Clascoterone API - Topical Anti-Androgen for Acne

Product Name: Clascoterone
Product Code: GKT2200306
CAS No.: 19608-29-8
MF: C₂₄H₃₄O₅
EINECS: 685-282-9
Assay (Purity): 99%
Appearance: White powder
Quantity: 1 kg
Packaging: 1 kg/bag (double-layer polyethylene bag + single-layer aluminum foil bag)

Description

Chemical Identity

Clascoterone (USAN) is a synthetic steroidal compound chemically identified as cortexolone 17α-propionate. Its empirical formula is C24H34O5 and its molecular weight is 402.52 g/mol. The CAS registry number is 19608-29-8, and the EINECS number is 685-282-9. In pharmaceutical literature, the compound is also known by the laboratory code CB-03-01.

The substance is a white to off-white crystalline powder. It belongs to the class of corticosteroids, but its pharmacological profile is fundamentally distinct from classical glucocorticoids: the molecule is designed to exert local anti-androgenic activity without systemic glucocorticoid effects at therapeutic concentrations.

Mechanism of Action

Clascoterone is a selective androgen receptor (AR) antagonist. Unlike systemically acting anti-androgens, when applied topically the molecule penetrates the sebaceous glands and competitively binds to androgen receptors in sebocytes, blocking dihydrotestosterone (DHT) binding and preventing downstream androgenic gene activation. The result is reduced sebum production and decreased release of inflammatory mediators, which are considered key drivers of acne pathogenesis.

Following skin penetration, clascoterone is hydrolysed to cortexolone, a physiological component of the endogenous corticosteroid pool and an intermediate in glucocorticoid synthesis. This property ensures metabolic compatibility with natural steroidogenic pathways. Systemic exposure after topical application remains low: in clinical studies, maximum plasma concentrations after application of a 1% cream to extensive areas in adult acne patients were in the low nanogram-per-millilitre range, with steady state achieved within several days.

Technical Specifications of the Commercial Grade

The supplied clascoterone active pharmaceutical ingredient (API) is intended for the manufacture of semi-solid and liquid dermatological dosage forms. The declared purity (active content) is not less than 99%. Appearance: white powder. Key identity parameters to be controlled in the specification include melting point, specific rotation, impurity profile (including cortexolone 21-propionate as the main degradation product and metabolite), residual solvents, and water content.

Solubility: clascoterone is practically insoluble in water, moderately soluble in ethanol and other organic solvents, and freely soluble in dimethyl sulfoxide (DMSO) and dimethylformamide. For laboratory use, stock solutions are prepared in non-aqueous media (methanol, acetonitrile, DMSO) and stored in tightly sealed containers at reduced temperature and protected from light.

Applications

The primary pharmaceutical application of clascoterone is the manufacture of medicinal products for topical therapy of moderate-to-severe acne vulgaris in patients from adolescence onward. Its mechanism of action, targeting androgen-induced sebum production, distinguishes it from conventional approaches (retinoids, antibiotics, benzoyl peroxide) and positions it as a first-in-class topical androgen receptor antagonist for dermatology.

Additionally, clascoterone is being investigated in the context of androgenetic alopecia, where androgen-dependent miniaturisation of hair follicles is a key mechanism. However, this dermatological API is supplied primarily for the development and manufacture of acne treatments.

Packaging, Logistics, and Supply Conditions

The product is supplied in 1 kg packaging. The primary container is a double-layer polyethylene bag placed inside a single-layer aluminium foil bag. This configuration provides a barrier against moisture, oxygen, and light - critical factors in the degradation of steroidal APIs. During transport and storage, the powder should be kept in a tightly sealed container in a cool, dry, well-ventilated area, away from direct sunlight and ignition sources.

For long-term storage of the powder form, a temperature of -20°C (shelf life up to 3 years) or 2-8°C (shelf life up to 2 years) is recommended. Transport is carried out under temperature-controlled conditions in compliance with pharmaceutical substance handling requirements. Supplies originate from regions with established fine organic synthesis capabilities; the largest steroidal API production capacities are concentrated in China, with production also developing in India and other Asian countries.

Handling Safety

Clascoterone is a substance requiring standard precautions when handling pharmaceutical APIs. Safety data sheets specify avoiding contact with skin and eyes and avoiding inhalation of dust and aerosols; work should be performed in a well-ventilated area or in a chemical fume hood. Personal protective equipment includes protective gloves, safety goggles with side shields, a laboratory coat or impervious clothing, and a respirator where there is a risk of dust formation.

The substance is classified as harmful if swallowed. There are indications of potential to cause genetic defects (restricted handling category), requiring special instructions before use and handling as a restricted product. In case of skin or eye contact, rinse thoroughly with water; on inhalation, move the affected person to fresh air; on ingestion, do not induce vomiting and seek medical attention.

Given its mechanism of action (androgen receptor inhibition), the substance may cause fetal harm under systemic exposure, so handling requires particular caution for pregnant women and women of reproductive potential.

Market Context and Positioning

Clascoterone is a relatively new molecule in the dermatological API market. The emergence of the first topical androgen receptor antagonist approved by regulatory authorities for acne therapy has opened a distinct segment in pharmaceutical development - products targeting the hormonal component of acne pathogenesis without systemic absorption and its associated adverse effects.

For finished dosage form manufacturers, sourcing validated clascoterone API is the entry step into developing products in this class. Demand for the substance comes from companies specialising in dermatology that plan to launch topical formulations for acne and androgenetic alopecia. Key criteria for supplier selection are confirmed purity (≥99%), a full impurity profile, GMP compliance for pharmaceutical ingredients, and supply chain stability.