Tedisamil
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This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
Explore a selection of our essential drug information below, or:
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
- Weight
- Average: 288.4708
Monoisotopic: 288.256549034 - Chemical Formula
- C19H32N2
- Synonyms
- Tedisamil
- External IDs
- KC-8857
- KC8857
Pharmacology
- Indication
Investigated for use/treatment in arrhythmia, atrial fibrillation, and angina.
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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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcebutolol Acebutolol may increase the arrhythmogenic activities of Tedisamil. Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Tedisamil. Acrivastine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Tedisamil. Adenosine Adenosine may increase the arrhythmogenic activities of Tedisamil. Ajmaline Ajmaline may increase the arrhythmogenic activities of Tedisamil. - Food Interactions
- Not Available
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- 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
- 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]
- External Links
- PubChem Compound
- 65825
- ChemSpider
- 59237
- BindingDB
- 50088367
- ChEMBL
- CHEMBL113461
- Wikipedia
- Tedisamil
Clinical Trials
- Clinical Trials
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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
Property Value Source Water Solubility 0.0214 mg/mL ALOGPS logP 3.54 ALOGPS logP 2.78 Chemaxon logS -4.1 ALOGPS pKa (Strongest Basic) 9.26 Chemaxon Physiological Charge 2 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 6.48 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 88.51 m3·mol-1 Chemaxon Polarizability 35.7 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9531 Blood Brain Barrier + 0.9902 Caco-2 permeable + 0.5654 P-glycoprotein substrate Substrate 0.5855 P-glycoprotein inhibitor I Inhibitor 0.5632 P-glycoprotein inhibitor II Inhibitor 0.7142 Renal organic cation transporter Inhibitor 0.6926 CYP450 2C9 substrate Non-substrate 0.8756 CYP450 2D6 substrate Non-substrate 0.5146 CYP450 3A4 substrate Non-substrate 0.6512 CYP450 1A2 substrate Non-inhibitor 0.9246 CYP450 2C9 inhibitor Non-inhibitor 0.9269 CYP450 2D6 inhibitor Non-inhibitor 0.7712 CYP450 2C19 inhibitor Non-inhibitor 0.8482 CYP450 3A4 inhibitor Inhibitor 0.5997 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.6721 Ames test Non AMES toxic 0.5268 Carcinogenicity Non-carcinogens 0.9445 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.7945 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.781 hERG inhibition (predictor II) Inhibitor 0.5367
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-0a4m-5090000000-de8bc4d98d09ff7cfe72 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-000i-0090000000-59a9762dd930cb32205e Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-000i-0090000000-91b0bfc74b84f9e26f25 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-000i-0090000000-3fb63cfa43769486535b Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-000i-0090000000-9eabda7cbb8314cad4a0 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-000t-1090000000-72ba46b5b9e56fe50c8d Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-004i-0940000000-fc664831753866749fba Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 180.606308 predictedDarkChem Lite v0.1.0 [M-H]- 171.39803 predictedDeepCCS 1.0 (2019) [M+H]+ 180.617308 predictedDarkChem Lite v0.1.0 [M+H]+ 173.75604 predictedDeepCCS 1.0 (2019) [M+Na]+ 181.518108 predictedDarkChem Lite v0.1.0 [M+Na]+ 179.8492 predictedDeepCCS 1.0 (2019)
Drug created at March 19, 2008 16:17 / Updated at February 21, 2021 18:52