Trifarotene (Topical) (Monograph)

Drug class: Skin and Mucous Membrane Agents, Miscellaneous

Medically reviewed by Drugs.com on Nov 21, 2023. Written by ASHP.

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

• Use of a moisturizer is recommended as frequently as needed.

• 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

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.

• 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.

• Exact mechanism by which trifarotene improves acne not known.

Advice to Patients

• 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.

• 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.

• 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.

• 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.

• 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.

• 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.

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