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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 acer, nausea, neoplasms, and vomiting. It is known to target substance-P receptor.
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
neoplasmsD009369
signs and symptoms pathological conditionsD013568
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
AKYNZEOHelsinn HealthcareN-205718 RX2014-10-10
1 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
akynzeoNew Drug Application2020-10-22
Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
No data
Patent Expiration
Patent
Expires
Flag
FDA Information
Netupitant / Palonosetron Hydrochloride, Akynzeo, Helsinn Hlthcare
99510162035-09-25DS, DP
102331542035-09-25DP
106764402035-09-25DS, DP
109611952035-09-25DS, DP
92719752031-09-09U-2293
108282972030-12-17U-2293
86238262030-11-18U-2293
89519692030-11-18DP
91863572030-11-18U-2293
99435152030-11-18U-2293
115595232030-11-18DPU-3522
62973752023-03-17DP
ATC Codes
No data
HCPCS
Code
Description
J1454
Injection, fosnetupitant 235 mg and palonosetron 0.25 mg
J8655
Netupitant 300 mg and palonosetron 0.5 mg, oral
Clinical
Clinical Trials
18 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
VomitingD014839HP_0002013R11.1371110
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
NeoplasmsD009369C80212
NauseaD009325HP_0002018R11.0212
Drug-related side effects and adverse reactionsD064420T88.7111
Uterine cervical neoplasmsD002583111
Breast neoplasmsD001943EFO_0003869C5011
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Gallbladder neoplasmsD005706EFO_0004606C2311
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Healthy volunteers/patients11
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameNETUPITANT
INNnetupitant
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 classtachykinin (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
PDB6HLP
CAS-ID290297-26-6
RxCUI1552337
ChEMBL IDCHEMBL206253
ChEBI ID85155
PubChem CID6451149
DrugBankDB09048
UNII ID7732P08TIR (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
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
Mock data
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Additional graphs summarizing 339 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
Mock data
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25,752 adverse events reported
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