Tazarotene

(BAN, USAN, rINN)
Tazarotene Chemical formula
Synonyms: AGN-190168; Tatsaroteeni; Tazaroten; Tazarotène; Tazaroteno; Tazarotenum. Ethyl 6-[(4,4-dimethylthiochroman-6-yl)ethynyl]nicotinate.
Cyrillic synonym: Тазаротен.

💊 Chemical information

Chemical formula: C21H21NO2S = 351.5.
CAS — 118292-40-3.
ATC — D05AX05.
ATC Vet — QD05AX05.

💊 Adverse Effects and Precautions

As for Tretinoin. Systemic absorption from tazarotene applied topically is low, and the most frequent adverse effects are on the skin; the incidence of adverse events appears to be concentration related. Animal studies have indicated that tazarotene is fetotoxic and teratogenic, and licensed product information recommends that tazarotene should not be used during pregnancy or in women planning a pregnancy. Similarly, tazarotene should not be used, or used with caution, during breast feeding, as animal data indicate that it may be distributed into breast milk.

Effects on the skin.

A 57-year-old man with diabetes and recalcitrant psoriasis on the trunk and limbs developed acute dermatitis1 in the genital area 2 weeks after starting treatment with topical tazarotene 0.1%. The affected areas became ulcerated over the next few days. It was suspected that accidental contact with the tazarotene that had been applied to the truncal psoriasis was responsible. Pyogenic granuloma has been associated with topical tazarotene and other retinoids given orally or applied topically.
1. Wollina U. Genital ulcers in a psoriasis patient using topical tazarotene. Br J Dermatol 1998; 138: 713–14.

💊 Uses and Administration

Tazarotene is a retinoid used for the topical treatment of mild to moderate acne and plaque psoriasis, and to treat signs of photoageing. Tazarotene is a prodrug that is de-esterified in the skin to its active form, tazarotenic acid. The mode of action is unknown but it appears to modulate cell proliferation and differentiation. In the treatment of psoriasis, tazarotene 0.05% cream or gel is used initially and increased to 0.1% if necessary. It is applied once daily in the evening. In the UK tazarotene is licensed for use in patients with psoriasis affecting up to 10% of the body-surface; in the USA, it may be used on psoriasis involving up to 20% of the body-surface. In the treatment of acne, tazarotene is applied as a 0.1% gel or cream once daily in the evening. There may be exacerbation of acne during early treatment or of psoriasis at any time during treatment. The treatment period is usually up to 12 weeks, although tazarotene has been used for up to 12 months in the treatment of psoriasis. A 0.1% cream is used in the topical treatment of certain signs of photoageing (facial fine wrinkling, mottled hypo- and hyperpigmentation, and benign facial lentigines). It is applied once daily at bedtime to lightly cover the entire face.
1. Foster RH, et al. Tazarotene. Drugs 1998; 55: 705–11
2. Tang-Liu DD-S, et al. Clinical pharmacokinetics and drug metabolism of tazarotene: a novel topical treatment for acne and psoriasis. Clin Pharmacokinet 1999; 37: 273–87
3. Guenther LC. Optimizing treatment with topical tazarotene. Am J Clin Dermatol 2003; 4: 197–202.

Malignant neoplasms.

There has been some interest in the use of topical tazarotene in the treatment of neoplasms affecting the skin. Preliminary studies have reported some lesion regression or clearance in basal cell1 and squamous cell carcinomas2, and mycosis fungoides3.
1. Bianchi L, et al. Topical treatment of basal cell carcinoma with tazarotene: a clinicopathological study on a large series of cases. Br J Dermatol 2004; 151: 148–56
2. Bardazzi F, et al. A pilot study on the use of topical tazarotene to treat squamous cell carcinoma in situ. J Am Acad Dermatol 2005; 52: 1102–4
3. Apisarnthanarax N, et al. Tazarotene 0.1% gel for refractory mycosis fungoides lesions: an open-label pilot study. J Am Acad Dermatol 2004; 50: 600–607.

Skin disorders.

Tazarotene is used for the topical treatment of mild to moderate acne1,2 and plaque psoriasis3,4; benefit has also been reported for psoriasis of the nails.5,6 Improvement has been reported too in keratinisation disorders such as Darier’s disease7,8 and congenital ichthyosis9-11. Topical tazarotene can also improve some signs of photoageing, including fine wrinkling, mottled hyperpigmentation, and lentigines (liver spots).12-14
1. Leyden JJ. Meta-analysis of topical tazarotene in the treatment of mild to moderate acne. Cutis 2004; 74 (4 suppl): 9–15
2. Shalita AR, et al. Effects of tazarotene 0.1% cream in the treatment of facial acne vulgaris: pooled results from two multicenter, double-blind, randomized, vehicle-controlled, parallel-group trials. Clin Ther 2004; 26: 1865–73
3. Weinstein GD, et al. Tazarotene cream in the treatment of psoriasis: two multicenter, double-blind, randomized, vehicle-controlled studies of the safety and efficacy of tazarotene creams 0.05% and 0.1% applied once daily for 12 weeks. J Am Acad Dermatol 2003; 48: 760–7
4. Dando TM, Wellington K. Topical tazarotene: a review of its use in the treatment of plaque psoriasis. Am J Clin Dermatol 2005; 6: 255–72
5. Scher RK, et al. Tazarotene 0.1% gel in the treatment of fingernail psoriasis: a double-blind, randomized, vehicle-controlled study. Cutis 2001; 68: 355–8
6. Bianchi L, et al. Tazarotene 0.1% gel for psoriasis of the fingernails and toenails: an open, prospective study. Br J Dermatol 2003; 149: 207–9
7. Oster-Schmidt C. The treatment of Darier’s disease with topical tazarotene. Br J Dermatol 1999; 141: 603–4
8. Brazzelli V, et al. Linear Darier’s disease successfully treated with 0.1% tazarotene gel “short-contact” therapy. Eur J Dermatol 2006; 16: 59–61
9. Hofmann B, et al. Effect of topical tazarotene in the treatment of congenital ichthyosis. Br J Dermatol 1999; 141: 642–6
10. Marulli GC, et al. Type I lamellar ichthyosis improved by tazarotene 0.1% gel. Clin Exp Dermatol 2003; 28: 391–3
11. Kundu RV, et al. Lamellar ichthyosis treated with tazarotene 0.1% gel. J Am Acad Dermatol 2006; 55 (suppl 5): S94–S95
12. Phillips TJ, et al. Efficacy of 0.1% tazarotene cream for the treatment of photodamage: a 12-month multicenter, randomized trial. Arch Dermatol 2002; 138: 1486–93
13. Machtinger LA, et al. Histological effects of tazarotene 0.1% cream vs. vehicle on photodamaged skin: a 6-month, multicentre, double-blind, randomized, vehicle-controlled study in patients with photodamaged facial skin. Br J Dermatol 2004; 151: 1245–52
14. Kang S, et al. A multicenter, randomized, double-blind trial of tazarotene 0.1% cream in the treatment of photodamage. J Am Acad Dermatol 2005; 52: 268–74.

💊 Preparations

Proprietary Preparations

Austria: Zorac; Belg.: Zorac; Braz.: Zorac†; Canad.: Ta zo r ac ; Cz.: Tazorac; Fin.: Zorac†; Fr.: Zorac; Ger.: Zorac; Gr.: Zorac; India: La Tez; Ta z r e t † ; Irl.: Zorac; Israel: Zorac; Ital.: Zorac; Mex.: Suretin; Pol.: Zorac; S.Afr.: Zorak; Spain: Zorac; Swed.: Zorac†; Switz.: Zorac; UK: Zorac; USA: Avage; Tazorac.
Published January 21, 2019.