| Bioactivity | Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. | ||||||||||||
| Invitro | Tazarotene (AGN 190168), in both gel and cream formulations, has been used both as monotherapy and as an adjuvant therapy. For psoriasis it has been combined with steroids, calcipotriene and phototherapy, and for acne, with antibiotics. Tazarotene (AGN 190168) has been shown to upregulate the tumor suppressor, Tazarotene (AGN 190168) induced gene 3, which is overexpressed in psoriasis and skin cancer[1]. In human epidermal cell cultures, Tazarotene (AGN 190168) suppresses the gene expression of 2 marker proteins, MRP-8 (calgranulin A) and SKALP (skin derived anti-leukoproteinase), highly elevated in psoriatic epidermis[2]. | ||||||||||||
| In Vivo | Topical gel application provides direct delivery of Tazarotene (AGN 190168) into the skin. At 10 hours after a topical application of 0.1% Tazarotene (AGN 190168) gel to the skin of healthy individuals and patients with psoriasis, approximately 4 to 6% of the dose resides in the stratum corneum and 2% of the dose distributed to the viable epidermis and dermis. Tazarotene (AGN 190168) is designed to undergo rapid and complete metabolism to its active metabolite tazarotenic acid. Tazarotenic acid has a short systemic residence time and limited tissue distribution in animals[3].When topically applied, Tazarotene (AGN 190168) blocks the induction of ornithine decarboxylase (ODC) activity by the tumour promoter 12-O-tetradecanoylphorbol 13-acetate (TPA) in the epidermis of the hairless mouse[3]. | ||||||||||||
| Name | Tazarotene | ||||||||||||
| CAS | 118292-40-3 | ||||||||||||
| Formula | C21H21NO2S | ||||||||||||
| Molar Mass | 351.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Talpur R, et al. Efficacy and safety of topical tazarotene: a review. Expert Opin Drug Metab Toxicol. 2009 Feb;5(2):195-210. [2]. Nagpal S, et al. Negative regulation of two hyperproliferative keratinocyte differentiation markers by a retinoic acidreceptor-specific retinoid: insight into the mechanism of retinoid action in psoriasis. Cell Growth Differ. 1996 Dec;7(12):1783-91. [3]. Tang-Liu DD, et al. Clinical pharmacokinetics and drug metabolism of tazarotene: a novel topical treatment for acne and psoriasis. Clin Pharmacokinet. 1999 Oct;37(4):273-87. |
Tazarotene
CAS: 118292-40-3 F: C21H21NO2S W: 351.46
Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and ac
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