Litoxetine Explained

Litoxetine (developmental code names SL 81-0385, IXA-001) is an antidepressant which was under clinical development for the treatment of depression in the early 1990s but was never marketed.[1] [2] It acts as a potent serotonin reuptake inhibitor (Ki for = 7 nM) and modest 5-HT3 receptor antagonist (Ki = 315 nM).[3] [4] It has antiemetic activity, and unlike the selective serotonin reuptake inhibitors (SSRIs), appears to have a negligible incidence of nausea and vomiting.[5] The drug is structurally related to indalpine. Development of litoxetine for depression was apparently ceased in the late 1990s. However, as of March 2017, development of litoxetine has been reinitiated and the drug is now in the phase II stage for the treatment of urinary incontinence.

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Notes and References

  1. Web site: Litoxetine - IXALTIS . AdisInsight . Springer Nature Switzerland AG . en. 2018-08-25.
  2. Fairweather DB, Patat A, Rosenzweig P, Curson VH, Dunmore C, Dubruc C, Hindmarch I . The psychomotor and cognitive effects of litoxetine in young and middle aged volunteers . British Journal of Clinical Pharmacology . 40 . 2 . 119–125 . August 1995 . 8562293 . 1365170 . 10.1111/j.1365-2125.1995.tb05767.x .
  3. Book: Gallagher PT . Beyond SSRIs: Second-generation Reuptake Inhibitors for the Treatment of Depression . Rankovic Z, Hargreaves R, Bingham M . Drug Discovery for Psychiatric Disorders. https://books.google.com/books?id=e3YoDwAAQBAJ&pg=PA195. 8 October 2012. Royal Society of Chemistry. 978-1-84973-494-3. 195–.
  4. Book: Olivier B, Soudijn W, van Wijngaarden I . Serotonin, dopamine, and norepinephrine transporters . Jucker E . Progress in Drug Research. https://books.google.com/books?id=-d8FCAAAQBAJ&pg=PA80. 6 December 2012. Birkhäuser. 978-3-0348-8391-7. 80–.
  5. Angel I, Schoemaker H, Prouteau M, Garreau M, Langer SZ . Litoxetine: a selective 5-HT uptake inhibitor with concomitant 5-HT3 receptor antagonist and antiemetic properties . European Journal of Pharmacology . 232 . 2–3 . 139–145 . March 1993 . 8385615 . 10.1016/0014-2999(93)90767-C .