Femoxetine Explained

Femoxetine (INN; tentative brand name Malexil; developmental code name FG-4963) is a drug related to paroxetine that was being developed as an antidepressant by Danish pharmaceutical company Ferrosan in 1975 before acquisition of the company by Novo Nordisk. It acts as a selective serotonin reuptake inhibitor (SSRI). Development was halted to focus attention on paroxetine instead, as femoxetine could not be administered as a daily pill.

Both femoxetine and paroxetine were invented in the 1970s. Jørgen Anders Christensen's name is on the patents and Jorgen Buus-Lassen's name is on the pharmacology paper.[1]

After Ferrosan's acquisition, femoxetine died from neglect.[2]

In a separate patent, Ferrosan stated that Femoxetine could be used as an appetite suppressant, using ten times the dosage than for paroxetine, 300 - 400mg daily.

Femoxetine has the same stereochemical properties as Nocaine, another agent with a similar structure claimed to have been synthesized using arecoline as the starting alkaloid.

Analogs

  1. Addition of the para-fluoro atom results in a different compound that is a hybrid of femoxetine & paroxetine named FG 7080,[3] which has a separate patent. According to the patent tables, incorporation of the fluorine atom potentiated the 5-HT affinity considerably.
  2. Pfizer made some similar analogs E.g. a Viloxazine type of catechol ether is used, but 4-phenyl instead of based on a morpholine ring.
  3. NNC-63-0780.[4] [5] binds to ORL1 instead of SERT.

See also

Notes and References

  1. Lassen JB, Petersen E, Kjellberg B, Olsson SO . Comparative studies of a new 5HT-uptake inhibitor and some tricyclic thymoleptics . European Journal of Pharmacology . 32 . 1 . 108–15 . May 1975 . 1149822 . 10.1016/0014-2999(75)90329-5 .
  2. Book: Healy D . Let them eat Prozac: the unhealthy relationship between the pharmaceutical industry and depression. 2004. New York Univ. Press. New York, NY. 9780814736692. 26–27. registration. Jørgen Buus Lassen femoxetine..
  3. Web site: (3S,4R)-4-(4-Fluorophenyl)-3-[(4-methoxyphenoxy)methyl]piperidine ]. PubChem . U.S. National Library of Medicine .
  4. Bignan GC, Connolly PJ, Middleton SA . Recent advances towards the discovery of ORL-1 receptor agonists and antagonists. Expert Opinion on Therapeutic Patents. 15. 4. 2005. 357–388 6. 10.1517/13543776.15.4.357. 94720416.
  5. Web site: CID:9862655 . PubChem . U.S. National Library of Medicine .

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