“One of the knocks on crisaborole is that while it has a useful place in our non-steroidal armamentarium, the separation between the medication and the vehicle isn’t that great, whereas with tapinarof you’re seeing a much larger delta between the active ingredient and the placebo control vehicle.”
In an early eczema trial, tapinarof achieved investigator global assessment (IGA) reductions of 43% and 56% in treated patients, vs. 15% for placebo.1
An aryl hydrocarbon agonist, tapinarof inhibits many proinflammatory mediators associated with cutaneous infl ammation, including interferon gamma, TNF-alpha, interleukin (IL)-6 and IL-17.1 Additionally, tapinarof has been shown to enhance skin barrier function, which is a helpful feature in AD.2
“It is an intriguing molecule,” Dr. Han says. “If you look closely at the atopic dermatitis trials, the vast majority of patients who responded to treatment remained clear one month later. There are many reasons to believe that tapinarof will be helpful in more than one infl ammatory skin condition due to its broad eff ect on pro-inflammatory cytokines.”
In phase 2 psoriasis trials, 53% of tapinarof-treated patients achieved IGA 0/1 (with a two-point improvement from baseline) at week 12, versus 24% for placebo.3 Treatment-emergent adverse events aff ected 56% of the tapinarof group, versus 41%
for placebo. Most adverse events were mild.
“Those are the best numbers we’ve seen for any nonsteroidal treatment so far,” says Dr. Han.
Dr. Han has been an advisor for Intraderm, Janssen, UCB and Eli Lilly; an investigator for MC2 Therapeutics; a speaker for Sun Pharma; an investigator and speaker for Pfizer; and an advisor and speaker for Sanofi Regeneron.
George Han MD. “New and Upcoming Topicals in Psoriasis and Atopic Dermatitis,” Atlantic Dermatological Conference. May 5, 2019. New York.
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2. 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;137:2110-2119.
3. Peppers J, Paller AS, Maeda-Chubachi T, et al. A phase 2, randomized dose-finding study of tapinarof (GSK2894512 cream) for the treatment of atopic dermatitis. J Am Acad Dermatol. 2019;80:89-98.e3.
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