netupitant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| neurokinin NK1 (substance P) receptor antagonist | 4898 | 290297-26-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. Delayed emesis has been largely associated with the activation of tachykinin family neurokinin 1 (NK-1) receptors (broadly distributed in the central and peripheral nervous systems) by substance P. As shown in in vitro and in vivo studies, netupitant inhibits substance P mediated responses.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 5.54 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.83 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.00 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 34.28 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 10, 2014 | FDA | HELSINN HLTHCARE |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| FDA MoA | N0000010262 | Neurokinin 1 Antagonists |
| FDA EPC | N0000175786 | Substance P/Neurokinin-1 Receptor Antagonist |
| FDA MoA | N0000182141 | Cytochrome P450 3A4 Inhibitors |
| FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
| FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
| CHEBI has role | CHEBI:50919 | antiemetico |
| CHEBI has role | CHEBI:55350 | neurokinin-1 receptor antagonists |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chemotherapy-induced nausea and vomiting | indication | 236084000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.9 | Basic |
| pKa2 | 3.35 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 300MG;EQ 0.5MG BASE | AKYNZEO | HELSINN HLTHCARE | N205718 | Oct. 10, 2014 | RX | CAPSULE | ORAL | 8623826 | Nov. 18, 2030 | USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY |
| 300MG;EQ 0.5MG BASE | AKYNZEO | HELSINN HLTHCARE | N205718 | Oct. 10, 2014 | RX | CAPSULE | ORAL | 9186357 | Nov. 18, 2030 | USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY |
| 300MG;EQ 0.5MG BASE | AKYNZEO | HELSINN HLTHCARE | N205718 | Oct. 10, 2014 | RX | CAPSULE | ORAL | 9943515 | Nov. 18, 2030 | USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY |
| 300MG;EQ 0.5MG BASE | AKYNZEO | HELSINN HLTHCARE | N205718 | Oct. 10, 2014 | RX | CAPSULE | ORAL | 10828297 | Dec. 17, 2030 | USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY |
| 300MG;EQ 0.5MG BASE | AKYNZEO | HELSINN HLTHCARE | N205718 | Oct. 10, 2014 | RX | CAPSULE | ORAL | 9271975 | Sept. 9, 2031 | USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF CANCER CHEMOTHERAPY, INCLUDING, BUT NOT LIMITED TO, HIGHLY EMETOGENIC CHEMOTHERAPY |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Substance-P receptor | GPCR | ANTAGONIST | Ki | 9.02 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| 7732P08TIR | UNII |
| D05152 | KEGG_DRUG |
| 4033795 | VUID |
| N0000191094 | NUI |
| 4033795 | VANDF |
| C1700730 | UMLSCUI |
| CHEBI:85155 | CHEBI |
| GAW | PDB_CHEM_ID |
| CHEMBL206253 | ChEMBL_ID |
| 6451149 | PUBCHEM_CID |
| DB09048 | DRUGBANK_ID |
| 8409 | INN_ID |
| C508854 | MESH_SUPPLEMENTAL_RECORD_UI |
| 5742 | IUPHAR_LIGAND_ID |
| 1552337 | RXNORM |
| 30612 | MMSL |
| d08299 | MMSL |
| 015714 | NDDF |
| 716123009 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| AKYNZEO | HUMAN PRESCRIPTION DRUG LABEL | 2 | 69639-101 | CAPSULE | 300 mg | ORAL | NDA | 26 sections |