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phenoxybenzamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2136 | 59-96-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 30 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 2.82 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 25 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 15 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 | 5.138 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.324 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 9.954 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 60.954 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.120 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.430 | % | High | 1 |
| herg | hERG pIC50 | 5.392 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 178.238 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 291.072 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.180 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K7,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,TEK,TGFBR1 | 35 | |||
| kinase-selectivity-class | AKT3,AXL,BRAF,EIF2AK3,ERBB2,GRK2,PDK4,SIK2 | 8 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.022 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 272.270 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.290 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.061 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.270 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 291.743 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 1.810 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.150 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 0.731 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 26, 1953 | FDA | COVIS PHARMA SARL |
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 | C04AX02 | CARDIOVASCULAR SYSTEM PERIPHERAL VASODILATORS PERIPHERAL VASODILATORS Other peripheral vasodilators |
| FDA MoA | N0000000099 | Adrenergic alpha-Antagonists |
| FDA EPC | N0000175553 | alpha-Adrenergic Blocker |
| MeSH PA | D000317 | Adrenergic alpha-Antagonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
C04AX Other peripheral vasodilators 16 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pheochromocytoma | indication | 302835009 | |
| Acute cerebrovascular insufficiency | contraindication | 29322000 | |
| Low blood pressure | contraindication | 45007003 | |
| Lower respiratory tract infection | contraindication | 50417007 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Disorder of coronary artery | contraindication | 414024009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.86 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | GPCR | ANTAGONIST | IC50 | 6.28 | WOMBAT-PK | CHEMBL | |||
| Alpha-1A adrenergic receptor | GPCR | ANTAGONIST | IC50 | 7.27 | WOMBAT-PK | CHEMBL | |||
| Alpha-2B adrenergic receptor | GPCR | ANTAGONIST | Ki | 8.46 | PDSP | CHEMBL | |||
| Alpha-1D adrenergic receptor | GPCR | ANTAGONIST | Ki | 8.40 | IUPHAR | ||||
| Solute carrier family 22 member 1 | Transporter | IC50 | 4.82 | CHEMBL | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 4.35 | CHEMBL | |||||
| Dopamine receptor | GPCR | Ki | 6.92 | CHEMBL | |||||
| Adrenergic receptor alpha-1 | GPCR | Ki | 8.74 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019890 | VUID |
| N0000147975 | NUI |
| D00507 | KEGG_DRUG |
| 63-92-3 | SECONDARY_CAS_RN |
| 4018006 | VANDF |
| 4019890 | VANDF |
| C0031441 | UMLSCUI |
| CHEBI:8077 | CHEBI |
| CHEMBL753 | ChEMBL_ID |
| DB00925 | DRUGBANK_ID |
| CHEMBL1200787 | ChEMBL_ID |
| D010643 | MESH_DESCRIPTOR_UI |
| 4768 | PUBCHEM_CID |
| 7268 | IUPHAR_LIGAND_ID |
| 608 | INN_ID |
| 0TTZ664R7Z | UNII |
| 203778 | RXNORM |
| 3842 | MMSL |
| 5276 | MMSL |
| 71910 | MMSL |
| d00734 | MMSL |
| 001843 | NDDF |
| 004738 | NDDF |
| 372838003 | SNOMEDCT_US |
| 44293009 | SNOMEDCT_US |
| 74771007 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| PHENOXYBENZAMINE HYDROCHLORIDE | Human Prescription Drug Label | 1 | 35573-473 | CAPSULE | 10 mg | ORAL | ANDA | 17 sections |
| PHENOXYBENZAMINE HYDROCHLORIDE | Human Prescription Drug Label | 1 | 59651-327 | CAPSULE | 10 mg | ORAL | ANDA | 17 sections |
| Phenoxybenzamine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-1502 | CAPSULE | 10 mg | ORAL | ANDA | 18 sections |
| Phenoxybenzamine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1502 | CAPSULE | 10 mg | ORAL | ANDA | 18 sections |
| Phenoxybenzamine Hydrochloride | Human Prescription Drug Label | 1 | 70954-365 | CAPSULE | 10 mg | ORAL | ANDA | 19 sections |
| PHENOXYBENZAMINE HYDROCHLORIDE | Human Prescription Drug Label | 1 | 72603-229 | CAPSULE | 10 mg | ORAL | ANDA | 17 sections |