Aklief

Aklief Uses, Dosage, Side Effects, Food Interaction and all others data.

Aklief is a topical retinoid cream used in the treatment of acne vulgaris that was first approved for use in the United States in October 2019. Retinoids are a class of medications structurally and functionally analogous to vitamin A, though later generation retinoids such as trifarotene and adapalene bear little structural resemblance to vitamin A and are analogous only in function. Aklief is considered the first of the "fourth-generation" retinoids due to its uniquely selective activity - this selectivity appears to confer improved efficacy and reduced side effects as compared to older, less selective retinoids.

Aklief exerts its effects via agonism at retinoid receptors - these receptors function to alter DNA transcription, resulting in downstream modulation of the expression of various genes involved in acne pathogenesis. It may be associated with skin irritation and should not be applied to cuts, abrasions, or otherwise damaged skin. As trifarotene may result in photosensitivity, patients should be cautioned to avoid excess sun exposure and to use sunscreen and/or protective clothing if exposure is unavoidable.

Aklief
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Aklief
Generic	Trifarotene
Trifarotene Other Names	Trifarotene
Weight	0.005%,
Type	Topical Cream Date Of Approval: October 4, 2019 Company: Galderma Treatment For: Acne Vulgaris, Topical Cream
Formula	C₂₉H₃₃NO₄
Weight	Average: 459.586 Monoisotopic: 459.240958547
Protein binding	Trifarotene is 99.9% protein bound in plasma.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	Canada, United States,
Last Updated:	September 19, 2023 at 7:00 am

Uses

Aklief is a topical retinoid indicated for the treatment of acne vulgaris.

Aklief is indicated for the topical treatment of acne vulgaris in patients 9 years of age and older.

Aklief is also used to associated treatment for these conditions: Acne Vulgaris

How Aklief works

Aklief is a potent and selective agonist of retinoic acid receptor-γ (RAR-γ). It has significantly less activity at RAR-β and RAR-α (16- and 65-fold lower than activity at RAR-γ, respectively), and has no activity at retinoid X receptors (RXRs). Agonism at retinoic acid receptors results in dimerization, and the resulting receptor-ligand dimer binds to specific DNA regulatory sequences (retinoic acid response elements, or RAREs) in the promotor regions of retinoid-responsible genes. Downstream alterations to gene expression induced by binding to these regions is the principle mechanism through which trifarotene exerts its comedolytic, anti-inflammatory, and depigmenting effects.

Like other retinoids, trifarotene influences the expression of a number of genes involved in retinoid metabolism, epidermal differentiation/proliferation, and epidermal response to stress. In addition, trifarotene appears to modulate retinoid-mediated pathways involved in proteolysis, skin hydration, and cell adhesion - modulation of these additional pathways has not been observed with other retinoids and may therefore be unique to trifarotene.

Toxicity

Aklief does not appear to carry any risk of carcinogenesis when used at standard doses. Systemic exposures in mice following both topical and oral administration were up to 1642 times higher than those seen in humans at the maximal recommended human dose, and these systemic concentrations did not result in observed carcinogenicity. Data regarding overdosage of trifarotene is unavailable.

Food Interaction

No interactions found.

Elimination Route

Systemic absorption of trifarotene is minimal. In a pharmacokinetic study involving 19 subjects, systemic concentrations were only quantifiable in 7 - steady state C_max values ranged from undetectable (0-24h ranged from 75 to 104 pg.h/mL.