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The Background of Retinoids
Published in Ayse Serap Karadag, Berna Aksoy, Lawrence Charles Parish, Retinoids in Dermatology, 2019
Ayse Serap Karadag, Berna Aksoy, Lawrence Charles Parish
Recently, trifarotene has been formulated as a cream for the treatment of facial and truncal acne for which selective retinoic acid receptor-γ (RAR-γ) activity that has recently been developed for moderate facial and truncal acne. The selectivity of trifarotene for RAR-γ distinguishes it from the existing first- and third-generation topical retinoids, which target both RAR-β and RAR-γ. Trifarotene has comedolytic, anti-inflammatory, and anti-pigmenting properties with a comparable safety profile due to its pharmacokinetic stability in keratinocytes and rapid metabolism by hepatic microsomes (18).
Low irritation potential of tazarotene 0.045% lotion: Head-to-head comparison to adapalene 0.3% gel and trifarotene 0.005% cream in two studies
Published in Journal of Dermatological Treatment, 2023
Tolerability of topical retinoids is impacted by a number of factors, including the retinoid itself, the concentration used, and the vehicle used for its delivery (8), as well as skin hydration and moisturization (5). Third- and fourth-generation topical retinoid formulations use lower drug concentrations, enhanced vehicles, and/or novel retinoids to be clinically efficacious while providing a more patient-friendly tolerability profile (2). For example, adapalene was specifically designed to have a particle size of 3–10 microns to provide preferential delivery into the pilosebaceous unit and is considered one of the best-tolerated topical retinoids (9,10); prescription-strength adapalene 0.3% gel is approved for the treatment of acne in patients aged 12 years and older (11). Tazarotene 0.045% lotion, approved for the treatment of acne in patients 9 years of age and older (12), uses a proprietary polymeric emulsion vehicle to uniformly deliver hydrating excipients onto the skin along with a lower dose of tazarotene than other commercially available 0.1% tazarotene formulations (13). Trifarotene is a first-in-class fourth-generation retinoid, developed to have greater specificity for the gamma subtype of retinoic acid receptors than its predecessors (14). Trifarotene 0.005% cream, indicated for the treatment of facial and truncal acne in patients 9 years of age and older, is the most-recently approved single-agent topical retinoid for acne (2,14–16).
Alitretinoin for the treatment of severe chronic eczema of the hands
Published in Expert Opinion on Pharmacotherapy, 2022
Maddalena Napolitano, Luca Potestio, Mario De Lucia, Mariateresa Nocerino, Gabriella Fabbrocini, Cataldo Patruno
The use of alitretinoin during pregnancy is absolutely contraindicated, because of its risk of teratogenicity as foremost of retinoids [18]. Only few retinoids, such as trifarotene, showed a safety profile of application also in childbearing potential women [32]. Alitretinoin can be administered in women childbearing potential only if effective contraceptive measures are respected and regular pregnancy testing is performed [26]. Moreover, contraception must be continued up to one month after treatment discontinuation. Hypothyroidism is another contraindication; in fact, alitretinoin can reduce thyroid function decreasing the levels of Thyroid-Stimulating-Hormone (TSH) and free T4 by binding these hormones [26]. Breastfeeding, severe renal insufficiency, uncontrolled hypertriglyceridemia, and/or hypercholesterolemia, hypervitaminosis A, and concomitant therapies with tetracyclines are the other contraindications to treatment with alitretinoin [26]. However, no significant differences were revealed comparing the pharmacokinetics of alitretinoin and its metabolites in patients with cirrhosis and healthy controls [26–28]. In Table 1 are reported all the blood examinations to perform before and during alitretinoin treatment.
Emerging drugs for the treatment of acne: a review of phase 2 & 3 trials
Published in Expert Opinion on Emerging Drugs, 2022
Siddharth Bhatt, Rohit Kothari, Durga Madhab Tripathy, Sunmeet Sandhu, Mahsa Babaei, Mohamad Goldust
Two-phase III double-blinded, randomized, vehicle-controlled trials have shown the efficacy and tolerability of trifarotene 50 µg/g once-daily application in facial and truncal acne on subjects aged 9 years and above.To prevent local irritation side effects of trifarotene, trials with a 0.45% polymeric lotion formulation have been made.