NAV

Tedisamil

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

Identification

Generic Name
Tedisamil
DrugBank Accession Number
DB06200
Background

Tedisamil (planned trade name Pulzium) is an investigational drug for atrial fibrillation and atrial flutter. It is currently being developed by Solvay and is currently under regulatory review by the United States Food and Drug Administration.

Type
Small Molecule
Groups
Investigational
Structure
3D
Similar Structures
Weight
Average: 288.4708
Monoisotopic: 288.256549034
Chemical Formula
C19H32N2
Synonyms
  • Tedisamil
External IDs
  • KC-8857
  • KC8857
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Pharmacology

Indication

Investigated for use/treatment in arrhythmia, atrial fibrillation, and angina.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

It is hypothesized tedisamil prevents Ca2+ overload by the cAMP dependent SR Ca2+ uptake [PMID: 10707827].

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
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Toxicity

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
Integrate drug-drug
interactions in your software
AcebutololAcebutolol may increase the arrhythmogenic activities of Tedisamil.
AcetyldigitoxinAcetyldigitoxin may increase the arrhythmogenic activities of Tedisamil.
AcrivastineThe risk or severity of QTc prolongation can be increased when Acrivastine is combined with Tedisamil.
AdenosineAdenosine may increase the arrhythmogenic activities of Tedisamil.
AjmalineAjmaline may increase the arrhythmogenic activities of Tedisamil.
Food Interactions
Not Available

Products

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International/Other Brands
Pulzium

Categories

ATC Codes
C01BD06 — Tedisamil
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as azaspirodecane derivatives. These are organic compounds containing a spirodecane moiety with at least one nitrogen atom.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Azaspirodecane derivatives
Sub Class
Not Available
Direct Parent
Azaspirodecane derivatives
Alternative Parents
Piperidines / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Aliphatic heteropolycyclic compound / Amine / Azacycle / Azaspirodecane / Hydrocarbon derivative / Organic nitrogen compound / Organonitrogen compound / Organopnictogen compound / Piperidine / Tertiary aliphatic amine
Molecular Framework
Aliphatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
A5VAY2U3R8
CAS number
90961-53-8
InChI Key
CTIRHWCPXYGDGF-UHFFFAOYSA-N
InChI
InChI=1S/C19H32N2/c1-2-8-19(7-1)17-11-20(9-15-3-4-15)12-18(19)14-21(13-17)10-16-5-6-16/h15-18H,1-14H2
IUPAC Name
3,7-bis(cyclopropylmethyl)-3,7-diazaspiro[bicyclo[3.3.1]nonane-9,1'-cyclopentane]
SMILES
C(C1CC1)N1CC2CN(CC3CC3)CC(C1)C21CCCC1

References

General References
  1. Manoach M, Varon D, Tribulova N, Zinman T, Kaplan D, Khananshvili D, Shainberg A: The role of sarcoplasmic reticulum in the protective effect of class III drugs against Ca2+ overload. Gen Physiol Biophys. 1999 Dec;18 Suppl 1:19-25. [Article]
PubChem Compound
65825
ChemSpider
59237
BindingDB
50088367
ChEMBL
CHEMBL113461
Wikipedia
Tedisamil

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0214 mg/mLALOGPS
logP3.54ALOGPS
logP2.78Chemaxon
logS-4.1ALOGPS
pKa (Strongest Basic)9.26Chemaxon
Physiological Charge2Chemaxon
Hydrogen Acceptor Count2Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area6.48 Å2Chemaxon
Rotatable Bond Count4Chemaxon
Refractivity88.51 m3·mol-1Chemaxon
Polarizability35.7 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9531
Blood Brain Barrier+0.9902
Caco-2 permeable+0.5654
P-glycoprotein substrateSubstrate0.5855
P-glycoprotein inhibitor IInhibitor0.5632
P-glycoprotein inhibitor IIInhibitor0.7142
Renal organic cation transporterInhibitor0.6926
CYP450 2C9 substrateNon-substrate0.8756
CYP450 2D6 substrateNon-substrate0.5146
CYP450 3A4 substrateNon-substrate0.6512
CYP450 1A2 substrateNon-inhibitor0.9246
CYP450 2C9 inhibitorNon-inhibitor0.9269
CYP450 2D6 inhibitorNon-inhibitor0.7712
CYP450 2C19 inhibitorNon-inhibitor0.8482
CYP450 3A4 inhibitorInhibitor0.5997
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6721
Ames testNon AMES toxic0.5268
CarcinogenicityNon-carcinogens0.9445
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7945 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.781
hERG inhibition (predictor II)Inhibitor0.5367
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-0a4m-5090000000-de8bc4d98d09ff7cfe72
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0090000000-59a9762dd930cb32205e
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-000i-0090000000-91b0bfc74b84f9e26f25
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0090000000-3fb63cfa43769486535b
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-000i-0090000000-9eabda7cbb8314cad4a0
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-000t-1090000000-72ba46b5b9e56fe50c8d
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-0940000000-fc664831753866749fba
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-180.606308
predicted
DarkChem Lite v0.1.0
[M-H]-171.39803
predicted
DeepCCS 1.0 (2019)
[M+H]+180.617308
predicted
DarkChem Lite v0.1.0
[M+H]+173.75604
predicted
DeepCCS 1.0 (2019)
[M+Na]+181.518108
predicted
DarkChem Lite v0.1.0
[M+Na]+179.8492
predicted
DeepCCS 1.0 (2019)

Drug created at March 19, 2008 16:17 / Updated at February 21, 2021 18:52