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Flibanserin

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Flibanserin chemical structure
Flibanserin

1-[2-[4-(3-trifluoromethyl phenyl) piperazin-1-yl] ethyl] benzimidazol- [1H]-2-one
IUPAC name
CAS number
167933-07-5 		ATC code

none{{{ATC_suffix}}}

PubChem
6918248 		DrugBank
{{{DrugBank}}}
Chemical formula {{{chemical_formula}}}
Molecular weight 390.40 g/mol
Bioavailability {{{bioavailability}}}
Metabolism {{{metabolism}}}
Elimination half-life {{{elimination_half-life}}}
Excretion {{{excretion}}}
Pregnancy category {{{pregnancy_category}}}
Legal status {{{legal_status}}}
Routes of administration {{{routes_of_administration}}}

Flibanserin (BIMT-17) is a drug produced by Boehringer Ingelheim.[1] It is currently being investigated as a drug for women with decreased sexual desire.[2] It is a 5-HT1A serotonin receptor agonist, a 5-HT2A serotonin receptor antagonist, and a dopamine D4 receptor partial agonist that had initially been developed as an anti-depressant.[3][4] As with Viagra, the effects of flibanserin were discovered serendipitously after it was trialled as an antidepressant.[5]

Contents

Early results

On November 16, 2009, Boehringer Ingelheim reported that late-stage trials showed that the drug promoted sexual desire and increased the number of "satisfying sexual events" in women suffering from abnormally low libido.

The results of four Phase III studies involving more than 2,000 pre-menopausal woman suffering from so-called Hypoactive Sexual Desire Disorder (HSDD) were presented at the congress of the European Society for Sexual Medicine in Lyon, France. Women with the drug said that the average number of times they had "satisfying sexual experiences" rose from 2.8 to 4.5 times a month. However, women with the placebo said the number of times rose to 3.7 times a month. Flibanserin must be taken once a day and takes up to 4 weeks to have an effect. In animals, flibanserin increases dopamine and noradrenalin and decreases serotonin.[6]

Mechanism of action

Flibanserin directly manipulates the chain of chemical reactions in the brain believed to trigger sexual desire[7]. This is unlike Procter & Gamble's hormone patch Intrinsa, which is targeted at post-menopausal women.

Clinical trials

As of November 2009, Phase III clinical trials are assessing safety and efficacy in pre- and post-menopausal women.[8][9]

See also

References

  1. ↑ Borsini F, Evans K, Jason K, Rohde F, Alexander B, Pollentier S (summer 2002). Pharmacology of flibanserin. CNS Drug Rev. 8 (2): 117–142.
  2. ↑ Jolly E, Clayton A, Thorp J, Lewis-D’Agostino D, Wunderlich G, Lesko L. Design of Phase III pivotal trials of flibanserin in female Hypoactive Sexual Desire Disorder (HSDD). Sexologies. Volume 17, Supplement 1, April 2008, Pages S133-S134. DOI:10.1016/S1158-1360(08)72886-X
  3. ↑ D'Aquila P, Monleon S, Borsini F, Brain P, Willner P (December 1997). Anti-anhedonic actions of the novel serotonergic agent flibanserin, a potential rapidly-acting antidepressant. European Journal of Pharmacology 340 (2-3): 121–32.
  4. ↑ Invernizzi RW, Sacchetti G, Parini S, Acconcia S, Samanin R (August 2003). Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors.. Br J Pharmacol. 139 (7): 1281–8.
  5. ↑ 'Female Viagra' discovery claim. BBC News, Tuesday, 17 November 2009
  6. ↑ Limp reception for female 'libido booster,' Clare Wilson, New Scientist, 21 November 2009, p. 11
  7. ↑ includeonly>"Boehringer Drug Shown to Kindle Female Sex Drive", ABC News, November 16, 2009. Retrieved on November 16, 2009.
  8. ↑ ClinicalTrials.gov NCT00996164
  9. ↑ ClinicalTrials.gov NCT00996372

External links


Antidepressants (ATC N06A) edit
Monoamine oxidase inhibitors (MAOI) Harmaline, Iproclozide, Iproniazid, Isocarboxazid, Nialamide, Phenelzine, Selegiline, Toloxatone, Tranylcypromine
Reversible inhibitor of monoamine oxidase A (RIMA) Brofaromine, Moclobemide
Dopamine reuptake inhibitor (DARI) Amineptine, Phenmetrazine, Vanoxerine, Modafinil
Norepinephrine-dopamine reuptake inhibitors Bupropion
Norepinephrine reuptake inhibitor (NRI) or (NARI) Atomoxetine, Maprotiline, Reboxetine, Viloxazine
Serotonin-norepinephrine reuptake inhibitor (SNRI) Duloxetine, Milnacipran, Venlafaxine
Selective serotonin reuptake inhibitor (SSRI) Alaproclate, Etoperidone, Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Zimelidine
Selective serotonin reuptake enhancer (SSRE) Tianeptine
Tricyclic antidepressants (TCA) Amitriptyline, Amoxapine, Butriptyline, Clomipramine, Desipramine, Dibenzepin, Dothiepin, Doxepin, Imipramine, Iprindole, Lofepramine, Melitracen, Nortriptyline, Opipramol, Protriptyline, Trimipramine
Tetracyclic antidepressants Maprotiline, Mianserin, Nefazodone, Trazodone
Noradrenergic and specific serotonergic antidepressant (NaSSA) Mirtazapine

Template:Piperazines



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