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Tapinarof: Drug information

Tapinarof: Drug information
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For additional information see "Tapinarof: Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: US
  • Vtama
Pharmacologic Category
  • Aryl Hydrocarbon Receptor Agonist
Dosing: Adult
Atopic dermatitis

Atopic dermatitis: Topical: Apply a thin layer to the affected area once daily.

Plaque psoriasis

Plaque psoriasis: Topical: Apply a thin layer to the affected area once daily; the treatment period in clinical trials was up to 12 weeks (Ref).

Dosing: Kidney Impairment: Adult

The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.

Altered kidney function: Topical: No dosage adjustment necessary for any degree of kidney dysfunction (minimal systemic absorption (Ref)) (Ref).

Hemodialysis, intermittent (thrice weekly): Topical: No supplemental dose or dosage adjustment necessary (minimal systemic absorption (Ref)) (Ref).

Peritoneal dialysis: Topical: No dosage adjustment necessary (minimal systemic absorption (Ref)) (Ref).

CRRT: Topical: No dosage adjustment necessary (Ref).

PIRRT (eg, sustained, low-efficiency diafiltration): Topical: No dosage adjustment necessary (Ref).

Dosing: Liver Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults, unless otherwise noted.

>10%:

Dermatologic: Folliculitis (children, adolescents, adults: 9% to 20%)

Respiratory: Nasopharyngitis (11%), upper respiratory tract infection (children, adolescents, adults: 12%)

1% to 10%:

Dermatologic: Contact dermatitis (7%), pruritus (3%)

Gastrointestinal: Abdominal pain (children, adolescents, adults: 1%), vomiting (children, adolescents, adults: 2%)

Infection: Influenza (2%)

Local: Application-site reaction (children, adolescents, adults: 4%)

Nervous system: Headache (children, adolescents, adults: 4%)

Neuromuscular & skeletal: Limb pain (children, adolescents, adults: 2%)

Otic: Ear disease (children: 2%; including otitis externa, otitis media)

Respiratory: Asthma (children, adolescents, adults: 2%), lower respiratory tract infection (children, adolescents, adults: 5%)

<1%: Dermatologic: Urticaria

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Cream, External:

Vtama: 1% (60 g) [contains benzoic acid, edetate (edta) disodium, polysorbate 80, propylene glycol]

Generic Equivalent Available: US

No

Pricing: US

Cream (Vtama External)

1% (per gram): $30.20

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Topical: For topical use only; not for oral, ophthalmic, or intravaginal use. Apply as a thin layer to the affected area. Wash hands after use (unless used for treatment of the hands).

Use: Labeled Indications

Atopic dermatitis: Treatment of atopic dermatitis in adults and pediatric patients ≥2 years of age.

Plaque psoriasis: Treatment of plaque psoriasis in adults.

Metabolism/Transport Effects

None known.

Drug Interactions

There are no known significant interactions.

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies following SUBQ administration.

Breastfeeding Considerations

It is not known if tapinarof is present in breast milk following topical administration.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.

Mechanism of Action

Binds to and activates the aryl hydrocarbon receptor (AhR), a ligand-dependent transcription factor that regulates cytokine and skin-barrier-protein expression and antioxidant activity (Lebwohl 2021). The specific mechanism of action is not known (manufacturer's labeling).

Pharmacokinetics (Adult Data Unless Noted)

Absorption: Minimally absorbed; serum concentrations range from undetectable to 0.9 ± 1.4 ng/mL on day 1 and 0.12 ± 0.15 ng/mL on day 29 (Jett 2022).

Protein binding: 99% (in vitro).

Metabolism: Hepatic, via multiple pathways (oxidation, glucuronidation, and sulfation) in vitro.

  1. Expert opinion. Senior Renal Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
  2. Jett JE, McLaughlin M, Lee MS, et al. Tapinarof cream 1% for extensive plaque psoriasis: a maximal use trial on safety, tolerability, and pharmacokinetics. Am J Clin Dermatol. 2022;23(1):83-91. doi:10.1007/s40257-021-00641-4 [PubMed 34713415]
  3. Lebwohl MG, Stein Gold L, Strober B, et al. Phase 3 trials of tapinarof cream for plaque psoriasis. N Engl J Med. 2021;385(24):2219-2229. doi:10.1056/NEJMoa2103629 [PubMed 34879448]
  4. Vtama (tapinarof) [prescribing information]. Long Beach, CA: Dermavant Sciences Inc; December 2024.
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