Clinical data
Routes of
ATC code
  • none
Legal status
Legal status
  • US: Unscheduled
Pharmacokinetic data
Elimination half-life 1.6 hours
Excretion renal
CAS Number
PubChem CID
ECHA InfoCard 100.124.957
Chemical and physical data
Formula C12H15N
Molar mass 173.25 g/mol
3D model (JSmol)
 NY (what is this?)  (verify)

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


  1. Marks DM, Pae CU, Patkar AA. Triple reuptake inhibitors: a premise and promise. Psychiatry Investig. 2008 Sep;5(3):142-7. PMID 20046357 PMC 2796030
  2. SEC Filing: Wyeth-DOV Restated License Agreement Page accessed July 15, 2015]
  3. Neubauer, DN. "Indiplon". pp 453-464 in GABA and Sleep: Molecular, Functional and Clinical Aspects. Eds Jaime M. Monti, Seithikurippu Ratnas Pandi-Perumal, Hanns Möhler. Springer Science & Business Media, 2010 ISBN 9783034602266
  4. BioCentury, July 26, 2010
  5. "Euthymics: Balancing act" (PDF). BioCentury, The Bernstein Report on Biobusiness. December 5, 2011. p. A13.
  6. John Caroll for Fierce Biotech. Jan 07, 2007 XTL licenses development rights to pain therapy
  7. Fierce Biotech. December 9, 2008 Tiny XTL cuts costs, jobs
  8. XTL Form 6-K March, 2013
  9. Fierce Biotech July 22, 2010 Euthymics lands $24M to fund antidepressant work
  10. Wang, R. I.; Johnson, R. P.; Lee, J. C.; Waite, E. M. (1982). "The Oral Analgesic Efficacy of Bicifadine Hydrochloride in Postoperative Pain". Journal of Clinical Pharmacology. 22 (4): 160–164. doi:10.1002/j.1552-4604.1982.tb02157.x. PMID 7096604.
  11. Basile, A.; Janowsky, A.; Golembiowska, K.; Kowalska, M.; Tam, E.; Benveniste, M.; Popik, P.; Nikiforuk, A.; Krawczyk, M.; Nowak, G.; Krieter, P. A.; Lippa, A. S.; Skolnick, P.; Koustova, E. (2007). "Characterization of the Antinociceptive Actions of Bicifadine in Models of Acute, Persistent, and Chronic Pain". The Journal of Pharmacology and Experimental Therapeutics. 321 (3): 1208–1225. doi:10.1124/jpet.106.116483. PMID 17325229.
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