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Drug ReportsFILOREXANT
FILOREXANT
Filorexant is a small molecule pharmaceutical. It is currently being investigated in clinical studies. It is known to target orexin receptor type 2 and orexin/Hypocretin receptor type 1.
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Variants
Financial
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Events Timeline
5D
1M
3M
6M
YTD
1Y
2Y
5Y
Max
Events
FDA approval date
EMA approval date
Patent expiration date
Study first post date
Last update post date
Start date
Primary completion date
Completion date
Results first post date
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Commercial
No data
Clinical
Clinical Trials
5 clinical trials
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Indications Phases 4
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Indications Phases 3
No data
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
DepressionD003863F33.911
Major depressive disorderD003865EFO_0003761F2211
Depressive disorderD003866EFO_1002014F32.A11
PainD010146EFO_0003843R5211
Diabetic neuropathiesD003929EFO_100078311
Migraine disordersD008881EFO_0003821G4311
HeadacheD006261HP_0002315R5111
Sleep initiation and maintenance disordersD007319F51.0111
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
PolysomnographyD01728611
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameFILOREXANT
INNfilorexant
Description
Filorexant (INN, USAN; 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).
Classification
Small molecule
Drug classOrexin antagonist
Image (chem structure or protein)Loading
Structure (InChI/SMILES or Protein Sequence)
Cc1ccc(-c2ncccn2)c(C(=O)N2C[C@H](COc3ccc(F)cn3)CC[C@H]2C)c1
Identifiers
PDB
CAS-ID1088991-73-4
RxCUI
ChEMBL IDCHEMBL2107822
ChEBI ID
PubChem CID25128145
DrugBank
UNII IDE6BTT8VA5Z (ChemIDplus, GSRS)
Target
Agency Approved
No data
Alternate
HCRTR2
HCRTR2
HCRTR1
HCRTR1
Organism
Homo sapiens
Gene name
HCRTR2
Gene synonyms
NCBI Gene ID
Protein name
orexin receptor type 2
Protein synonyms
hypocretin (orexin) receptor 2, Hypocretin receptor type 2, orexin type-2 receptor
Uniprot ID
Mouse ortholog
Hcrtr2 (387285)
orexin receptor type 2 (Q8BG12)
Variants
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Safety
Black-box Warning
No Black-box warning
Adverse Events
0 adverse events reported
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