AT A GLANCE

A series of early phase clinical trials evaluated clascoterone cream 1%, revealing low systemic exposure, minimal irritation, and a favorable safety profile in both healthy participants and patients with acne vulgaris.

In a comprehensive set of five phase 1 studies, researchers investigated the pharmacokinetics, safety, and local tolerability of clascoterone cream 1%, an androgen receptor inhibitor designed for the topical management of acne vulgaris. Across these trials, systemic absorption of clascoterone was minimal even after repeated daily applications of up to six weeks, with urinary excretion limited to less than 1% of the applied dose. The findings confirm that topical delivery of this molecule effectively confines its activity to the skin, mitigating concerns over systemic hormonal effects.

Safety assessments across more than 300 participants demonstrated that adverse events were infrequent, mild to moderate, and reversible. No clinically meaningful laboratory or vital sign abnormalities were observed. Importantly, both irritation and sensitization potential were minimal—an essential consideration for chronic topical therapies targeting the sebaceous unit. Together, these early-phase results provided the pharmacological foundation for the later pivotal studies that led to clascoterone’s regulatory approval as a novel, first-in-class topical antiandrogen for acne management.

Reference: Di Stefano AFD, Radicioni MM, Garhöfer G, et al. Pharmacokinetics, Safety, and Skin Irritation and Sensitization Potential of Clascoterone Cream in Early-Phase Clinical Study Participants. Clin Pharmacol Drug Dev. 2025 Oct;14(10):742-753. doi: 10.1002/cpdd.1561. Epub 2025 Jun 24. PMID: 40552433; PMCID: PMC12486194.

DRUG AT A GLANCE

WINLEVI^® (clascoterone) cream 1% is a first-in-class topical androgen receptor inhibitor developed by Cassiopea (a subsidiary of Cosmo Pharmaceuticals) for the treatment of acne vulgaris in patients aged 12 years and older. Unlike systemic antiandrogens, WINLEVI^® acts locally within the skin to reduce sebum production and inflammation without affecting systemic hormone levels. Clinical trials have shown low systemic absorption, favorable tolerability, and minimal irritation, establishing it as a safe and innovative alternative to traditional acne therapies.