Filorexant
Filorexant is a small molecule pharmaceutical. It is currently being investigated in clinical studies. It is known to target orexin/Hypocretin receptor type 1 and orexin receptor type 2.
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Commercial
Therapeutic Areas
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Trade Name
FDA
EMA
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Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
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Labels
FDA
EMA
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Indications
FDA
EMA
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Agency Specific
FDA
EMA
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Patent Expiration
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ATC Codes
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HCPCS
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Clinical
Clinical Trials
5 clinical trials
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Indications Phases 4
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Indications Phases 3
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Major depressive disorder | D003865 | EFO_0003761 | F22 | — | 1 | — | — | — | 1 |
| Diabetic neuropathies | D003929 | EFO_1000783 | — | 1 | — | — | — | 1 | |
| Migraine disorders | D008881 | EFO_0003821 | G43 | — | 1 | — | — | — | 1 |
| Headache | D006261 | HP_0002315 | R51 | — | 1 | — | — | — | 1 |
| Sleep initiation and maintenance disorders | D007319 | F51.01 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Polysomnography | D017286 | 1 | — | — | — | — | 1 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | FILOREXANT |
| INN | filorexant |
| 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).
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| Classification | Small molecule |
| Drug class | Orexin antagonist |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | Cc1ccc(-c2ncccn2)c(C(=O)N2C[C@H](COc3ccc(F)cn3)CC[C@H]2C)c1 |
Identifiers
| PDB | 6TP6 |
| CAS-ID | 1088991-73-4 |
| RxCUI | — |
| ChEMBL ID | CHEMBL2107822 |
| ChEBI ID | — |
| PubChem CID | 25128145 |
| DrugBank | DB12158 |
| UNII ID | E6BTT8VA5Z (ChemIDplus, GSRS) |
Target
Agency Approved
No data
Alternate
HCRTR1
HCRTR1
HCRTR2
HCRTR2
Organism
Homo sapiens
Gene name
HCRTR1
Gene synonyms
NCBI Gene ID
Protein name
orexin/Hypocretin receptor type 1
Protein synonyms
hypocretin (orexin) receptor 1, Hypocretin receptor type 1, orexin receptor 1, Orexin receptor type 1, Ox-1-R, Ox1-R, Ox1R
Uniprot ID
Mouse ortholog
Hcrtr1 (230777)
orexin/Hypocretin receptor type 1 (Q80T45)
Variants
Clinical Variant
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Financial
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Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 65 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
0 adverse events reported
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