Landiolol

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Name
Landiolol
Accession Number
DB12212
Description

Landiolol has been used in trials studying the treatment of Pharmacokinetics/Dynamics Study.

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 509.6
Monoisotopic: 509.273715228
Chemical Formula
C25H39N3O8
Synonyms
  • Landiolol
  • Landiololum
External IDs
  • AOP-200704
  • AOP200704
  • LDLL-600
  • LDLL600
  • ONO 1101
  • ONO-1101

Pharmacology

Indication
Not Available
Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics
Not Available
Mechanism of action
Not Available
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life
Not Available
Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbataceptThe metabolism of Landiolol can be increased when combined with Abatacept.
AbirateroneThe metabolism of Landiolol can be decreased when combined with Abiraterone.
AcebutololAcebutolol may increase the arrhythmogenic activities of Landiolol.
AceclofenacThe therapeutic efficacy of Landiolol can be decreased when used in combination with Aceclofenac.
AcemetacinThe therapeutic efficacy of Landiolol can be decreased when used in combination with Acemetacin.
AcetaminophenThe metabolism of Landiolol can be decreased when combined with Acetaminophen.
AcetyldigitoxinLandiolol may increase the arrhythmogenic activities of Acetyldigitoxin.
Acetylsalicylic acidAcetylsalicylic acid may decrease the antihypertensive activities of Landiolol.
AdalimumabThe metabolism of Landiolol can be increased when combined with Adalimumab.
AdenosineAdenosine may increase the arrhythmogenic activities of Landiolol.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

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Food Interactions
Not Available

Products

Product Ingredients
IngredientUNIICASInChI Key
Landiolol HydrochlorideG8HQ634Y17144481-98-1DLPGJHSONYLBKP-IKGOIYPNSA-N

Categories

ATC Codes
C07AB14 — Landiolol
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as morpholine carboxylic acids and derivatives. These are heterocyclic compounds containing a morpholine ring substituted by one or more carboxylic acid groups (or derivative thereof).
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Oxazinanes
Sub Class
Morpholines
Direct Parent
Morpholine carboxylic acids and derivatives
Alternative Parents
Phenoxy compounds / Phenol ethers / Ketals / Alkyl aryl ethers / Fatty acid esters / 1,3-dioxolanes / Ureas / Secondary alcohols / 1,2-aminoalcohols / Carboxylic acid esters
show 10 more
Substituents
1,2-aminoalcohol / Acetal / Alcohol / Alkyl aryl ether / Amine / Amino acid or derivatives / Aromatic heteromonocyclic compound / Azacycle / Benzenoid / Carbonic acid derivative
show 26 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available

Chemical Identifiers

UNII
62NWQ924LH
CAS number
133242-30-5
InChI Key
WMDSZGFJQKSLLH-RBBKRZOGSA-N
InChI
InChI=1S/C25H39N3O8/c1-25(2)35-18-22(36-25)17-34-23(30)8-5-19-3-6-21(7-4-19)33-16-20(29)15-26-9-10-27-24(31)28-11-13-32-14-12-28/h3-4,6-7,20,22,26,29H,5,8-18H2,1-2H3,(H,27,31)/t20-,22+/m0/s1
IUPAC Name
[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl 3-{4-[(2S)-2-hydroxy-3-({2-[(morpholine-4-carbonyl)amino]ethyl}amino)propoxy]phenyl}propanoate
SMILES
CC1(C)OC[[email protected]@H](COC(=O)CCC2=CC=C(OC[[email protected]@H](O)CNCCNC(=O)N3CCOCC3)C=C2)O1

References

General References
  1. BASG Product Information: Rapibloc (landiolol hydrochloride) for infusion [Link]
PubChem Compound
114905
PubChem Substance
347828494
ChemSpider
102855
ChEBI
135809
ChEMBL
CHEMBL1742466
ZINC
ZINC000003929810
Wikipedia
Landiolol

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4RecruitingTreatmentAtrial Fibrillation (AF) / Surgery, Cardiac1
3CompletedDiagnosticCoronary Artery Disease (CAD)1
3CompletedTreatmentAtrial Fibrillation (AF)1
2CompletedDiagnosticCoronary Artery Disease (CAD)2
2CompletedTreatmentHealthy Volunteers / Pharmacokinetics/Dynamics Study1
2CompletedTreatmentPostoperative Supraventricular Tachyarrythmia1
2, 3CompletedTreatmentPostoperative Supraventricular Tachyarrythmia1
1CompletedTreatmentHealthy Volunteers1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solution, concentrateIntravenous20 mg/2ml
Injection, powder, for solutionIntravenous300 mg
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.334 mg/mLALOGPS
logP0.44ALOGPS
logP0.35ChemAxon
logS-3.2ALOGPS
pKa (Strongest Acidic)14.04ChemAxon
pKa (Strongest Basic)8.79ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area127.82 Å2ChemAxon
Rotatable Bond Count14ChemAxon
Refractivity131.29 m3·mol-1ChemAxon
Polarizability56.5 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Sternieri E, Coccia CP, Pinetti D, Guerzoni S, Ferrari A: Pharmacokinetics and interactions of headache medications, part II: prophylactic treatments. Expert Opin Drug Metab Toxicol. 2006 Dec;2(6):981-1007. doi: 10.1517/17425255.2.6.981 . [PubMed:17125412]
  2. Brodde OE, Kroemer HK: Drug-drug interactions of beta-adrenoceptor blockers. Arzneimittelforschung. 2003;53(12):814-22. [PubMed:14732961]
  3. Iwaki M, Niwa T, Bandoh S, Itoh M, Hirose H, Kawase A, Komura H: Application of substrate depletion assay to evaluation of CYP isoforms responsible for stereoselective metabolism of carvedilol. Drug Metab Pharmacokinet. 2016 Dec;31(6):425-432. doi: 10.1016/j.dmpk.2016.08.007. Epub 2016 Sep 2. [PubMed:27836712]

Drug created on October 20, 2016 15:37 / Updated on October 21, 2020 05:27

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