Bicifadine Explained

Bicifadine (DOV-220,075) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) discovered at American Cyanamid as an analgesic drug candidate, and licensed to DOV Pharmaceutical in 1998 after American Cyanamid was acquired by Wyeth.[1] [2] [3]

In January 2007, Dov licensed the rights to bicifadine to XTL Biopharmaceuticals after bicifadine failed in a Phase III clinical trial for chronic lower back pain.[4] [5] [6] XTL ran a PhaseIIb clinical trial for pain caused by diabetic neuropathy, which failed in 2008;[7] XTL terminated the agreement in 2010.[8] In 2010 Dov was acquired by Euthymics Bioscience which intended to continue development of other candidates from Dov's portfolio.[9]

Bicifadine has a non-opioid, non-NSAID mechanism for the treatment of pain, which should have less abuse potential than opioid drugs and less propensity to cause gastric ulcers than NSAID drugs.[10] While the drug is purported to be a serotonin (SERT) and noradrenaline transporter (NET) inhibitor, it also has effects at the dopamine transporter (DAT), effectively making it a broad-spectrum monoamine transporter inhibitor or "triple reuptake inhibitor."[11]

See also

Notes and References

  1. Marks DM, Pae CU, Patkar AA . Triple reuptake inhibitors: a premise and promise . Psychiatry Investigation . 5 . 3 . 142–7 . September 2008 . 20046357 . 2796030 . 10.4306/pi.2008.5.3.142 .
  2. https://www.sec.gov/Archives/edgar/data/1066833/000114420404018172/v08017_ex10-51.txt SEC Filing: Wyeth-DOV Restated License Agreement
  3. Book: Neubauer DN . Indiplon . 453––464 . GABA and Sleep: Molecular, Functional and Clinical Aspects . Monti JM, Pandi-Perumal SR, Möhler H . Springer Science & Business Media . 2010 . 9783034602266 .
  4. Web site: Lawrence S, Hansen S . Bear Out of Hibernation . BioCentury . 26 July 2010 .
  5. Web site: Euthymics: Balancing act . A13 . BioCentury, The Bernstein Report on Biobusiness . December 5, 2011 . May 7, 2012 . https://web.archive.org/web/20140813091046/http://euthymics.com/wp-content/uploads/2011/12/EUTHYMICS_BIOSCIENCE_ECP_BERNSTEIN_REPORT_120511bc1.pdf . August 13, 2014 . dead .
  6. Web site: Caroll J . Fierce Biotech . 7 January 2007 . XTL licenses development rights to pain therapy .
  7. Fierce Biotech. December 9, 2008 Tiny XTL cuts costs, jobs
  8. Web site: XTL Form 6-K March, 2013 . 2015-07-15 . 2015-07-15 . https://web.archive.org/web/20150715173024/http://markets.on.nytimes.com/research/stocks/fundamentals/drawFiling.asp?docKey=137-000114420413017126-72672IPVQ4UFBUKR6AA4FI0HPE&docFormat=HTM&formType=6-K . dead .
  9. Fierce Biotech July 22, 2010 Euthymics lands $24M to fund antidepressant work
  10. Wang RI, Johnson RP, Lee JC, Waite EM . The oral analgesic efficacy of bicifadine hydrochloride in postoperative pain . Journal of Clinical Pharmacology . 22 . 4 . 160–4 . April 1982 . 7096604 . 10.1002/j.1552-4604.1982.tb02157.x . 35998284 .
  11. Basile AS, Janowsky A, Golembiowska K, Kowalska M, Tam E, Benveniste M, Popik P, Nikiforuk A, Krawczyk M, Nowak G, Krieter PA, Lippa AS, Skolnick P, Koustova E . 6 . Characterization of the antinociceptive actions of bicifadine in models of acute, persistent, and chronic pain . The Journal of Pharmacology and Experimental Therapeutics . 321 . 3 . 1208–25 . June 2007 . 17325229 . 10.1124/jpet.106.116483 . 17215882 .