Trifarotene (Topical) (Monograph)
Drug class: Keratolytic Agents
Introduction
Retinoid skin agent.
Uses for Trifarotene (Topical)
Acne vulgaris
Topical treatment of acne vulgaris in patients ≥9 years of age.
Topical retinoids are recommended first-line options for the treatment of acne vulgaris; these agents may be used alone or in combination with other therapies, depending on acne severity.
Trifarotene (Topical) Dosage and Administration
General
Other General Considerations
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Use of a moisturizer is recommended as frequently as needed.
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Minimize unprotected skin exposure to ultraviolet rays (including sunlight and sunlamps) during treatment with trifarotene. If sun exposure cannot be avoided, sunscreen and protective clothing worn over treated areas of skin is recommended.
Administration
Topical Administration
For topical use only; not recommended for oral, ophthlamic, or intravaginal use. Avoid contact with the eye, lips, paranasal creases, and mucous membranes.
Apply to clean, dry skin.
One pump actuation should be enough to cover the face (i.e., forehead, cheeks, nose, chin); 2 pump actuations should be enough to cover the upper trunk (i.e., reachable upper back, shoulders, chest). One additional pump actuation may be used for middle and lower back if needed.
Dosage
Pediatric Patients
Acne Vulgaris
Topical
Pediatric patients ≥9 years of age: apply a thin layer once daily in the evening to affected areas.
Adults
Acne Vulgaris
Topical
Apply a thin layer once daily in the evening to affected areas.
Special Populations
Hepatic Impairment
No specific dosage recommendations; expected systemic absorption minimal.
Renal Impairment
No specific dosage recommendations; expected systemic absorption minimal.
Geriatric Use
No specific dosage recommendations.
Cautions for Trifarotene (Topical)
Contraindications
-
None.
Warnings/Precautions
Skin Irritation
Skin reactions such as erythema, scaling, dryness, and stinging or burning can occur. Most severe reactions often occur within the first 4 weeks of treatment, and decrease in severity with continued use.
Depending on skin reaction severity, instruct patients to use a topical moisturizer concurrently, reduce frequency of application, or suspend use temporarily.
If severe skin reactions persist, discontinue trifarotene.
Avoid applying cream to cuts, abrasions, or eczematous or sunburned areas. Avoid waxing areas treated with trifarotene.
Ultraviolet Light and Environmental Exposure
During treatment, minimize exposure to ultraviolet rays, including sunlight and sunlamps. Exercise caution in patients who are usually exposed to large amounts of sun, or who are sensitive to sun exposure.
Advise patients to wear sunscreen and protective clothing over treated areas when sun exposure cannot be avoided.
Specific Populations
Pregnancy.
A drug-associated risk of major birth defects, miscarriage, or adverse fetal or maternal outcomes not identified with trifarotene cream based on available clinical data in pregnancy.
Lactation.
Unknown if present in breastmilk; effects on the breastfed infant or milk production not known.
Use trifarotene cream on the smallest area of skin and for the shortest duration possible to minimize potential infant exposure. To prevent direct infant exposure, avoid applying trifarotene cream directly to the nipple or areola.
Pediatric Use.
Safety and efficacy established in pediatric patients 9–17 years of age.
Safety and efficacy not established in pediatric patients <9 years of age.
Geriatric Use.
Not studied in patients ≥65 years of age.
Hepatic Impairment.
Not studied in hepatic impairment.
Renal Impairment.
Not studied in renal impairment.
Common Adverse Effects
Most common adverse reactions (≥1%): application site irritation, application site pruritus, sunburn.
Drug Interactions
In vitro, primarily metabolized via CYP2C9, CYP3A4, and CYP2C8; metabolized to a lesser extent by CYP2B6. Not expected to inhibit or induce CYP1A2, CYP2B6, or CYP3A4; not expected to inhibit CYP2C8, CYP2C9, CYP2C19, or CYP2D6.
Not expected to inhibit multidrug and toxin extrusion (MATE) protein, organic anion transporter polypeptide (OATP), organic anion transporter (OAT), organic cation transporter (OCT), breast cancer resistance protein (BCRP), P-glycoprotein (P-gp), bile salt export pump (BSEP), or mannose phosphate receptor (MPR).
Specific Drugs
Drug |
Interaction |
---|---|
Fluconazole |
No effect on trifarotene pharmacokinetics |
Oral hormonal contraceptives |
Plasma concentrations of oral hormonal contraceptives containing ethinyl estradiol and levonorgestrel not expected to be affected by trifarotene |
Trifarotene (Topical) Pharmacokinetics
Absorption
Following topical once daily application of 1.5–2 g trifarotene to various sites (face, shoulders, chest, upper back) for 29 days in 19 adult patients with acne vulgaris, steady state plasma concentrations were attained after 14 days, and were below the limit of quantification in all but 7 patients.
Accumulation not expected with long-term use.
Distribution
Extent
Not known whether trifarotene is distributed into human milk.
Plasma Protein Binding
99.9%.
Elimination
Metabolism
Metabolized by CYP2C9, CYP3A4, CYP2C8, and, to a lesser extent, CYP2B6.
Elimination Route
Primarily excreted in feces.
Half-life
2–9 hours.
Stability
Storage
Topical
Cream
20—25ºC; excursions permitted between 15—30°C.
Actions
-
Retinoic acid receptor (RAR) agonist.
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Stimulates activity at the RAR gamma subtype, which results in modulation of target genes associated with various processes such as cell differentiation and mediation of inflammatory processes.
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Exact mechanism by which trifarotene improves acne not known.
Advice to Patients
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Advise patients to cleanse the area to be treated and pat dry prior to using trifarotene cream. Apply a thin layer of trifarotene cream once daily in the evening to the face, chest, shoulders, or back. Avoid application to the eyes, lips, nasolabial folds, and mucous membranes.
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Advise patients to avoid applying trifarotene to damaged skin (i.e., skin with cuts and abrasions), sunburned skin, or eczematous areas.
-
Inform patients that trifarotene cream can cause skin irritation, including redness, scaling, dryness, stinging, or burning; this is most common during the first 4 weeks of treatment. Advise patients to use a moisturizer when starting treatment to the reduce the risk of skin irritation. Advise patients to inform their healthcare provider if local skin irritation develops, and that trifarotene application frequency may also be reduced or temporarily suspended to reduce skin irritation.
-
Advise patients to minimize exposure to sunlight, including sunlamps and phototherapy devices, during treatment with trifarotene cream. If sun exposure cannot be avoided, wear sunscreen with a sun protection factor (SPF) of 15 or higher and protective apparel to protect areas where trifarotene has been applied.
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Advise patients to avoid concomitant use of other irritating skin products, such as medicated or abrasive soaps and cleansers, drying cleansers or cosmetics, or products with high amounts of alcohol. Waxing skin areas treated with trifarotene should also be avoided.
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Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.
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Advise women to inform their clinician if they are or plan to become pregnant or plan to breast-feed. If breastfeeding during trifarotene treatment, advise patients to use the smallest amount of cream for the shortest possible duration. Trifarotene cream should not be directly applied to the nipple or areola if breastfeeding.
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Inform patients of other important precautionary information.
Additional Information
The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
Routes |
Dosage Forms |
Strengths |
Brand Names |
Manufacturer |
---|---|---|---|---|
Topical |
Cream |
0.005% |
AKLIEF |
Galderma Laboratories |
AHFS DI Essentials™. © Copyright 2025, Selected Revisions May 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
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