INTRODUCTION
Psoriasis is a chronic, immune-mediated, multisystem, inflammatory dermatological condition that is persistent and relapsing.1 It affects 3.2% of the American adult population and an estimated 125 million people worldwide. The incidence is estimated to be 80 new cases per 100,000 person-years. The prevalence varies based on geographical region. For example, psoriasis prevalence is 0.5% in certain parts of Asia and as high as 8% in Norway.2-4 The age of disease onset is usually before the age of 40 years. Two peak age ranges of disease onset exist. Most patients are affected between the ages of 18 to 39 years or 50 to 69 years. Various types of psoriasis exist including plaque, guttate, inverse, pustular, erythrodermic, nail, and psoriatic arthritis.5 The clinical presentation of plaque psoriasis involves lesions characterized by sharp margins, erythema, and silvery scales. Psoriasis is associated with medical and psychiatric comorbidities such as autoimmune disease, cardiovascular disease, metabolic syndrome, lymphoma, melanoma, nonmelanoma skin cancer, and depression. The impact of the disease on occupational function and psychosocial morbidity has been described.6 Severity of psoriasis can range from mild to severe disease.
Although there is no cure for the condition, several effective treatment options exist, and management strategies range from nonpharmacologic recommendations, topical drugs, phototherapy, and systemic agents, both biologic and non-biologic agents. Appropriate treatment of psoriasis involves recognition of the condition, patient-specific pharmacotherapy selection based on disease severity, monitoring of the treatment and disease progression, and treatment of comorbidities. Tapinarof (Vtama®), a topical aryl hydrocarbon receptor modulating drug was approved by the US Food and Drug Administration for the treatment of plaque psoriasis in adults in May 2022.7 Tapinarof is the first and only non-steroidal topical drug option in its class for adults with plaque psoriasis.
Although there is no cure for the condition, several effective treatment options exist, and management strategies range from nonpharmacologic recommendations, topical drugs, phototherapy, and systemic agents, both biologic and non-biologic agents. Appropriate treatment of psoriasis involves recognition of the condition, patient-specific pharmacotherapy selection based on disease severity, monitoring of the treatment and disease progression, and treatment of comorbidities. Tapinarof (Vtama®), a topical aryl hydrocarbon receptor modulating drug was approved by the US Food and Drug Administration for the treatment of plaque psoriasis in adults in May 2022.7 Tapinarof is the first and only non-steroidal topical drug option in its class for adults with plaque psoriasis.
MATERIALS AND METHODS
Data Selection
A search of PubMed, MEDLINE, and ClinicalTrials.gov databases was conducted for articles published before January 2023, to identify clinical and preclinical trials evaluating the pharmacokinetics, efficacy, or safety of tapinarof. The following search terms were used: tapinarof, psoriasis, GSK2894512. Relevant articles in English and results from human clinical trials were included. Additional articles were identified by hand from references. Data from the package insert was used to complement information found in cited references.
Chemistry and Pharmacology
Tapinarof (GSK2894512 or WBI-1001) is a non-steroidal, natural product. It is an isopropyl-substituted stilbene metabolite produced by gammaproteobacteria Photorhabdus.8,9
Structurally, tapinarof or 5-dihydroxy-4-isopropyl-trans-stilbene is a small molecular aryl hydrocarbon with a molecular weight of 254.32 g/mol.7 In comparing its structure to other naturally produced stilbenes, it is a derivative of plant-derived polyphenol resveratrol.9 Although similar in structure to resveratrol, the activity of tapinarof is significantly different.
