Thiamidol: A Breakthrough Innovation in the Treatment of Hyperpigmentation

June 2025 | Volume 24 | Issue 6 | 608 | Copyright © June 2025


Published online May 30, 2025

doi:10.36849/JDD.9093

Cheri Frey MDa, Pearl Grimes MDb, Valerie D. Callender MDc,d, Andrew Alexis MDe, Hilary Baldwin MDf,g, Nada Elbuluk MDh, Patricia Farris MDi, Susan Taylor MDj, Seemal R. Desai MDk,l

aDepartment of Dermatology, Howard University Hospital, Washington DC
bDepartment of Dermatology, David Geffen School of Medicine, University of California - Los Angeles, Los Angeles, CA
cCallender Dermatology and Cosmetic Center, Glenn Dale, MD
dHoward University College of Medicine, Washington, DC
eWeill Cornell Medical College, New York, NY
fThe Acne Treatment and Research Center, Brooklyn, NY
gDepartment of Dermatology, Rutgers Robert Wood Johnson Medical Center, New Brunswick, NJ
hDepartment of Dermatology, Keck School of Medicine, University of Southern California, Los Angeles, CA
iTulane University School of Medicine, New Orleans, LA
jDepartment of Dermatology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA
kDepartment of Dermatology, The University of Texas Southwestern Medical Center, Dallas, TX
lInnovative Dermatology, Plano, TX

Abstract
Cutaneous hyperpigmentation, including melasma, solar lentigines, and post-inflammatory hyperpigmentation (PIH), results in a significant impact on patients’ quality of life. Unfortunately, many currently available over-the-counter (OTC) options have been limited by efficacy, safety, and tolerability concerns. Additionally, limited patient awareness and education on disease manifestation and root causes of hyperpigmentation often leave patients undiagnosed and untreated. Melanogenesis is driven by a complex pathway resulting in the ultimate production and deposition of melanin in the skin. The major rate-limiting step of melanogenesis centers on the conversion of L-Dopa to the final melanin product mediated by a cellular tyrosinase, causing the overproduction of melanin clinically resulting in hyperpigmentation. Recently, isobutylamido thiazolyl resorcinol (Thiamidol) has been identified as the most effective inhibitor of human tyrosinase out of 50,000 compounds screened, and thus, a novel ingredient for inclusion in OTC products to address hyperpigmentation. We describe here the current pre-clinical and clinical safety and efficacy data of Thiamidol formulations aimed at educating the dermatology community on a safe and effective OTC option for use as part of the overall management of hyperpigmentation in patients.

Citation: Frey C, Grimes P, Callender VD, et al. Thiamidol: a breakthrough innovation in the treatment of hyperpigmentation. J Drugs Dermatol. 2025;24(6):608-616. doi:10.36849/JDD.9093

INTRODUCTION

Hyperpigmentation disorders, including melasma, post-inflammatory hyperpigmentation (PIH), dermal macular hyperpigmentation, seborrheic melanosis, hyperpigmentation associated with acanthosis nigricans, and solar lentigines, represent a set of pigmentary disorders that are usually characterized by overstimulation of the melanin production pathway, resulting in the deposition of excess melanin in the skin.1-3 The stimuli of melanin production can include hormonal causes, ultraviolet (UV) radiation, endogenous factors (eg, inflammatory conditions), or exogenous factors (eg, mechanical trauma) in PIH.1,3

Pigmentary disorders, including hyperpigmentation, represent one of the most common dermatologic diagnoses in individuals with skin of color (SOC), particularly individuals with African, Asian, or Hispanic heritage.4,5 In a recent survey of 48,000 individuals in 34 countries from December 2022-2023 responding to an online auto-administered questionnaire, 15% (n=7,126) of responders (56% women, 30% Fitzpatrick Skin Types (FST) IV-VI, mean age = 39 years) reported suffering from PIH.6 For melasma, the prevalence in the general population is approximately 1% but has been reported as high as 50% in high-risk populations and accounts for between 4 to 10% of dermatology diagnoses in Central and South America.3,7 The incidence of solar lentigines increases with age, affecting more than 90% of individuals with FSTs I-II older than 50 years.8

Effective treatment options for hyperpigmentation include agents that reduce melanin synthesis or enhance the dispersion and removal of melanin once formed.9 Prior to the passing of the CARES Act on September 20, 2023, 2% hydroquinone