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Chemical Compound Review

PubChem16389     6-[2-(4,4- dimethylthiochroman-6...

Synonyms: SureCN678713, AG-D-40589, ACMC-20enbg, CHEBI:73129, AGN-190299, ...
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Disease relevance of Tazarotenic acid

  • At standard application rates in patients with acne vulgaris, the maximum average C(max) and AUC values of tazarotenic acid were 0.10 +/- 0.06 microg/L (n = 8) and 1.54 +/- 1.01 microg. h/L (n = 8), respectively, and occurred on day 15 [1].
  • Also, lentigines, elastosis, pore size, irregular depigmentation, tactile roughness, coarse wrinkling, telangiectasia, actinic keratoses, overall integrated assessment of photodamage, global response to treatment, patients' overall assessment of photodamage, and plasma levels of tazarotenic acid [2].

High impact information on Tazarotenic acid

  • In both studies, the pharmacokinetics of tazarotenic acid on study day 61 (third cycle day 6) were evaluated from plasma tazarotenic acid concentrations [3].
  • At standard application rates in patients with photodamaged skin, the maximum average C(max) and AUC values of tazarotenic acid were 0.236 +/- 0.255 microg/L (n = 8) and 2.44 +/- 1.38 microg. h/L (n = 8), respectively, and occurred on day 15 [1].
  • The involvement of these isozymes in tazarotenic acid metabolism was further confirmed by inhibition of metabolite formation in pooled human liver microsomes by specific inhibitors of CYP2C8 or FMO [4].
  • Tazarotenic acid was incubated with 1 mg/ml pooled human liver microsomes, in 100 mM potassium phosphate buffer (pH 7.4), at 37 degrees C, over a period of 30 min [4].
  • The microsomal enzymes that may be involved in tazarotenic acid metabolism were identified through incubation with microsomes containing cDNA-expressed human microsomal isozymes [4].

Biological context of Tazarotenic acid


Associations of Tazarotenic acid with other chemical compounds


Gene context of Tazarotenic acid


Analytical, diagnostic and therapeutic context of Tazarotenic acid


  1. 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]
  2. Efficacy of 0.1% tazarotene cream for the treatment of photodamage: a 12-month multicenter, randomized trial. Phillips, T.J., Gottlieb, A.B., Leyden, J.J., Lowe, N.J., Lew-Kaya, D.A., Sefton, J., Walker, P.S., Gibson, J.R. Archives of dermatology. (2002) [Pubmed]
  3. 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]
  4. Cytochrome P450 2C8 and flavin-containing monooxygenases are involved in the metabolism of tazarotenic acid in humans. Attar, M., Dong, D., Ling, K.H., Tang-Liu, D.D. Drug Metab. Dispos. (2003) [Pubmed]
  5. 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]
  6. Tazarotene--first of a new generation of receptor-selective retinoids. Chandraratna, R.A. Br. J. Dermatol. (1996) [Pubmed]
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