TEDISAMIL

Details

Stereochemistry	ACHIRAL
Molecular Formula	C19H32N2
Molecular Weight	288.4708
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

C(C1CC1)N2CC3CN(CC4CC4)CC(C2)C35CCCC5

InChI

InChIKey=CTIRHWCPXYGDGF-UHFFFAOYSA-N

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

HIDE SMILES / InChI

Description
Sources: https://www.fdanews.com/articles/102230-advisory-committee-recommends-no-approval-for-pulzium?v=preview | https://clinicaltrials.gov/ct2/show/NCT00126061 | http://www.mhra.gov.uk/home/groups/par/documents/websiteresources/con031129.pdf | https://www.ncbi.nlm.nih.gov/pubmed/14996649 | https://www.ncbi.nlm.nih.gov/pubmed/11527020

Tedisamil is an antiarrhythmic with additional anti-ischaemic properties, which acts via potassium channel blockade. This drug can be categorised as a class III antiarrhythmic agent due to its effects of action potential and QT interval prolongation in these patients. Although tedisamil has been shown to be an effective anti-ischaemic agent, with Phase III trials for angina pectoris now completed, the company are now pursuing the use of tedisamil for the treatment of atrial fibrillation, for which tedisamil is still in Phase II/III clinical trials. The FDA’s Cardiovascular and Renal Drugs Advisory Committee voted not to recommend approval for Solvay Pharmaceuticals’ investigational anti-arrhythmic drug Pulzium (Tedisamil) and asked the company to give the FDA more information.

Originator

Approval Year

PubMed

Title	Date	PubMed
Tedisamil and dofetilide-induced torsades de pointes, rate and potassium dependence.	2001 Apr	11264243
Tedisamil blocks BK-type Ca(2+)-dependent K(+) channels and modulates action potentials in rat hippocampal neurons.	2002 Feb 15	11825675
Atrial fibrillation: emerging possibilities for drug treatment: an overview of current opportunities and recent developments.	2003 Jun	12746746
Trial finds new anti-arrhythmic, tedisamil, is superior to placebo for converting recent onset atrial fibrillation or atrial flutter.	2004 Dec	16379966
Effect of the antifibrillatory compound tedisamil (KC-8857) on transmembrane currents in mammalian ventricular myocytes.	2004 Dec	15579009
Theoretical possibilities for the development of novel antiarrhythmic drugs.	2004 Jan	14754422
Electrical storms in Brugada syndrome: review of pharmacologic and ablative therapeutic options.	2005 Jan 1	16943940
Do we need pharmacological therapy for atrial fibrillation in the ablation era?	2006 Dec	17340189
New horizons in antiarrhythmic therapy: will novel agents overcome current deficits?	2008 Sep 22	18790110
Atrial fibrillation: from ion channels to bedside treatment options.	2009 Nov-Dec	19520377

Sample Use Guides

In Vivo Use Guide

The recommended dose is 0.32 mg/kg

Route of Administration: Intravenous

Name

Type

Language

TEDISAMIL

Official Name

English

3',7'-BIS(CYCLOPROPYLMETHYL)SPIRO(CYCLOPENTANE-1,9'-(3,7)DIAZABICYCLO(3.3.1)NONANE)

Common Name

English

TEDISAMIL [USAN]

Common Name

English

TEDISAMIL [MI]

Common Name

English

Tedisamil [WHO-DD]

Common Name

English

KC8857

Code

English

TEDISAMIL [MART.]

Common Name

English

SPIRO(CYCLOPENTANE-1,9'-(3,7)DIAZABICYCLO(3.3.1)NONANE), 3',7'-BIS(CYCLOPROPYLMETHYL)-

Common Name

English

tedisamil [INN]

Common Name

English

KC-8857

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C47793