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nilvadipine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| calcium channel blockers, nifedipine derivatives | 1934 | 75530-68-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 8 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.00 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.92 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 14 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.579 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.055 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 28.973 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 85.901 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.620 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 3.760 | % | High | 1 |
| herg | hERG pIC50 | 4.914 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 112.202 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 191.426 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.720 | % | High | 1 |
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK1,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKDC,STK33,TEK,TTK,ZAP70 | 39 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,DYRK1B,GRK2,MAPK7,PDK4,PIK3CD,PRKDC,STK33,TEK | 11 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.882 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 142.233 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.080 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 8.872 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.68 | |
| pppb | Pig plasma protein binding (% unbound) | 2.660 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 201.372 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 25.010 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 1.710 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 20.701 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1992 | YEAR INTRODUCED |
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 | C08CA10 | CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS Dihydropyridine derivatives |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C08CA Dihydropyridine derivatives 17 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 1.64 | Basic |
Orange Book patent data (new drug applications)
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Voltage-gated L-type calcium channel | Ion channel | BLOCKER | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||||
| Voltage-dependent calcium channel gamma-1 subunit | Ion channel | WOMBAT-PK | |||||||
| Voltage-dependent L-type calcium channel subunit alpha-1C | Ion channel | WOMBAT-PK | |||||||
| Voltage-dependent L-type calcium channel subunit alpha-1D | Ion channel | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| D01908 | KEGG_DRUG |
| C0132512 | UMLSCUI |
| CHEBI:31911 | CHEBI |
| CHEMBL517427 | ChEMBL_ID |
| DB06712 | DRUGBANK_ID |
| C035100 | MESH_SUPPLEMENTAL_RECORD_UI |
| 4494 | PUBCHEM_CID |
| 10160 | IUPHAR_LIGAND_ID |
| 5459 | INN_ID |
| 0214FUT37J | UNII |
| 53692 | RXNORM |
| 006271 | NDDF |
| 713436005 | SNOMEDCT_US |
Pharmaceutical products:
None