- Guide to PHARMACOLOGY
Synonyms: GSK-2894512 | GSK2894512  | Vtama® | WB-1001 | WBI 1001 | WBI-1001
tapinarof is an approved drug (FDA (2022))
Compound class: Synthetic organic
Comment: Tapinarof (GSK2894512) is an aryl hydrocarbon receptor (AhR) agonist . It is a naturally occurring polyphenol derived from bacteria that exist symbiotically with entomopathogenic nematodes. AhR was identified as the primary molecular target based on phenotypic screening using the DiscoveRx BioMAP Diversity Plus System and confirmed using AhR knockout mice. Tapinarof was the first steroid-free topical drug in this class to be approved as a plaque psoriasis medication.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Bissonnette R, Bolduc C, Maari C, Nigen S, Webster JM, Tang L, Lyle M. (2012)
Efficacy and safety of topical WBI-1001 in patients with mild to moderate psoriasis: results from a randomized double-blind placebo-controlled, phase II trial.
J Eur Acad Dermatol Venereol, 26 (12): 1516-21. [PMID:22077962]
2. Lebwohl MG, Stein Gold L, Strober B, Papp KA, Armstrong AW, Bagel J, Kircik L, Ehst B, Hong HC, Soung J et al.. (2021)
Phase 3 Trials of Tapinarof Cream for Plaque Psoriasis.
N Engl J Med, 385 (24): 2219-2229. [PMID:34879448]
3. Smith SH, Jayawickreme C, Rickard DJ, Nicodeme E, Bui T, Simmons C, Coquery CM, Neil J, Pryor WM, Mayhew D et al.. (2017)
Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans.
J Invest Dermatol, 137 (10): 2110-2119. [PMID:28595996]