clascoterone topical

Action and Spectrum

Actions and spectrum: 

clascoterone topical is a medication used for the treatment of acne. It acts as a selective androgen receptor antagonist, which means it blocks the effects of androgens (male hormones) on the skin. This helps reduce the production of sebum, a major contributor to acne development.

clascoterone also has anti-inflammatory properties, which further contribute to its effectiveness in treating acne. The spectrum of clascoterone topical is primarily focused on the management of acne vulgaris, particularly in individuals with moderate to severe forms of the condition. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Pruritus (7.7%) 

Edema (3.6%) 

Skin atrophy (1.6%) 

Stinging/burning (4.2%) 

Striae rubrae (2.5%) 

Telangiectasia (1.2%)  

>10% 

Dryness/scaling (10.5%) 

Redness/Erythema (12.2%)  

Frequency not defined 

Reproductive: amenorrhea, Polycystic ovaries 

Metabolism: Hyperkalemia 

Black Box Warning

Black Box Warning: 

There is no specific black box warning associated with clascoterone topical 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

clascoterone topical is contraindicated in individuals who have a known hypersensitivity or allergy to clascoterone. It is also contraindicated in patients with broken or damaged skin in application. Additionally, there may be specific contraindications based on individual medical conditions.  

Caution: 

• Avoid contact with lips, eyes, and mucous membranes. If accidentally contact occurs, rinse thoroughly with water. 
• Use with caution in individuals with known skin sensitivities or allergies. 
• Exercise caution when applying clascoterone topical on open wounds, cuts, or irritated skin. 
• Inform your healthcare provider about any other topical medications or skincare products you are using to avoid potential interactions. 
• The safety of clascoterone topical in pregnancy and breast-feeding woman are not well-established. 

Comorbidities: 

clascoterone topical is not associated with specific comorbidities, as it targets a specific dermatological condition rather than systemic health conditions. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: N/A  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

clascoterone topical is a synthetic steroidal antiandrogen. It acts as a competitive antagonist of androgen receptors in the skin, inhibiting the binding of dihydrotestosterone (DHT) to these receptors. By blocking androgen receptor activation, clascoterone reduces the stimulation of sebaceous glands, inhibits sebum production, and helps to normalize the hyperkeratinization process in the pilosebaceous unit. This mechanism of action makes clascoterone topical effective in treating acne vulgaris by reducing inflammation, decreasing sebum production, and promoting the resolution of acne lesions.  

Pharmacodynamics: 

The pharmacodynamics of clascoterone topical primarily involves its interaction with androgen receptors in the skin. clascoterone acts as a competitive antagonist, inhibiting the binding of dihydrotestosterone (DHT) to these receptors. By blocking androgen receptor activation, it reduces the effects of androgens on sebaceous gland activity, sebum production, and the hyperkeratinization process in the pilosebaceous unit. 

The inhibition of androgen receptor activation by clascoterone may lead to a decrease in sebum production, which helps to alleviate acne symptoms. It also exhibits anti-inflammatory properties, contributing to the resolution of acne lesions. 

Pharmacokinetics: 

Absorption 

clascoterone is topically applied to the skin as a cream or gel formulation. It is primarily absorbed through the skin and acts locally at the site of application. The absorption rate and extent may vary depending on factors such as skin integrity, formulation, and application technique. 

Distribution 

After absorption, clascoterone remains primarily localized to the site of application on the skin. It does not extensively distribute throughout the body due to its limited systemic absorption. 

Metabolism 

clascoterone undergoes metabolism primarily in the skin. It is metabolized by enzymes in the skin to its active metabolite, 11β-hydroxy-4′-methoxy-3′,5′-dioxospiro[chromane-2,6′-tetrahydroimidazo[2,1-b] thiazole]-4-carboxylic acid (MB-75). 

Elimination and excretion 

The metabolites of clascoterone, including MB-75, are excreted primarily through urine and feces. However, the systemic exposure to clascoterone and its metabolites is minimal due to its topical application, resulting in limited systemic elimination. 

Adminstartion

Administration: 

• Clean the affected skin area: Before applying clascoterone topical, ensure that the affected skin area is clean and dry.  
• Apply a thin layer: Take a small amount of clascoterone topical cream or gel on your fingertip or a clean applicator. Apply to the affected skin area. Massage or rub it gently until it is evenly distributed. 
• Follow the recommended dosage and frequency: The specific dosage and frequency of application will depend on the condition being treated and the formulation strength of clascoterone topical. 
• Wash hands after application: After applying clascoterone topical, wash hands thoroughly to remove any residual medication and prevent unintentional transfer to other areas of the body. 
• Avoid contact with eyes, mouth, and mucous membranes: clascoterone topical is for external use only.  
• Continue regular use: clascoterone topical is typically used daily as prescribed. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: clascoterone topical 

Pronounced: (klas-ko-TER-ohn top-i-kal)  

Why do we use clascoterone topical? 

clascoterone topical is primarily used for the treatment of acne. It is specifically used to treat topical acne vulgaris in patients of 12 years and older. It is also used as a comprehensive acne treatment regimen and can be applied to affected areas of the face, chest, or back. clascoterone topical may be prescribed by healthcare professionals to help in appearance of acne lesions, reduce inflammation, and promote clearer skin.