VTAMA is the first and only aryl hydrocarbon receptor (AhR) agonist indicated for the treatment of atopic dermatitis

The role of AhR agonism

Activation of the AhR has been shown to support normalization of skin barrier function. AhR is highly expressed in epithelial and immune cells of barrier tissues, including the skin, gastrointestinal tract, and lungs. AhR activation can promote the following1-3:

scales

A balanced immune response by reducing proinflammatory cytokines.3-5

barrier

Skin barrier restoration through increased expression of genes that encode skin barrier proteins, such as filaggrin, and genes involved in ceramide production.2-4,6

cells

Tapinarof activates AhR
which regulates pathways involved in atopic dermatitis4

In preclinical studies, tapinarof was shown to decrease proinflammatory cytokines and increase expression of genes that encode skin barrier proteins, such as filaggrin, and genes that are involved in lipid production, such as ceramides. This may lead to an anti-inflammatory effect and potential skin barrier restoration.2-4,6-9

The specific mechanisms by which VTAMA exerts its therapeutic actions are unknown.

cell
scales

Anti-inflammatory activity
Through reduction of inflammatory Th2 cytokines involved in atopic dermatitis (as demonstrated in mouse models and in vitro)4,8,9

barrier

Potential skin barrier restoration
Through increased expression of genes that encode skin barrier proteins and genes that are involved in lipid production (as demonstrated in vitro)3,4,6,7

Th, T helper.

Once-Daily Dosing

See more info on VTAMA dosing

Visible Results

See photos of clinical trial patients with atopic dermatitis

INDICATION: VTAMA® (tapinarof) cream, 1% is an aryl hydrocarbon receptor (AhR) agonist indicated for the topical treatment of atopic dermatitis in adults and pediatric patients 2 years of age and older.

SELECTED SAFETY INFORMATION

Adverse Events: In atopic dermatitis, the most common adverse reactions (incidence ≥1%) were: upper respiratory tract infection, folliculitis, lower respiratory tract infection, headache, asthma, vomiting, ear infection, pain in extremity, and abdominal pain.

INDICATION: VTAMA® (tapinarof) cream, 1% is an aryl hydrocarbon receptor (AhR) agonist indicated for the topical treatment of atopic dermatitis in adults and pediatric patients 2 years of age and older.

SELECTED SAFETY INFORMATION

Adverse Events: In atopic dermatitis, the most common adverse reactions (incidence ≥1%) were: upper respiratory tract infection, folliculitis, lower respiratory tract infection, headache, asthma, vomiting, ear infection, pain in extremity, and abdominal pain.

Before prescribing VTAMA cream, please read the Prescribing Information.

References: 1. Esser C, Rannug A. The aryl hydrocarbon receptor in barrier organ physiology, immunology, and toxicology. Pharmacol Rev. 2015;67(2):259-279. 2. Furue M, Tsuji G, Mitoma C, et al. Gene regulation of filaggrin and other skin barrier proteins via aryl hydrocarbon receptor. J Dermatol Sci. 2015;80(2):83-88. 3. Smith SH, Jayawickreme C, Rickard DJ, et al. Tapinarof is a natural AhR agonist that resolves skin inflammation in mice and humans. J Invest Dermatol. 2017;137(10):2110-2119. 4. Silverberg JI, Boguniewicz M, Quintana FJ, et al. Tapinarof validates the aryl hydrocarbon receptor as a therapeutic target: a clinical review. J Allergy Clin Immunol. 2024;154(1):1-10. 5. Tsuji G, Takahara M, Uchi H, et al. Identification of ketoconazole as an AhR-Nrf2 activator in cultured human keratinocytes: the basis of its anti-inflammatory effect. J Invest Dermatol. 2012;132(1):59-68. 6. Sutter CH, Azim S, Wang A, et al. Ligand activation of the aryl hydrocarbon receptor upregulates epidermal uridine diphosphate glucose ceramide glucosyltransferase and glucosylceramides. J Invest Dermatol. 2023;143(10):1964-1972.e4. 7. Silverberg JI, Eichenfield LF, Hebert AA, et al. Tapinarof cream 1% once daily: significant efficacy in the treatment of moderate to severe atopic dermatitis in adults and children down to 2 years of age in the pivotal phase 3 ADORING trials. J Am Acad Dermatol. 2024;91(3):457-465. 8. Organon DOF. DMVT-505-AD Mouse Model. 2016. 9. Organon DOF. DMVT-505-Th2 Polarization. 2015.

Back to top