Stem definition | Drug id | CAS RN |
---|---|---|
neurokinin NK1 (substance P) receptor antagonist | 4898 | 290297-26-6 |
None
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Oct. 10, 2014 | FDA | HELSINN HLTHCARE |
None
None
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 |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Chemotherapy-induced nausea and vomiting | indication | 236084000 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 8.9 | Basic |
pKa2 | 3.35 | Basic |
None
None
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 |
ID | Source |
---|---|
D05152 | KEGG_DRUG |
4033795 | VUID |
N0000191094 | NUI |
4033795 | VANDF |
C1700730 | UMLSCUI |
CHEBI:85155 | CHEBI |
GAW | PDB_CHEM_ID |
CHEMBL206253 | ChEMBL_ID |
DB09048 | DRUGBANK_ID |
C508854 | MESH_SUPPLEMENTAL_RECORD_UI |
5742 | IUPHAR_LIGAND_ID |
8409 | INN_ID |
7732P08TIR | UNII |
6451149 | PUBCHEM_CID |
1552337 | RXNORM |
30612 | MMSL |
d08299 | MMSL |
015714 | NDDF |
716123009 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
AKYNZEO | HUMAN PRESCRIPTION DRUG LABEL | 2 | 69639-101 | CAPSULE | 300 mg | ORAL | NDA | 26 sections |