|3D model (JSmol)|
Adapalene is a third-generation topical retinoid primarily used in the treatment of mild-moderate acne, and is also used off-label to treat keratosis pilaris as well as other skin conditions. It is effective against acne conditions where comedones are predominant.
It is used for the treatment of acne.
Adapalene has the unique ability to inhibit keratinocyte differentiation and decrease keratin deposition. This property makes adapalene an effective treatment for keratosis pilaris and callus. It may be used by men undergoing foreskin restoration to reduce excess keratin that forms a layer on the exterior of the human penis after circumcision.
It is common (between 1% and 10% of users) to experience a brief sensation of warmth or stinging, as well as skin redness and dryness during the first 2–4 weeks of using the medication. These effects generally decrease over time. Any serious allergic reaction is rare.
This use has not been well studied. Thus far, there is no evidence that the cream causes problems in the baby if used during pregnancy. Use is at the consumer’s own risk.
Adapalene has been shown to enhance the efficacy of topical clindamycin, although adverse effects are also increased. Application of adapalene gel to the skin 3–5 minutes before application of clindamycin enhances penetration of clindamycin into the skin, which may enhance the overall efficacy of the treatment as compared to clindamycin alone.
Absorption of adapalene through the skin is low. A study with six acne patients treated once daily for five days with two grams of adapalene cream applied to 1000 cm² of skin found no quantifiable amounts, or less than 0.35 ng/mL of the drug, in the patients' blood plasma.
Unlike tretinoin, adapalene inhibits keratinocyte differentiation. This inhibition of keratinocyte differentiation and proliferation is responsible for adapalene’s comedolytic effect. It has both exfoliating and anti-inflammatory effects. In an in vivo study, adapalene’s ability to reduce comedo formation was demonstrated by a 50–60% reduction in comedo counts compared with vehicle.
Adapalene selectively targets retinoic acid receptor beta and retinoic acid receptor gamma when applied to epithelial cells such as those that constitute skin. Its agonism of the gamma subtype is largely responsible for adapalene's observed effects. In fact, when adapalene is applied in conjunction with a retinoic acid receptor gamma antagonist, adapalene loses clinical efficacy.
In the United States, adapalene is available under the brand name Differin in three preparations: 0.1% cream, 0.1% gel, and 0.3% gel. The 0.1% gel is available as a generic made by Teva. It is also available combined with benzoyl peroxide under the brand name Epiduo. In Europe, only the 0.1% cream and 0.1% gel are available. Adapalene is currently marketed by Galderma under the trade names Differin in some countries, and Adaferin in India. It is mostly available in 0.1% w/w gel form.
As of July 8, 2016, Galderma received approval from the U.S. Food and Drug Administration (FDA) for Differin Gel (adapalene gel 0.1%) as an over-the-counter (OTC) treatment for acne.
The Proactiv Company also sells the adapalene gel 0.1% under its brand name Proactiv MD Adapalene 0.1%.
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