DOV-216,303 explained

DOV 216,303 is an experimental antidepressant drug originally developed by DOV Pharmaceutical and was licensed to Merck & Co. in 2004;^[1] Merck and DOV terminated their relationship in December 2006.^{[2] [3]}

It is a triple reuptake inhibitor (TRI), or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).^[4] It is the racemic mixture of amitifadine (DOV-21,947) and its (–)-enantiomer, DOV-102,677. Its IC₅₀ values for SERT, NET, and DAT are K_i 14 nM, 20 nM, and 78 nM, respectively.^[4]

As of March 2008, DOV had no intention to further develop DOV-216,303 because the patent on the compound had expired.^[2]

In a mouse model, DOV-216,303 has shown the ability to promote recovery after spinal cord contusion.^[5]

See also

• Bicifadine

Notes and References

1. News: McCoy . Michael . vanc . Merck and DOV Pharmaceutical In Drug Pact . Chemical & Engineering News . August 12, 2004.
2. Web site: 10-K For the fiscal year ended December 31, 2007. Dov Pharmaceutical via SEC Edgar. March 31, 2008. DOV 216,303 was originally in development for depression; however as the patented composition of matter claim has expired, there are no ongoing clinical trials of DOV 216,303 and none are planned..
3. Web site: DOV 216303 . Adis Insight . Springer Nature Switzerland AG . 26 February 2017. en.
4. Skolnick P, Krieter P, Tizzano J, Basile A, Popik P, Czobor P, Lippa A . Preclinical and clinical pharmacology of DOV 216,303, a "triple" reuptake inhibitor . CNS Drug Reviews . 12 . 2 . 123–34 . 2006 . 16958986 . 6494125 . 10.1111/j.1527-3458.2006.00123.x .
5. Chu TH, Cummins K, Stys PK . The triple monoamine re-uptake inhibitor DOV 216,303 promotes functional recovery after spinal cord contusion injury in mice . Neuroscience Letters . 675 . 1–6 . May 2018 . 29578004 . 10.1016/j.neulet.2018.03.050 . 5007186 .