AKLIEF 50 µg/g Cream

What is AKLIEF 50 µg/g

AKLIEF (trifarotene) 50 µg/g cream is a next-generation topical retinoid specifically approved for the treatment of moderate-to-severe acne vulgaris of the face and trunk. Each gram of cream delivers 50 micrograms of trifarotene—a highly selective retinoic-acid-receptor-gamma (RAR-γ) agonist—formulated in a light, non-comedogenic vehicle dispensed from a polypropylene pump bottle to ensure dose accuracy and protect the active ingredient from light and oxidation. Trifarotene was first authorized by the U.S. FDA in 2019 and later by EMA and other health authorities after demonstrating robust efficacy and a favorable safety profile in pivotal Phase III trials (PERFECT 1 & 2). Unlike earlier “broad-spectrum” topical retinoids (tretinoin, adapalene, tazarotene), trifarotene’s receptor selectivity targets keratinocyte differentiation and comedolytic pathways with minimal off-target irritation, allowing effective once-daily use on large body areas.

• Pharmacological class – Fourth-generation retinoid (RAR-γ agonist).
• Indications – Approved for inflammatory and non-inflammatory lesions of acne vulgaris on face, chest, shoulders, and back in patients ≥ 9 years.
• Presentation – 75 g polypropylene (PP) pump bottle with over-cap, delivering ~250 metered actuations (0.3 g/actuation).
• Formulation highlights – Alcohol-free, fragrance-free lotion-like cream; contains moisturizing excipients (isododecane, glycerin) to enhance tolerability.
• Regulatory status – Prescription-only medicine (Rx); Pregnancy Category C (US) / Category D (AU); contraindicated in pregnancy despite low systemic exposure.
• Unique benefits – First retinoid specifically studied for truncal acne; superior lesion-count reduction versus vehicle by Week 12; maintains long-term clearance up to 52 weeks with continued use.
• Patient suitability – Adolescents and adults with papulopustular or comedonal acne who need a once-daily, high-potency retinoid with streamlined application over extensive skin surfaces.

How to use AKLIEF 50 µg/g

Proper application technique maximizes therapeutic benefit while minimizing irritation. In clinical practice, counseling on cleansing, dosing, and sun protection consistently improves adherence and outcomes.

• Preparation
  • Wash the affected skin gently with a mild, non-soap cleanser; pat dry thoroughly—residual moisture can enhance retinoid penetration and irritation.
  • Allow skin to rest for ≥ 10 minutes after washing to minimize transient stinging.
• Pump priming & dosing
  • Before first use, depress pump three times to achieve uniform dosing.
  • Standard regimen: once daily in the evening. Dispense the number of actuations matched to body region:
    • Face – 1 pump (≈ 0.3 g)
    • Upper trunk (chest/shoulders) – 2 pumps
    • Mid/Lower back – 2–3 pumps as needed
    Do not exceed 4 pumps per session unless specifically directed by a clinician.
• Application technique
  • Spread the cream as a thin, invisible film using clean fingertips—thicker layers do not improve efficacy but heighten irritation.
  • Keep product out of eyes, nostrils, lips, and mucous membranes; wipe excess with a tissue if accidental contact occurs.
• Adjunctive skin care
  • Use an oil-free moisturizer each morning; apply sunscreen SPF 30 + broad-spectrum daily (photosensitivity risk).
  • Avoid abrasive cleansers, astringents, and concurrent “peeling” agents (e.g., salicylic acid) during the first 4 weeks.
• Titration & tolerability
  • If irritation (erythema, scaling) becomes bothersome, consider alternate-night application for 1 week, then resume nightly.
  • Therapeutic response typically emerges by Week 4 and continues to improve through Week 12–24.
• Missed dose – Skip and apply next evening; avoid “double-dosing.”
• Cosmetic use – Non-comedogenic makeup may be applied once cream has fully dried (≈ 5 minutes).

Mode of Action AKLIEF 50 µg/g

Trifarotene is the first topical retinoid engineered for selective high-affinity binding to retinoic-acid-receptor-gamma (RAR-γ), the predominant RAR isoform in epidermal keratinocytes. This precision pharmacology yields potent comedolytic and anti-inflammatory effects with reduced off-target activity compared with earlier retinoids.

• RAR-γ activation
  • Trifarotene binds RAR-γ with ≥ 20-fold greater affinity than RAR-α or β.
  • Ligand-bound RAR-γ forms heterodimers with RXR, translocates to nuclei, and modulates transcription of genes governing keratinocyte proliferation, differentiation, and desquamation.
• Normalization of follicular epithelium
  • Reduces hyper-keratinization within the pilosebaceous unit, promoting expulsion of existing micro-comedones and preventing formation of new plugs.
• Anti-inflammatory cascade
  • Down-regulates toll-like-receptor-2 and AP-1-mediated expression of pro-inflammatory cytokines (IL-6, IL-8), dampening the inflammatory milieu that fuels papular and pustular lesions.
• Selective metabolism
  • Undergoes rapid hepatic metabolism (CYP 3A4-mediated hydroxylation) with negligible systemic accumulation—systemic availability is < 1% of topical dose, supporting its favorable safety profile.
• Unique truncal benefit
  • RAR-γ predominates on truncal skin, explaining trifarotene’s superior efficacy on chest/back vs. legacy retinoids.
• Synergy with standard acne therapy – Enhances penetration of topical antibiotics and benzoyl peroxide by loosening stratum corneum; complementary to systemic agents (e.g., doxycycline) by targeting the follicular microenvironment.

AKLIEF 50 µg/g Interactions AKLIEF 50 µg/g

Because cutaneous absorption of trifarotene is minimal, clinically significant systemic drug–drug interactions are unlikely. Nonetheless, certain topical or systemic agents can potentiate irritation, photosensitivity, or diminish therapeutic benefit. Consider the following when co-prescribing:

• Topical retinoids & keratolytics
  • Concurrent use with other retinoids (tretinoin, adapalene, tazarotene) or peeling agents (salicylic, glycolic, lactic acids) amplifies erythema and desquamation—avoid or stagger (morning vs. evening).
• Benzoyl peroxide (BPO)
  • Stable in presence of trifarotene; clinical trials support combined nightly trifarotene + morning 2.5–5% BPO for inflammatory acne. Advise separate application to reduce irritation.
• Topical antibiotics
  • Clindamycin/erythromycin gels pair well; apply in the morning. Retinoid-BPO-antibiotic combinations mitigate bacterial resistance.
• Systemic photosensitizers
  • Thiazides, tetracyclines, fluoroquinolones, and St John’s wort increase UV reactivity; counsel patients on stringent photoprotection when these drugs cannot be discontinued.
• Corticosteroids & immunosuppressants
  • Topical steroids may be used short-term to quell severe retinoid dermatitis; long-term co-use risks atrophy.
• Pregnancy-related considerations
  • Systemic retinoids (isotretinoin) are contraindicated during pregnancy; while AKLIEF’s systemic exposure is minimal, prudent practice is to discontinue trifarotene upon confirmed or planned pregnancy.
• Cosmetic procedures
  • Avoid dermabrasion, waxing, and chemical peels on treated areas within 5–7 days before and after application due to epidermal fragility.

Dosage of AKLIEF 50 µg/g

The goal is to deliver an even, thin layer over all acne-prone areas without saturating the skin. The metered pump simplifies standardized dosing:

• Adults & adolescents (≥ 9 years)
  • Face only – 1 pump (≈ 0.3 g) once nightly.
  • Face + upper trunk – 3 pumps total (1 face + 2 trunk) once nightly.
  • Full trunk – up to 4 pumps (distributed across chest, shoulders, back).
• Children < 9 years – Safety/efficacy not established; off-label use discour­aged pending pediatric studies.
• Renal or hepatic impairment – No dose adjustment required given negligible systemic absorption.
• Treatment duration
  • Initial review at 8–12 weeks; continue until satisfactory clearance, then reassess need for maintenance.
  • Long-term data up to 52 weeks show sustained efficacy without tachyphylaxis.
• Missed dose – Skip and resume next evening; excessive application does not accelerate results.
• Combination therapy – Can be paired with oral doxycycline or hormonal therapy for nodular or hormonal acne; retain once-daily trifarotene schedule.
• Adjustment for irritation
  • If significant dryness occurs, reduce frequency to every other night for 1–2 weeks, then return to nightly as tolerated.
  • Introduce non-comedogenic moisturizers and barrier creams (ceramide-based) twice daily.

Possible side effects of AKLIEF 50 µg/g

Most adverse reactions are mild-to-moderate, dose-dependent, and confined to the application site. Educating patients on expected “retinization” helps maintain adherence.

• Very common (≥ 10%)
  • Erythema, dryness, scaling (peak Weeks 2–4).
  • Transient burning/stinging immediately after application.
• Common (1–10%)
  • Pruritus, edema, increased skin sensitivity.
  • Photosensitivity—sunburn with minimal UV exposure.
• Uncommon (< 1%)
  • Hypo- or hyper-pigmentation, especially in Fitzpatrick IV–VI skin, usually reversible over months.
  • Contact dermatitis (allergic or irritant).
• Rare (< 0.1%)
  • Anaphylaxis, angio-edema—discontinue immediately and seek emergency care.
• Systemic events – Headache, gastrointestinal upset have been reported but causal linkage is weak given low absorption.
• Management strategies
  • Begin with smaller application area (“test zone”) for 3 nights before full-area use.
  • Emollient “sandwich” technique: moisturizer → trifarotene → moisturizer to buffer retinoid action.
  • Temporary dose reduction or short-course topical steroid (hydrocortisone 1%) for severe dermatitis.
• Patient counseling – Side-effects often peak early and wane by Week 8; persistence usually predicts better clinical outcomes.

AKLIEF 50 µg/g Contraindications AKLIEF 50 µg/g

• Known hypersensitivity to trifarotene or any excipients (e.g., isododecane, propylene glycol, polysorbate 80); manifests as acute dermatitis or urticaria.
• Pregnancy
  • All topical retinoids carry teratogenic risk, albeit theoretical for trifarotene due to minimal systemic exposure. Discontinue upon positive pregnancy test; advise effective contraception for women of child-bearing potential.
• Breast-feeding – Avoid application to chest to prevent infant exposure; otherwise deemed low risk.
• Eczema or sun-burned skin – Delay treatment until epidermal barrier recovers; retinoids exacerbate inflammation.
• Concomitant photosensitizing therapy – Relative contraindication; weigh benefits vs. heightened phototoxicity.
• Severe rosacea or perioral dermatitis – May worsen these conditions.
• Open wounds or mucosal surfaces – Absorption and irritation unpredictable; contraindicated.

Storage of AKLIEF 50 µg/g

• Temperature – Store at 20–25 °C (68–77 °F); excursions permitted between 15 °C and 30 °C (59–86 °F).
• Packaging integrity – Keep the polypropylene pump tightly closed with over-cap to protect from air and microbial contamination.
• Light & humidity – Retinoids degrade with UV exposure; store in original carton away from direct light and high humidity bathrooms.
• Freezing & excessive heat – Avoid freezing; do not expose to temperatures > 40 °C (104 °F) such as parked cars—thermal stress reduces potency.
• In-use shelf-life – Discard 6 months after first pump actuation or by the carton’s stamped expiry date (whichever comes first); write the opening date on the label to track.
• Disposal – Do not rinse leftover cream into drains; dispose of container with household waste per local regulations.
• Keep out of reach of children – Accidental ingestion may cause retinoid toxicity; small children are particularly susceptible.