Dosing & Uses
Dosage Forms & Strengths
topical cream
- 10mg/g (1%)
Plaque Psoriasis
Apply thin layer to affected areas once daily
Dosing Considerations
Not for oral, ophthalmic, or intravaginal use
Safety and efficacy not established
Adverse Effects
>10%
Folliculitis (20%)
Nasopharyngitis, including nasal congestion, pharyngitis, respiratory tract infection (RTI) viral, rhinorrhea, sinus congestion, upper RTI, and viral upper RTI (11%)
1-10%
Contact dermatitis, including dermatitis, hand dermatitis, and rash (7%)
Headache, including migraine and tension headache (4%)
Pruritus, including application site pruritus, generalized pruritus, and genital pruritus (3%)
Influenza, including influenza-like illness (2%)
Warnings
Contraindications
None
Cautions
Apply medication to skin lesions only, and avoid unaffected areas of skin
Advise patients that medication is for external use only
Pregnancy & Lactation
Pregnancy
Available data in pregnant women are insufficient to evaluate for drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes
Animal data
- In animal reproduction studies, subcutaneous administration of tapinarof to pregnant rats and rabbits during the period of organogenesis resulted in no significant adverse effects at doses 268 and 16 times, respectively, the maximum recommended human dose (MRHD)
Lactation
No data available regarding presence of drug in human milk, effects on breastfed infant, or on milk production; drug was detected in rat offspring following subcutaneous administration to pregnant female rats, which suggest that drug was transferred into milk of lactating rats; when drug is present in animal milk, it is likely that the drug will be present in human milk
Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from therapy or from underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Aryl hydrocarbon receptor (AhR) agonist; efficacy of tapinarof in psoriasis is attributed to its binding and activation of the aryl hydrocarbon receptor (AhR), a ligand-dependent transcription factor, leading to the downregulation of proinflammatory cytokines, including interleukin 17
Absorption
Mean ± SD Cmax at day 29: 0.12 ± 0.15 ng/mL
AUC0-last at Day 29: 0.61 ± 0.65 ng.h/mL
Distribution
Protein-bound: 99% in vitro to human plasma protein
Metabolism
Metabolized in liver through multiple pathways, including oxidation, glucuronidation, and sulfation (in vitro)
Administration
Topical Administration
Apply to skin lesions only, and wash hands after application unless treating hands
Use only externally
Storage
Store at 20-25°C (68-77°F); excursions permitted at 15-30°C (59-86°F)
Do not freeze
Protect from exposure to excessive heat
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
