filorexant
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
Earliest trial started Nov 1, 2009 (NCT02549027)
Timeline
Indications
Mechanism of action
- Orexin receptorANTAGONIST
Orexin receptor antagonist
- Orexin receptorINHIBITOR
Orexin receptor inhibitor
Chemistry & pharmacology
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
- WikipediaFilorexant ↗
- ChEMBLCHEMBL2107822 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01554176 | Phase 2 | May 1, 2012 | Merck |
| NCT01564459 | Phase 2 | Mar 1, 2012 | Merck |
| NCT01513291 | Phase 2 | Feb 1, 2012 | Merck |
| NCT01021852 | Phase 2 | Nov 1, 2009 | Merck |
| NCT02549027 | Phase 1 | Nov 1, 2009 | Merck |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Merck | For profit | 5 | 5 | 2 | 2009 |