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| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals neuraminidase inhibitors | 4823 | 330600-85-6 |
| Dose | Unit | Route |
|---|---|---|
| 0.60 | g | P |
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Hosey CM, Chan R, Benet LZ |
| fu (Fraction unbound in plasma) | 1 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
| CL (Clearance) | 1.46 mL/min/kg | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
| BA (Bioavailability) | 0 % |
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK2,JAK3,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PLK1,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 46 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,MAP2K6,TEK | 5 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 13, 2018 | EMA | BIOCRYST UK LIMITED | |
| Dec. 19, 2014 | FDA | BIOCRYST |
None
None
None
None
| Source | Code | Description |
|---|---|---|
| ATC | J05AH03 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Neuraminidase inhibitors |
| FDA MoA | N0000175436 | Neuraminidase Inhibitors |
| FDA EPC | N0000175524 | Neuraminidase Inhibitor |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000998 | Antiviral Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| CHEBI has role | CHEBI:36044 | antiviral drug |
| CHEBI has role | CHEBI:52425 | EC 3.2.1.18 (<i>exo</i>-α-sialidase) inhibitor |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Influenza | indication | 6142004 | DOID:8469 |
None
None
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.6 | acidic |
| pKa2 | 12.05 | acidic |
| pKa3 | 13.73 | acidic |
| pKa4 | 10.07 | Basic |
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 200MG/20ML (10MG/ML) | RAPIVAB | BIOCRYST | N206426 | Dec. 19, 2014 | RX | SOLUTION | INTRAVENOUS | 10391075 | Feb. 12, 2027 | TREATMENT OF ACUTE UNCOMPLICATED INFLUENZA IN PATIENTS 2 YEARS AND OLDER |
| 200MG/20ML (10MG/ML) | RAPIVAB | BIOCRYST | N206426 | Dec. 19, 2014 | RX | SOLUTION | INTRAVENOUS | 10391075 | Feb. 12, 2027 | TREATMENT OF ACUTE UNCOMPLICATED INFLUENZA IN PATIENTS 6 MONTHS AND OLDER |
| 200MG/20ML (10MG/ML) | RAPIVAB | BIOCRYST | N206426 | Dec. 19, 2014 | RX | SOLUTION | INTRAVENOUS | 8778997 | May 7, 2027 | TREATMENT OF ACUTE UNCOMPLICATED INFLUENZA IN ADULTS |
| 200MG/20ML (10MG/ML) | RAPIVAB | BIOCRYST | N206426 | Dec. 19, 2014 | RX | SOLUTION | INTRAVENOUS | 8778997 | May 7, 2027 | TREATMENT OF ACUTE UNCOMPLICATED INFLUENZA IN PATIENTS 2 YEARS AND OLDER |
| 200MG/20ML (10MG/ML) | RAPIVAB | BIOCRYST | N206426 | Dec. 19, 2014 | RX | SOLUTION | INTRAVENOUS | 8778997 | May 7, 2027 | TREATMENT OF ACUTE UNCOMPLICATED INFLUENZA IN PATIENTS 6 MONTHS AND OLDER |
None
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sialidase 2 | Enzyme | Ki | 4.25 | CHEMBL | |||||
| Neuraminidase | Enzyme | INHIBITOR | IC50 | 8.85 | CHEMBL | DRUG LABEL | |||
| Neuraminidase | Enzyme | INHIBITOR | IC50 | 8.30 | CHEMBL | DRUG LABEL | |||
| Neuraminidase | Enzyme | INHIBITOR | Ki | 9.08 | CHEMBL | DRUG LABEL | |||
| Neuraminidase | Enzyme | IC50 | 9.40 | CHEMBL | |||||
| Neuraminidase | Enzyme | IC50 | 10.15 | CHEMBL | |||||
| Neuraminidase | Enzyme | IC50 | 8.70 | CHEMBL | |||||
| Neuraminidase | Enzyme | IC50 | 7.03 | CHEMBL | |||||
| Sialidase | Enzyme | IC50 | 4.40 | CHEMBL | |||||
| Neuraminidase | Enzyme | IC50 | 9.52 | CHEMBL |
| ID | Source |
|---|---|
| D03829 | KEGG_DRUG |
| 1041434-82-5 | SECONDARY_CAS_RN |
| 4034033 | VANDF |
| CHEBI:85196 | CHEBI |
| BCZ | PDB_CHEM_ID |
| CHEMBL3989402 | ChEMBL_ID |
| CHEMBL139367 | ChEMBL_ID |
| C414210 | MESH_SUPPLEMENTAL_RECORD_UI |
| DB06614 | DRUGBANK_ID |
| 1598078 | RXNORM |
| 231961 | MMSL |
| 30814 | MMSL |
| d08335 | MMSL |
| 013296 | NDDF |
| 716121006 | SNOMEDCT_US |
| 763542005 | SNOMEDCT_US |
| C1675326 | UMLSCUI |
| 154234 | PUBCHEM_CID |
| QW7Y7ZR15U | UNII |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Rapivab | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61364-181 | SOLUTION | 600 mg | INTRAVENOUS | NDA | 27 sections |
| Rapivab | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72769-181 | SOLUTION | 600 mg | INTRAVENOUS | NDA | 30 sections |