Tapinarof for psoriasis and atopic dermatitis: 15 years of clinical research

Abstract

Tapinarof is a topical, aryl‐hydrocarbon receptor agonist that has recently received FDA‐approval for the treatment of psoriasis. This novel therapeutic has also been shown to be effective for atopic dermatitis and is currently in phase 3 for this indication. Beyond good efficacy and fast onset of action in patients with psoriasis, the clinical response to tapinarof is notable for durable remission or near remission, maintained for an average of 130 days beyond treatment discontinuation in patients with psoriasis in phase 3 studies. Tapinarof is usually well tolerated but can induce a follicular inflammatory reaction and dermatitis in some patients. This narrative review covers the historical development of this molecule, safety and efficacy data from clinical trials conducted with various topical formulations, and practical considerations derived from our 15 years of clinical trial experience with the drug.

An update on topical therapies for psoriasis

“…Tapinarof is a novel small molecule, the first in its class, which binds and activates AhR, leading to the downregulation of pro-inflammatory cytokines [20]. It is available as a topical preparation in the form of 1% cream and is licensed by the US FDA for treatment of plaque psoriasis [24 ▪▪ ]. Tapinarof cream was licensed following results of two phase III randomized, placebo-controlled clinical trials of identical design in adult populations.…”

Anti-inflammatory and biologic drugs for atopic dermatitis: a therapeutic approach in children and adolescents

“…Tapinarof (Table 1) is approved for plaque psoriasis. Tapinarof cream 1% twice daily has shown promise in adults with AD, with folliculitis being the most common adverse event (179)(180)(181). Phase III trials are currently underway in both adult and pediatric populations.…”

Aryl‐hydrocarbon receptor agonist: A novel topical therapeutic approach for inflammatory skin diseases

“…Furthermore, the AhR complex modulates the T-helper 17/22 and T regulatory axis, and some AHR ligands also exert a role in the neutralization of oxidative stress through the activation of the nuclear factor-erythroid 2-related factor-2 (NRF2) transcription factor and a ROS-scavenging structure. 3 Bissonnette et al 4 present a review article on tapinarof (3,5-dihydroxy-4-isopropylstilbene), an AhR agonist from a historical perspective. His group has been working with this component since 2007, and the initial studies focused on psoriasis.…”

“…Bissonnette et al 4 present a review article on tapinarof (3,5‐dihydroxy‐4‐isopropylstilbene), an AhR agonist from a historical perspective. His group has been working with this component since 2007, and the initial studies focused on psoriasis 5 .…”

“…Tapinarof 1% cream is a topical medication applied once daily, and the review shows the main outcomes of its use in clinical trials in patients with psoriasis and AD. The key point of this review indicates the profile of tapinarof in psoriasis and AD, as follows 4 :…”