Supply High Purity 99% White Powder Clascoterone CAS 19608-29-8 For Hair Growth

Clascoterone More Info

Clascoterone, also known as cortexolone 17α-propionate, is a novel topical antiandrogen therapy primarily indicated for the treatment of acne vulgaris. It is the first of its kind to target androgen receptors directly in the skin, providing a localized treatment option with minimal systemic effects.

Mechanism of Action

Clascoterone functions as an androgen receptor antagonist, competing with androgens such as dihydrotestosterone (DHT) for binding to androgen receptors in sebaceous glands and dermal papilla cells. By blocking the effects of DHT, clascoterone reduces the transcription of androgen-responsive genes that promote sebum production and inflammation, key factors in acne pathogenesis . This mechanism allows clascoterone to effectively mitigate the hormonal influences that contribute to acne formation.

Applications

Indicated for the treatment of moderate to severe acne in both males and females. Its unique action on androgen receptors makes it particularly effective for patients whose acne is influenced by hormonal factors.

In addition to its use in acne treatment, clascoterone is also being explored for its potential in treating androgenetic alopecia (AGA), a common form of hair loss.

Routes of Administration

Clascoterone is administered topically as a cream (1% concentration). The recommended application involves applying a thin layer to the affected areas twice daily.

Safety and Side Effects

Clascoterone is generally well tolerated but may cause several side effects:
Common Side Effects:
Localized irritation (itching, burning, redness)
Dry or scaly skin
Darkening of the skin
Mild gastrointestinal symptoms (nausea)
Serious Side Effects:
Hypothalamic-pituitary-adrenal (HPA) axis suppression has been observed in some patients, particularly with prolonged use or application over large areas. Symptoms may include fatigue, loss of appetite, or skin discoloration.
Signs of allergic reactions such as hives or difficulty breathing require immediate medical attention.

Pharmacokinetics

Absorption: Clascoterone is designed for topical application, leading to limited systemic absorption. Upon application, it penetrates the skin effectively, reaching dermal levels while minimizing systemic exposure.
Metabolism: It is rapidly metabolized into cortexolone, an inactive metabolite, primarily through hydrolysis by skin and plasma esterases. Plasma concentrations of cortexolone are typically low following topical application.
Distribution: Clascoterone shows high protein binding (approximately 84% to 89%) in plasma.
Elimination: The exact route of elimination has not been fully characterized; however, it is primarily excreted via the skin after local metabolism.
Half-life: The half-life of clascoterone has not been definitively established but is considered short due to rapid metabolism.

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