Tapinarof is a therapeutic aryl hydrocarbon receptor-modulating agent (TAMA) indicated for the treatment of adult psoriasis.
Brand Name Vtama
Tapinarof is a small-molecule AhR agonist that is indicated for the treatment of adult psoriasis.
It is available as a topical cream to be applied to the affected area once daily.
The pharmacodynamics of tapinarof are unknown.
It is a therapeutic aryl hydrocarbon receptor-modulating agent (TAMA) that binds to and activates the aryl hydrocarbon receptor (AhR).
AhR is a ligand-dependent transcription factor that regulates gene expression in macrophages, T-cells, antigen-presenting cells, fibroblasts, and keratinocytes.
Upon binding to its ligand, AhR forms a complex with a high affinity for DNA binding.
Dysregulation of AhR is one of the hallmarks of psoriasis, as psoriasis patients have a higher serum concentration of AhR compared to healthy individuals.
AhR activation causes the expansion and differentiation of Th17 and Th22, two major T cells responsible for releasing inflammatory cytokines IL-17 and IL-22.
AhR activation also recruits persistent skin resident memory T cells, thus contributing to the chronicity of psoriasis.
The specific binding of tapinarof to AhR modulates genes that are dysregulated in psoriasis.
Tapinarof also induces barrier protein expression, such as filaggrin, hornerin, and involucrin, and restores the skin barrier and epidermal function and decrease oxidative stress.
The anti-inflammatory effect of tapinarof as an AhR agonist might be due to Nrf2.
There is no accumulation with repeat topical application.