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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Commercial
Therapeutic Areas
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Trade Name
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Drug Products
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EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
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Agency Specific
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Clinical
Clinical Trials
32 clinical trials
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Indications Phases 4
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Vomiting | D014839 | HP_0002013 | R11.1 | 10 | 4 | 6 | — | — | 20 |
| Nausea | D009325 | HP_0002018 | R11.0 | 8 | 4 | 6 | — | — | 18 |
| Postoperative nausea and vomiting | D020250 | EFO_0004888 | — | — | 2 | 2 | — | — | 4 |
| Neoplasms | D009369 | — | C80 | — | — | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Sleep initiation and maintenance disorders | D007319 | — | F51.01 | — | 4 | — | — | — | 4 |
| Depression | D003863 | — | F33.9 | — | 2 | — | — | 1 | 3 |
| Depressive disorder | D003866 | EFO_1002014 | F32.A | — | 2 | — | — | 1 | 3 |
| Major depressive disorder | D003865 | EFO_0003761 | F22 | — | 2 | — | — | — | 2 |
| Overactive urinary bladder | D053201 | EFO_1000781 | N32.81 | — | 2 | — | — | — | 2 |
| Urinary incontinence | D014549 | HP_0000020 | R32 | — | 2 | — | — | — | 2 |
| Enuresis | D004775 | — | R32 | — | 2 | — | — | — | 2 |
| Anxiety disorders | D001008 | EFO_0006788 | F41.1 | 1 | 1 | — | — | — | 2 |
| Social phobia | D000072861 | EFO_1001917 | F40.1 | 1 | 1 | — | — | — | 2 |
| Dyspepsia | D004415 | EFO_0008533 | K30 | — | 1 | — | — | — | 1 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Renal insufficiency | D051437 | HP_0000083 | N19 | 1 | — | — | — | — | 1 |
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Myofascial pain syndromes | D009209 | EFO_1001054 | — | — | — | — | — | 1 | 1 |
| Fibromyalgia | D005356 | EFO_0005687 | M79.1 | — | — | — | — | 1 | 1 |
Epidemiology
Epidemiological information for investigational and approved indications
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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
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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
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Financial
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Trends
PubMed Central
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Additional graphs summarizing 143 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
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92 adverse events reported
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