Tapinarof

What is tapinarof?

Tapinarof is a topical aryl hydrocarbon receptor (AHR) agonist indicated for adults with plaque psoriasis.

Tapinarof (VTAMA®) is a once-daily novel topical agent for patients with mild, moderate, and severe plaque psoriasis, first approved by the US Food and Drug Administration (FDA) in May 2022. Phase II trials have indicated tapinarof is likely also effective for atopic dermatitis.

Chronic plaque psoriasis; topical treatment options would include tapinarof cream  

More images of chronic plaque psoriasis

What is tapinarof used for?

• Plaque psoriasis
• Under investigation: atopic dermatitis

How does tapinarof work?

Tapinarof is a topical aryl hydrocarbon receptor (AHR) agonist. It binds and activates AHRs (a ligand-dependent transcription factor). This promotes:

• Downregulation of T helper type 17 cytokines (eg, IL-17A, IL-17F) thereby inhibiting the inflammatory pathways involved in plaque psoriasis and atopic dermatitis
• Expression of proteins filaggrin and loricrin, aiding in skin barrier restoration
• Interaction with the nuclear factor erythroid-2-related factor 2 (NRF2) transcription factor pathway, which results in reduced oxidative stress.

What are the contraindications to tapinarof?

Apart from hypersensitivity, there are no known contraindications.

Administration

Tapinarof 1% cream:

• Should be applied in a thin layer to affected areas of skin once daily
• Can be used for all grades of disease severity
• Is not intended for oral, ophthalmic, or intravaginal use.

What are the benefits of tapinarof?

Tapinarof has demonstrated a reduction in the severity of mild, moderate, and severe plaque psoriasis in comparison to a control cream. During extended clinical trials, a significant proportion (~40%) of participants achieved disease clearance at least once compared to those receiving control cream (6%). With continued use, tapinarof can induce a prolonged remitting effective therapy (with a mean duration of 4 months remittance in extended trials).

Tapinarof has no known restriction on duration of treatment or extent of area treated; it exhibits low systemic absorption even in maximal use. It causes little to no irritation when used in sensitive skin areas and has overall been well tolerated in extended clinical trials.

Tapinarof provides an opportunity for steroid-sparing therapy for patients with plaque psoriasis.

What are the disadvantages of tapinarof?

Tapinarof has not yet been compared against pre-existing psoriasis treatments.

As it is newly approved, information on the risks of tapinarof are limited to pre-market clinical trials.

What are the side-effects and risks of tapinarof?

Most adverse events reported during clinical trials of tapinarof were mild or moderate.

Reported side-effects (with incidence) of tapinarof include:

• Folliculitis (~20%) — typically mild and self-limiting
• Nasopharyngitis (~10%)
• Contact dermatitis (~5%)
• Headache (<5%)
• Pruritus (<5%)
• Influenza (<5%).

Uncommon side-effects (<1%) included urticaria and drug eruptions.

Use in special populations

Pregnancy and breastfeeding

Tapinarof was not associated with adverse effects during pregnancy in animal reproduction studies. There is currently insufficient data to establish risks in human pregnancy.

It is unknown whether tapinarof is expressed in human breast milk.

Children

Tapinarof is under investigation for paediatric patients (aged 2–17) with plaque psoriasis.

Elderly

No differences in safety or efficacy were observed in patients >65 years in PSOARING 1 and PSOARING 2 trials.

Hepatic and renal impairment

No dose adjustments are suggested in hepatic or renal impairment.

Images of chronic plaque psoriasis

Approved datasheets are the official source of information for medicines, including approved uses, doses, and safety information. Check the individual datasheet in your country for information about medicines.

We suggest you refer to your national drug approval agency such as the Australian Therapeutic Goods Administration (TGA), US Food and Drug Administration (FDA), UK Medicines and Healthcare products regulatory agency (MHRA) / emc, and NZ Medsafe, or a national or state-approved formulary eg, the New Zealand Formulary (NZF) and New Zealand Formulary for Children (NZFC) and the British National Formulary (BNF) and British National Formulary for Children (BNFC).