Trifarotene

Registered South African indications:

• Cutaneous treatment of moderate acne vulgaris of the face and/or the trunk, when many comedones, papules and pustules are present

Registered contraindications in South Africa & other jurisdictions

• Hypersensitivity to the active ingredient or any of its excipients
• Pregnancy
• Women planning a pregnancy

Recommendations in South Africa & other jurisdictions

Caution in the following patient groups

• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly

Skin effects

• Erythema, scaling, dryness, and stinging/burning may occur with trifarotene cream use
• To mitigate these effects, patients should use a moisturiser from the start of treatment
• If necessary, the frequency of application should be reduced, or use should be temporarily suspended
• If severe reactions persist, discontinuation of treatment may be required

Application precautions

• Trifarotene should not be applied to cuts, abrasions, eczematous, or sunburned skin
• Waxing as a depilatory method should be avoided on skin treated with trifarotene
• If a reaction suggesting sensitivity to any component of trifarotene occurs, treatment should be discontinued
• Caution is advised when using cosmetics or acne treatments with desquamative, irritant, or drying effects, as they may exacerbate irritation

Eye and mucous membrane contact

• Trifarotene should not come into contact with the eyes, eyelids, lips, or mucous membranes
• If accidental contact occurs, rinse immediately and thoroughly with lukewarm water

Sun exposure

• Excessive exposure to sunlight, including sunlamps or phototherapy, should be avoided during treatment
• If sun exposure cannot be avoided, a broad-spectrum, water-resistant sunscreen with an SPF of 30 or higher and protective clothing should be used

Excipient precautions

• Trifarotene cream contains propylene glycol (E1520), which may cause skin irritation
• Trifarotene also contains 50mg alcohol (ethanol) per gram (equivalent to 5% w/w), which may cause a burning sensation on damaged skin

Ability to drive and use machines

• Trifarotene has no or negligible influence on the ability to drive and use machines

Forms avail. in SA and covered in this monograph: cre

South African registered indications and dosages

Cutaneous treatment of moderate acne vulgaris of the face and/or the trunk, when many comedones, papules and pustules are present

• Topical (cre): Apply a thin layer to the affected areas of the face and/or trunk once a day, in the evening, on clean and dry skin; Treatment duration: Assess the continued improvement of the patient after 3 months of treatment

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Patients should be instructed to avoid contact with the eyes, eyelids, lips and mucous membranes and to wash their hands after applying trifarotene

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The use of a moisturiser is recommended as needed from the initiation of treatment, while allowing sufficient time before and after the application of trifarotene cream to allow the skin to dry

 

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Method of administration: See additional prescribing points

Forms avail. in SA and covered in this monograph: cre

South African registered indications and dosages

Cutaneous treatment of moderate acne vulgaris of the face and/or the trunk, when many comedones, papules and pustules are present

Younger than 12 years

• Not established for use

12 years and older

• See adult dosage

Pregnancy

Recommendations below are applicable to South Africa and other jurisdictions

• Contraindicated
• Trifarotene is contraindicated during pregnancy or in women planning a pregnancy
• Studies in animals with trifarotene by the oral route have shown reproductive toxicity at high systemic exposure
• If trifarotene is used during pregnancy, or if the patient becomes pregnant while taking trifarotene, treatment should be discontinued

Breastfeeding

Recommendations below are applicable to South Africa and other jurisdictions

• Caution; not recommended
• It is unknown whether trifarotene or its metabolites are excreted in human milk
• Available pharmacodynamic/toxicological data in animals have shown excretion of trifarotene/metabolites in milk. A risk to the suckling child cannot be excluded
• Use of trifarotene during breastfeeding is not recommended
• To avoid the risk of ingestion by, and/or contact exposure of, an infant, nursing women should not apply trifarotene cream to the chest or breast area

Fertility

Recommendations below are applicable to South Africa and other jurisdictions

• No human fertility studies were conducted with trifarotene
• No effects of trifarotene on fertility were found in rats in reproductive studies of oral administration
• However, after oral administration to dogs, findings of Germ cell degeneration were observed

Recommendations below are applicable to South Africa and other jurisdictions

• Caution; no information available
  Trifarotene has not been studied in patients with renal impairment

Recommendations below are applicable to South Africa and other jurisdictions

• Caution; no information available
  Trifarotene has not been studied in patients with hepatic impairment

Recommendations below are applicable to South Africa and other jurisdictions

• Caution; no information available
  Safety and efficacy of trifarotene in elderly patients aged 65 years and above have not been established

General Disorders and Administration Site Conditions

Common

• Application site irritation
• Application site pruritus

Uncommon

• Application site pain
• Application site dryness
• Application site discolouration
• Application site erosion
• Application site rash
• Application site swelling

Rare

• Application site erythema
• Application site urticaria
• Application site vesicles

Injury, Poisoning and Procedural Complications

Common

• Sunburn

Skin and Subcutaneous Tissue Disorders

Uncommon

• Skin irritation
• Acne
• Dermatitis allergic
• Erythema

Rare

• Asteatotic eczema
• Seborrheic dermatitis
• Skin burning sensation
• Skin fissures
• Skin hyperpigmentation

Eye Disorders

Rare

• Eyelid exfoliation
• Eyelid oedema

Gastrointestinal Disorders

Rare

• Cheilitis

Vascular Disorders

Rare

• Flushing

• Cosmetics or acne medicines with desquamative, irritant or drying effects

None routine

Method of administration

• Cutaneous use only
• Before using the pump for the first time, prime it by pressing down several times until a small amount of medicine is dispensed (up to 10 times maximum)
• The pump is now ready to use
• Apply a thin layer of trifarotene cream to the affected areas of the face (forehead, nose, chin and right and left cheeks) and all affected areas of the trunk once a day, in the evening, on clean and dry skin:
  • One pump actuation should be enough to cover the face (i.e. forehead, cheeks, nose, and chin)
  • Two pump actuations should be enough to cover the upper trunk (i.e. reachable upper back, shoulders and chest). One additional pump actuation may be used for middle and lower back if acne is present

Trifarotene is a chemically stable, terphenyl acid derivative with retinoid-like activity. It is a potent RAR_γ agonist (retinoid acid receptor γ agonist), characterised by its high specificity to this receptor over RAR_α & RAR_β (50- and 8-fold, respectively, with no Retinoid X Receptor (RXR) activity). In addition, trifarotene modulates retinoid target genes (differentiation and inflammatory processes) in immortalised keratinocytes and reconstructed epidermis.