Akynzeo(netupitant)
Akynzeo (netupitant) is a small molecule pharmaceutical. Netupitant was first approved as Akynzeo on 2014-10-10. It has been approved in Europe to treat nausea, neoplasms, and vomiting. It is known to target substance-P receptor.
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Study first post date
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Commercial
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| neoplasms | D009369 |
| signs and symptoms pathological conditions | D013568 |
Trade Name
FDA
EMA
Combinations
Akynzeo
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Netupitant
+
Palonosetron hydrochloride
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| AKYNZEO | Helsinn Healthcare | N-205718 RX | 2014-10-10 | 1 products, RLD, RS |
Labels
FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| akynzeo | New Drug Application | 2023-12-10 |
Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
No data
Patent Expiration
Patent | Expires | Flag | FDA Information |
|---|---|---|---|
| Netupitant / Palonosetron Hydrochloride, Akynzeo, Helsinn Hlthcare | |||
| 9951016 | 2035-09-25 | DS, DP | |
| 10233154 | 2035-09-25 | DP | |
| 10676440 | 2035-09-25 | DS, DP | |
| 10961195 | 2035-09-25 | DS, DP | |
| 9271975 | 2031-09-09 | U-2293 | |
| 10828297 | 2030-12-17 | U-2293 | |
| 8623826 | 2030-11-18 | U-2293 | |
| 8951969 | 2030-11-18 | DP | |
| 9186357 | 2030-11-18 | U-2293 | |
| 9943515 | 2030-11-18 | U-2293 | |
| 11559523 | 2030-11-18 | DP | U-3522 |
| 6297375 | 2023-03-17 | DP | |
ATC Codes
No data
Clinical
Clinical Trials
24 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Vomiting | D014839 | HP_0002013 | R11.1 | — | 3 | 7 | 1 | 1 | 10 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Breast neoplasms | D001943 | EFO_0003869 | C50 | — | 1 | 1 | — | — | 2 |
| Neoplasms | D009369 | — | C80 | — | 2 | 1 | — | — | 2 |
| Nausea | D009325 | HP_0002018 | R11.0 | — | 2 | 1 | — | — | 2 |
| Drug-related side effects and adverse reactions | D064420 | — | T88.7 | — | 1 | 1 | — | — | 1 |
| Uterine cervical neoplasms | D002583 | HP_0030159 | — | — | 1 | 1 | — | — | 1 |
| Colorectal neoplasms | D015179 | — | — | — | — | 1 | — | — | 1 |
| Electroacupuncture | D015671 | — | — | — | — | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Gallbladder neoplasms | D005706 | EFO_0004606 | C23 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | — | — | 1 | — | — | — | — | 1 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Netupitant |
| INN | netupitant |
| Description | Netupitant is a monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-[3,5-bis(trifluoromethyl)phenyl]-2-methylpropanoic acid with the secondary amino group of N-methyl-4-(2-methylphenyl)-6-(4-methylpiperazin-1-yl)pyridin-3-amine; an antiemetic used in combination with palonosetron hydrochloride (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy. It has a role as an antiemetic and a neurokinin-1 receptor antagonist. It is a monocarboxylic acid amide, an organofluorine compound, an aminopyridine, a member of toluenes, a N-alkylpiperazine and a N-arylpiperazine. |
| Classification | Small molecule |
| Drug class | tachykinin (neurokinin) receptor antagonists: NK1 receptor antagonists |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | Cc1ccccc1-c1cc(N2CCN(C)CC2)ncc1N(C)C(=O)C(C)(C)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 |
Identifiers
| PDB | — |
| CAS-ID | 290297-26-6 |
| RxCUI | — |
| ChEMBL ID | CHEMBL206253 |
| ChEBI ID | 85155 |
| PubChem CID | 6451149 |
| DrugBank | DB09048 |
| UNII ID | 7732P08TIR (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
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 392 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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315 adverse events reported
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