filorexant

Small moleculeexperimental

Filorexant (INNTooltip International Nonproprietary Name, USANTooltip United States Approved Name; developmental code name MK-6096) is an orexin antagonist which was under development by Merck for the treatment of insomnia, depression, diabetic neuropathy, and migraine. It is a dual antagonist of the orexin OX1 and OX2 receptors. It has a relatively short elimination half-life of 3 to 6 hours. However, it dissociates slowly from the orexin receptors and may thereby have a longer duration. Possibly in relation to this, filorexant shows next-day somnolence similarly to suvorexant. In phase 2 clinical trials, filorexant was found to be effective in the treatment of insomnia, but was not effective in the treatment of major depressive disorder, painful diabetic neuropathy, or migraine. As of May 2015, filorexant was no longer listed on Merck's online development pipeline and hence development of the drug appears to have been discontinued. Development of filorexant may have been discontinued due to lack of differentiation from suvorexant (which was also developed by Merck). — Wikipedia

Clinical trial activity

5 trials · 1 clinical orgs · 0 marketing orgs

Phase 1
1
Phase 2
4
Phase 3
0
Phase 4
0

Earliest trial started Nov 1, 2009 (NCT02549027)

Timeline

2000s

  1. Jan 1, 2009

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2009

    Earliest Phase 2 Sponsor(trial)

Indications

Mechanism of action

Chemistry & pharmacology

Loading structure…

SMILES

Cc1ccc(-c2ncccn2)c(C(=O)N2C[C@H](COc3ccc(F)cn3)CC[C@H]2C)c1
Mol. weight
420.49 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • (5-((5-fluoropyridin-2-yloxy)methyl)-2-methylpiperidin-1-yl)(5-methyl-2-(pyrimidin-2-yl)phenyl)methanone
  • filorexant
  • filorexant
  • filorexant
  • filorexant
  • filorexant
  • mk-6096
  • mk-6096
  • mk-6096

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT01554176Phase 2May 1, 2012Merck
NCT01564459Phase 2Mar 1, 2012Merck
NCT01513291Phase 2Feb 1, 2012Merck
NCT01021852Phase 2Nov 1, 2009Merck
NCT02549027Phase 1Nov 1, 2009Merck
Showing 5 of 5 trials
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Organizations

Research & Development (1)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
MerckFor profit5522009
1 organizations
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