Casopitant
Casopitant is a small molecule pharmaceutical. It is currently being investigated in clinical studies. It is known to target substance-P receptor.
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Drug
Target
Variants
Financial
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Events Timeline
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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
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Agency Specific
FDA
EMA
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Patent Expiration
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HCPCS
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Clinical
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Drug
General
| Drug common name | Casopitant |
| INN | casopitant |
| Description | Casopitant (INNTooltip International Nonproprietary Name),: 208 former tentative trade names Rezonic (U.S.) and Zunrisa (Europe), is an NK1 receptor antagonist which was undergoing research for the treatment of chemotherapy-induced nausea and vomiting. It was under development by GlaxoSmithKline. In July 2008, the company filed a marketing authorisation application with the European Medicines Agency. The application was withdrawn and development was discontinued in September 2009 because GlaxoSmithKline decided that further safety assessment was necessary. However, a 2022 review listed casopitant as under development as a potential novel antidepressant for the treatment of major depressive disorder, with a phase 2 clinical trial having been completed.
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| Classification | Small molecule |
| Drug class | tachykinin (neurokinin) receptor antagonists: NK1 receptor antagonists |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | CC(=O)N1CCN([C@H]2CCN(C(=O)N(C)[C@H](C)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)[C@@H](c3ccc(F)cc3C)C2)CC1 |
Identifiers
| PDB | — |
| CAS-ID | 414910-27-3 |
| RxCUI | — |
| ChEMBL ID | CHEMBL1672054 |
| ChEBI ID | — |
| PubChem CID | 23725089 |
| DrugBank | — |
| UNII ID | 3B03KPM27L (ChemIDplus, GSRS) |
Target
Agency Approved
No data
Alternate
TACR1
TACR1
Organism
Homo sapiens
Gene name
TACR1
Gene synonyms
NK1R, TAC1R
NCBI Gene ID
Protein name
substance-P receptor
Protein synonyms
neurokinin receptor 1, NK-1 receptor, NK-1R, Tachykinin receptor 1, tachykinin receptor 1 (substance P receptor; neurokinin-1 receptor)
Uniprot ID
Mouse ortholog
Tacr1 (21336)
substance-P receptor (Q8BYR7)
Variants
No data
Financial
No data
Trends
No data
Safety
Black-box Warning
No Black-box warning
Adverse Events
0 adverse events reported
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