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Description: Etretinate is a medication used to treat severe psoriasis. It is a synthetic aromatic retinoid. The mechanism of action of etretinate is still incompletely understood although, like retinoic acid, it is thought to interfere with the terminal differentiation of keratinocytes. It is thought to bind to the retinoic acid receptors. Etretinate is also believed to enhance the binding of cAMP to the regulatory RI subunit of cAMP dependent protein kinases. It was removed from the United States market in 1998 and the Canadian market in 1996 as a psoriasis medication, due to the high risk of birth defects. Etretinate is now used to treat T-cell lymphomas. It also appears to inhibit NADH oxidase activity.
Drug Type: Small Molecule; Withdrawn
Pharmacology: The active metabolite responsible for etretinate's effects, acitretin, is a retinoid. Retinoids have a structure similar to vitamin A and are involved in the normal growth of skin cells. Acitretin works by inhibiting the excessive cell growth and keratinisation (process by which skin cells become thickened due to the deposition of a protein within them) seen in psoriasis. It therefore reduces the thickening of the skin, plaque formation and scaling.
Mechanism of Action: The mechanism of action of the active metabolite, acitretin, is unknown, however it is believed to work by targeting specific receptors (retinoid receptors) in the skin which help normalize the growth cycle of skin cells.
Indication: For the treatment of severe psoriasis in adults.
Half Life: In one study, the apparent terminal half-life of etretinate after 6 months of therapy was approximately 120 days. In another study of 47 patients who had undergone chronic therapy with etretinate, 5 patients had detectable serum drug concentrations (0.5 to 12 ng/mL) 2.1 to 2.9 years after therapy was completed.
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    The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information.

    Authors: David S Wishart, Craig Knox, An Chi Guo et al.

    Organization: Department of Computing Science, Univers…

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Thought leaders and organizations working on research involving etretinate.

  • Mariko Seishima
  • Yoshinao Shibuya
  • Atsuyuki Igarashi
  • Akira Ohkawara
  • M Mashiko
  • National Institute of Allergy and Infectious Diseases (NIAID)
  • Bristol-Myers Squibb
  • Rockefeller University
  • Children's Hospital & Research Center Oakland
  • Hoffmann-La Roche
  • Ogaki Municipal Hospital
  • Yamaguchi University School of Medicine
  • Sungkyunkwan University School of Medicine
  • Hoshigaoka Koseinenkin Hospital
  • Aichi Medical University School of Medicine

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