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quinupristin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibacterials, streptogramins, protein-synthesis inhibitors, pristinamycin derivatives | 2349 | 120138-50-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
component of RP 59500
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.50 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 3.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 4.40 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.67 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 16 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.34 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.87 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.00 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.994 | Moderate | 0.69 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 27.542 | Moderate | 0.69 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.579 | 10^-6 cm/s | Moderate | 0.69 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.105 | uL/min/10^6 cells | Moderate | 0.69 |
| dppb | Dog plasma protein binding (% unbound) | 28.900 | % | Moderate | 0.69 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 27.680 | % | Moderate | 0.69 |
| herg | hERG pIC50 | 4.704 | pIC50 | Moderate | 0.69 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.315 | uL/min/10^6 cells | Moderate | 0.69 |
| hlm-clint | Human liver microsomal intrinsic clearance | 5.649 | uL/min/mg protein | Moderate | 0.69 |
| hppb | Human plasma protein binding (% unbound) | 38.470 | % | Moderate | 0.69 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,PDK1,PDK2,PDK4,PRKDC,TEK | 17 | |||
| kinase-selectivity-class | GRK2 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 9.162 | Moderate | 0.69 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 9.528 | Moderate | 0.69 | |
| mppb | Mouse plasma protein binding (% unbound) | 25.610 | Moderate | 0.69 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 28.708 | Moderate | 0.69 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 38.090 | % | Moderate | 0.69 |
| rh-clint | Rat hepatocyte intrinsic clearance | 4.169 | uL/min/10^6 cells | Moderate | 0.69 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 60.270 | % | Moderate | 0.69 |
| rppb | Rat plasma protein binding (% unbound) | 31.870 | % | Moderate | 0.69 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 688.652 | uM | Moderate | 0.69 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 21, 1999 | FDA |
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 |
|---|---|---|
| ATC | J01FG02 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE MACROLIDES, LINCOSAMIDES AND STREPTOGRAMINS Streptogramins |
| FDA CS | M0022748 | Streptogramins |
| FDA EPC | N0000175502 | Streptogramin Antibacterial |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
Related Drugs by ATC class:
J01FG Streptogramins 2 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Vancomycin resistant enterococcus | indication | 113727004 | |
| Streptococcus pyogenes infection | indication | 302809008 | |
| Complicated Skin and Skin Structure Staphylococcus Aureus Infection | indication | ||
| Pyrexia of unknown origin | off-label use | 7520000 | |
| Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Pseudomembranous enterocolitis | contraindication | 397683000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.19 | acidic |
| pKa2 | 8.42 | Basic |
| pKa3 | 4.85 | Basic |
| pKa4 | 2.23 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
None
External reference:
| ID | Source |
|---|---|
| 4021184 | VUID |
| N0000179688 | NUI |
| D00852 | KEGG_DRUG |
| 4021184 | VANDF |
| C0756081 | UMLSCUI |
| CHEBI:8732 | CHEBI |
| H8Q | PDB_CHEM_ID |
| CHEMBL1200649 | ChEMBL_ID |
| DB01369 | DRUGBANK_ID |
| C113825 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10798 | IUPHAR_LIGAND_ID |
| 6582 | INN_ID |
| 23OW28RS7P | UNII |
| 5388937 | PUBCHEM_CID |
| 229367 | RXNORM |
| 8299 | MMSL |
| d04455 | MMSL |
| 007887 | NDDF |
| 116110009 | SNOMEDCT_US |
| 387015002 | SNOMEDCT_US |
| 441592000 | SNOMEDCT_US |
Pharmaceutical products:
None