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Chemical Compound Review

Suretin     ethyl6-[2-(4,4- dimethylthiochroman-6...

Synonyms: Tazorac, Tazoral, Fabior, tazarotene, tazaroteno, ...
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Disease relevance of Tazorac


High impact information on Tazorac


Chemical compound and disease context of Tazorac


Biological context of Tazorac


Anatomical context of Tazorac

  • TIG2 is neither expressed nor induced by tazarotene in primary keratinocyte and fibroblast cultures [15].
  • At 10 hours after a topical application of 0.1% tazarotene gel to the skin of healthy individuals and patients with psoriasis, approximately 4 to 6% of the dose resided in the stratum corneum and 2% of the dose distributed to the viable epidermis and dermis [4].
  • Indeed, tazarotene modulates the expression of the p73 gene in immortalized keratinocyte cell lines by inducing the pro-apoptotic and anti-proliferative TAp73 isoforms and by repressing the anti-apoptotic and pro-proliferative DeltaNp73 isoforms [16].
  • Metabolic deesterification of tazarotene in human blood and rat and human liver microsomes [17].
  • Third, tazarotene and its metabolites are rapidly eliminated from the blood in the urine and feces [18].

Associations of Tazorac with other chemical compounds


Gene context of Tazorac

  • Finally, we demonstrate that TIG1 is induced by AGN 190168 in psoriatic lesions during the course of clinical treatment of the disease [22].
  • Thus, TIG2 is expressed and induced by tazarotene only when keratinocytes and fibroblasts form a tissue-like 3-dimensional structure [15].
  • Tazarotene selectively transactivates RAR beta and RAR gamma subtypes and is inactive at retinoid X receptors (RXRs) [23].
  • These results indicate the relevance of p73 gene products in tazarotene-induced growth inhibition and effectiveness in the treatment of skin tumors [16].
  • By subtraction hybridization, we found that migration inhibitory factor-related protein (MRP-8) and skin-derived anti-leukoproteinase (SKALP) are down-regulated by AGN 190168 [14].

Analytical, diagnostic and therapeutic context of Tazorac


  1. Preliminary observations on the use of topical tazarotene to treat basal-cell carcinoma. Peris, K., Fargnoli, M.C., Chimenti, S. N. Engl. J. Med. (1999) [Pubmed]
  2. Topical tazarotene chemoprevention reduces Basal cell carcinoma number and size in Ptch1+/- mice exposed to ultraviolet or ionizing radiation. So, P.L., Lee, K., Hebert, J., Walker, P., Lu, Y., Hwang, J., Kopelovich, L., Athar, M., Bickers, D., Aszterbaum, M., Epstein, E.H. Cancer Res. (2004) [Pubmed]
  3. A retinoic acid receptor beta/gamma-selective prodrug (tazarotene) plus a retinoid X receptor ligand induces extracellular signal-regulated kinase activation, retinoblastoma hypophosphorylation, G0 arrest, and cell differentiation. Yen, A., Fenning, R., Chandraratna, R., Walker, P., Varvayanis, S. Mol. Pharmacol. (2004) [Pubmed]
  4. Clinical pharmacokinetics and drug metabolism of tazarotene: a novel topical treatment for acne and psoriasis. Tang-Liu, D.D., Matsumoto, R.M., Usansky, J.I. Clinical pharmacokinetics. (1999) [Pubmed]
  5. Tazarotene. Foster, R.H., Brogden, R.N., Benfield, P. Drugs (1998) [Pubmed]
  6. Identification and characterization of a retinoid-induced class II tumor suppressor/growth regulatory gene. DiSepio, D., Ghosn, C., Eckert, R.L., Deucher, A., Robinson, N., Duvic, M., Chandraratna, R.A., Nagpal, S. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  7. Retinoic acid receptor-nuclear factor-interleukin 6 antagonism. A novel mechanism of retinoid-dependent inhibition of a keratinocyte hyperproliferative differentiation marker. DiSepio, D., Malhotra, M., Chandraratna, R.A., Nagpal, S. J. Biol. Chem. (1997) [Pubmed]
  8. Management of scalp psoriasis: guidelines for corticosteroid use in combination treatment. van der Vleuten, C.J., van de Kerkhof, P.C. Drugs (2001) [Pubmed]
  9. Receptor specificity of retinoid-induced epidermal hyperplasia: effect of RXR-selective agonists and correlation with topical irritation. Thacher, S.M., Standeven, A.M., Athanikar, J., Kopper, S., Castilleja, O., Escobar, M., Beard, R.L., Chandraratna, R.A. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  10. Tazarotene versus tretinoin or adapalene in the treatment of acne vulgaris. Kakita, L. J. Am. Acad. Dermatol. (2000) [Pubmed]
  11. Calcipotriol vs. tazarotene as combination therapy with narrowband ultraviolet B (311 nm): efficacy in patients with severe psoriasis. Schiener, R., Behrens-Williams, S.C., Pillekamp, H., Kaskel, P., Peter, R.U., Kerscher, M. Br. J. Dermatol. (2000) [Pubmed]
  12. Pharmacokinetics of tazarotene cream 0.1% after a single dose and after repeat topical applications at clinical or exaggerated application rates in patients with acne vulgaris or photodamaged skin. Yu, Z., Sefton, J., Lew-Kaya, D., Walker, P., Yu, D., Tang-Liu, D.D. Clinical pharmacokinetics. (2003) [Pubmed]
  13. Evidence of increased apoptosis and reduced proliferation in basal cell carcinomas treated with tazarotene. Orlandi, A., Bianchi, L., Costanzo, A., Campione, E., Giusto Spagnoli, L., Chimenti, S. J. Invest. Dermatol. (2004) [Pubmed]
  14. Negative regulation of two hyperproliferative keratinocyte differentiation markers by a retinoic acid receptor-specific retinoid: insight into the mechanism of retinoid action in psoriasis. Nagpal, S., Thacher, S.M., Patel, S., Friant, S., Malhotra, M., Shafer, J., Krasinski, G., Asano, A.T., Teng, M., Duvic, M., Chandraratna, R.A. Cell Growth Differ. (1996) [Pubmed]
  15. Tazarotene-induced gene 2 (TIG2), a novel retinoid-responsive gene in skin. Nagpal, S., Patel, S., Jacobe, H., DiSepio, D., Ghosn, C., Malhotra, M., Teng, M., Duvic, M., Chandraratna, R.A. J. Invest. Dermatol. (1997) [Pubmed]
  16. The p73 gene is an anti-tumoral target of the RARbeta/gamma-selective retinoid tazarotene. Papoutsaki, M., Lanza, M., Marinari, B., Nisticò, S., Moretti, F., Levrero, M., Chimenti, S., Costanzo, A. J. Invest. Dermatol. (2004) [Pubmed]
  17. Metabolic deesterification of tazarotene in human blood and rat and human liver microsomes. Madhu, C., Duff, S., Baumgarten, V., Rix, P., Small, D., Tang-Liu, D. Journal of pharmaceutical sciences. (1997) [Pubmed]
  18. Pharmacokinetics and safety of tazarotene. Menter, A. J. Am. Acad. Dermatol. (2000) [Pubmed]
  19. Tazarotene does not affect the pharmacokinetics and efficacy of a norethindrone/ethinylestradiol oral contraceptive. Yu, Z., Yu, D., Walker, P.S., Tang-Liu, D.D. Clinical pharmacokinetics. (2004) [Pubmed]
  20. A pharmacoeconomic analysis of topical therapies for patients with mild-to-moderate stable plaque psoriasis: a US study. Marchetti, A., LaPensee, K., An, P. Clinical therapeutics. (1998) [Pubmed]
  21. The role of tazarotene in the treatment of psoriasis. Marks, R. Br. J. Dermatol. (1999) [Pubmed]
  22. Tazarotene-induced gene 1 (TIG1), a novel retinoic acid receptor-responsive gene in skin. Nagpal, S., Patel, S., Asano, A.T., Johnson, A.T., Duvic, M., Chandraratna, R.A. J. Invest. Dermatol. (1996) [Pubmed]
  23. Tazarotene: the first receptor-selective topical retinoid for the treatment of psoriasis. Chandraratna, R.A. J. Am. Acad. Dermatol. (1997) [Pubmed]
  24. Advances in therapy for psoriasis: an overview of infliximab, etanercept, efalizumab, alefacept, adalimumab, tazarotene, and pimecrolimus. Saini, R., Tutrone, W.D., Weinberg, J.M. Curr. Pharm. Des. (2005) [Pubmed]
  25. Clinical safety of tazarotene in the treatment of plaque psoriasis. Marks, R. J. Am. Acad. Dermatol. (1997) [Pubmed]
  26. Disposition and biotransformation of the acetylenic retinoid tazarotene in humans. Attar, M., Yu, D., Ni, J., Yu, Z., Ling, K.H., Tang-Liu, D.D. Journal of pharmaceutical sciences. (2005) [Pubmed]
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