Unveiling the potential of the aryl hydrocarbon receptor

Brought to you by Dermavant

Take a closer look at the novel science behind VTAMA® (tapinarof) cream, 1%'s effects on the skin through its unique interaction with the aryl hydrocarbon receptor.

The aryl hydrocarbon receptor (AhR) is a ligand-dependent transcription factor that plays various multi-functional roles in the body. It is particularly abundant in barrier tissues like the skin. AhR signaling is crucial for maintaining skin homeostasis, as it helps balance the immune response, preserve skin barrier function, and promote antioxidant activity.1 These processes are often disrupted in conditions like plaque psoriasis and atopic dermatitis. VTAMA cream is not FDA-approved for use in atopic dermatitis.

Tapinarof is an innovative topical cream that serves as a targeted therapeutic agent by acting as an AhR agonist. It binds selectively to AhR and activates it, although the specific mechanisms by which tapinarof exerts its therapeutic effects remain unknown. In a mouse model of psoriasis, tapinarof was found to down regulate IL-17 expression in skin, and reduce IL-17A and IL-17F cytokine production from T cells, and decrease psoriatic skin inflammation.2,3 Oxidative stress is known to cause damage to cellular structures and contribute to dermal inflammation.6 Tapinarof was shown to decrease oxidative stress by activating the antioxidant Nrf2 pathway and by directly reducing the levels of reactive oxygen species, as demonstrated in an ex vivo human skin study.1-4 Tapinarof also promotes skin barrier normalization by inducing expression of the skin barrier genes filaggrin, loricrin, and involucrin, which are down regulated in plaque psoriasis.1-4 Click on the video to watch how activation of AhR signaling by tapinarof inhibits pro-inflammatory cytokines, reduces oxidative stress, and restores skin homeostasis in plaque psoriasis.

IMPORTANT SAFETY INFORMATION 

Indication: VTAMA® (tapinarof) cream, 1% is an aryl hydrocarbon receptor agonist indicated for the topical treatment of plaque psoriasis in adults. Adverse Events: The most common adverse reactions (incidence ≥ 1%) in subjects treated with VTAMA cream were folliculitis (red raised bumps around the hair pores), nasopharyngitis (pain or swelling in the nose and throat), contact dermatitis (skin rash or irritation, including itching and redness, peeling, burning, or stinging), headache, pruritus (itching), and influenza (flu). 

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch or call 1-800-FDA-1088.

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. Bissonnette R, et al. J Am Acad Dermatol. 2021;84:1059–1067
  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. 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.
  5. Furue M, Hashimoto-Hachiya A, Tsuji G. Aryl Hydrocarbon Receptor in Atopic Dermatitis and Psoriasis. Int J Mol Sci. 2019;20(21):5424. Published 2019 Oct 31.
  6. Cannavò SP, Riso G, Casciaro M, Di Salvo E, Gangemi S. Oxidative stress involvement in psoriasis: a systematic review. Free Radic Res. 2019;53(8):829-840.

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