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landiolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-adrenoreceptor antagonists | 1545 | 133242-30-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Landiolol (INN) is a drug which acts as a highly cardioselective, ultra short-acting beta blocker. It is used as an anti-arrhythmic agent.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| CL (Clearance) | 36.33 mL/min/kg | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
| Vd (Volume of distribution) | 0.24 L/kg | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK2,PDK4,PIK3CB,PRKDC,SIK2,TEK | 22 | |||
| kinase-selectivity-class | BRAF,CDK4 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 5, 2002 | PMDA | Ono Pharmaceutical Co., Ltd | |
| June 29, 2016 | EMA | AOP Orphan Pharmaceuticals AG |
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 | C07AB14 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective |
| FDA MoA | N0000009923 | Adrenergic beta1-Antagonists |
| FDA EPC | N0000175556 | beta-Adrenergic Blocker |
| MeSH PA | D000319 | Adrenergic beta-Antagonists |
| MeSH PA | D000889 | Anti-Arrhythmia Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| CHEBI has role | CHEBI:38070 | anti-arrhythmia drug |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C07AB Beta blocking agents, selective 13 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Atrial flutter | indication | 5370000 | |
| Tachyarrhythmia | indication | 6285003 | |
| Supraventricular tachycardia | indication | 6456007 | |
| Sinus tachycardia | indication | 11092001 | |
| Atrial fibrillation | indication | 49436004 | DOID:0060224 |
| Ventricular fibrillation | indication | 71908006 | |
| Hemodynamically unstable ventricular tachycardia | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.78 | acidic |
| pKa2 | 7.77 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 280MG BASE/VIAL | RAPIBLYK | AOP HLTH US | N217202 | Nov. 22, 2024 | RX | POWDER | INTRAVENOUS | 10722516 | April 25, 2034 | A METHOD OF REDUCING THE HEART RATE OF A SUBJECT SUFFERING FROM SUPRAVENTRICULAR TACHYCARDIA, WHEREIN LANDIOLOL IS ADMINISTERED PARENTERALLY AT A CONSTANT DOSE OF MORE THAN 20 MCG/KG/MIN FOR 2-20 HOURS, WHEREIN THE DOSE IS NOT HIGHER THAN 40 MCG/KG/MIN |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 280MG BASE/VIAL | RAPIBLYK | AOP HLTH US | N217202 | Nov. 22, 2024 | RX | POWDER | INTRAVENOUS | Feb. 13, 2029 | NEW PATIENT POPULATION |
| EQ 280MG BASE/VIAL | RAPIBLYK | AOP HLTH US | N217202 | Nov. 22, 2024 | RX | POWDER | INTRAVENOUS | Nov. 22, 2029 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | GPCR | ANTAGONIST | Ki | 7 | IUPHAR | KEGG DRUG |
External reference:
| ID | Source |
|---|---|
| D01847 | KEGG_DRUG |
| 4043836 | VANDF |
| C0905464 | UMLSCUI |
| CHEBI:135809 | CHEBI |
| CHEMBL1742466 | ChEMBL_ID |
| CHEMBL2362410 | ChEMBL_ID |
| DB12212 | DRUGBANK_ID |
| C077049 | MESH_SUPPLEMENTAL_RECORD_UI |
| 13192 | IUPHAR_LIGAND_ID |
| 7516 | INN_ID |
| 144481-98-1 | SECONDARY_CAS_RN |
| 62NWQ924LH | UNII |
| 114905 | PUBCHEM_CID |
| 2712069 | RXNORM |
| 36344 | MMSL |
| 43557 | MMSL |
| d09185 | MMSL |
| 017430 | NDDF |
| 017431 | NDDF |
| 1084141000202107 | SNOMEDCT_US |
| 1084181000202102 | SNOMEDCT_US |
| 62NWQ924LH | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| RAPIBLYK | HUMAN PRESCRIPTION DRUG LABEL | 1 | 84381-110 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 280 mg | INTRAVENOUS | NDA | 27 sections |
| RAPIBLYK | HUMAN PRESCRIPTION DRUG LABEL | 1 | 87073-110 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 280 mg | INTRAVENOUS | NDA | 26 sections |