The discovery of the selective I(f) current inhibitor ivabradine. A new therapeutic approach to ischemic heart disease

Pharmacological Research : the Official Journal of the Italian Pharmacological Society
J P Vilaine

Abstract

Coronary artery disease is still a major cause of morbidity and mortality in the industrialized countries, despite the advances in pharmacological treatments, risk factor control and the beneficial effect of myocardial revascularization procedures. Medical anti-ischemic treatment is still essential in most patients, but should be improved in terms of efficacy and tolerance to ensure better prevention of mortality and improvement of the quality of life and symptom control. Since increased heart rate plays a major role in coronary artery disease, not only as a trigger of most of the ischemic episodes but also as an independent predictor of mortality, inhibition of the pacemaker I(f) current to induce a direct and selective decrease in heart rate represents an attractive therapeutic approach for coronary artery disease. The screening of original benzocycloalkane compounds, at Servier Research Institute, has led to the selection of ivabradine for clinical development. Preclinical data showed that ivabradine inhibits the I(f) current of the sinus node, induces a selective reduction in heart rate, both at rest and during exercise, preserves myocardial contractility, atrio-ventricular conduction and ventricular repolarization. Ivabrad...Continue Reading

Citations

Feb 2, 2008·International Urology and Nephrology·K StamatiouE Skoumbourdis
Jul 10, 2009·Cardiovascular Research·Eric Thorin, Nathalie Thorin-Trescases
Jan 28, 2012·American Journal of Veterinary Research·Sabine C RiesenJohn D Bonagura
Feb 19, 2014·Clinical Research in Cardiology : Official Journal of the German Cardiac Society·Ulrich Fischer-RasokatIoakim Spyridopoulos
Oct 16, 2012·Clinical Research in Cardiology : Official Journal of the German Cardiac Society·Vincenzo De SantisLuigi Tritapepe
Dec 22, 2015·Clinical Research in Cardiology : Official Journal of the German Cardiac Society·Ulrich Fischer-RasokatChristian W Hamm
May 27, 2016·Nature Reviews. Cardiology·Roberto Ferrari, Kim Fox
Jun 9, 2016·Expert Review of Cardiovascular Therapy·Andreas A GiannopoulosYiannis S Chatzizisis
Oct 13, 2009·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Alexandre SarreEric Raddatz
Jun 18, 2010·European Journal of Pharmacology·Jana Kmecova, Jan Klimas
Feb 3, 2009·International Journal of Cardiology·Arie O VerkerkRonald Wilders
Aug 11, 2006·Current Opinion in Cardiology·Ami B Bhatt, Peter H Stone
Sep 23, 2008·American Journal of Therapeutics·Jeffrey S Borer, Jean-Yves Le Heuzey
Nov 27, 2008·Journal of Cardiovascular Pharmacology·Fanny VaillantPhilippe Chevalier
Dec 6, 2007·Drugs·Dario DiFrancesco, Jeffrey S Borer
Sep 1, 2011·Expert Review of Cardiovascular Therapy·Roberto Ferrari, Claudio Ceconi
Feb 23, 2012·Journal of Cardiovascular Electrophysiology·Eugene A Sosunov, Evgeny P Anyukhovsky
Jun 21, 2007·The Journal of Pharmacology and Experimental Therapeutics·Lan ChengMichael C Sanguinetti
Nov 26, 2019·Anesthesiology·Alexandre BedetArmand Mekontso Dessap
May 5, 2009·American Journal of Physiology. Heart and Circulatory Physiology·Lance P ChristensenRobert J Tomanek
Mar 30, 2018·Heart Failure Reviews·Agata Bielecka-DabrowaMaciej Banach
Oct 27, 2018·Therapeutic Advances in Chronic Disease·Charles Badu-BoatengDaniel Hammersley
Jan 5, 2019·Circulation Journal : Official Journal of the Japanese Circulation Society·Tomomi IdeHiroyuki Tsutsui
Dec 13, 2019·Cardiology Research and Practice·Ryan ChabanChristian-Friedrich Vahl
Dec 17, 2008·American Journal of Physiology. Heart and Circulatory Physiology·Paul MilliezClaude Delcayre
Mar 27, 2007·American Journal of Physiology. Heart and Circulatory Physiology·Eduard I DedkovRobert J Tomanek
Sep 29, 2007·The Journal of Pharmacology and Experimental Therapeutics·Vlad CiobotaruDamien Logeart
Jan 16, 2020·Anesthesiology·Alexandre BedetArmand Mekontso Dessap
Aug 11, 2019·Current Topics in Medicinal Chemistry·Yue ZhouKun Sun
Oct 19, 2010·American Journal of Physiology. Heart and Circulatory Physiology·Claudio CeconiRoberto Ferrari
Feb 8, 2019·Nature Reviews. Drug Discovery·Heike WulffVladimir Yarov-Yarovoy

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antianginal Drugs: Mechanisms of Action

Antianginal drugs, including nitrates, beta-blockers, and calcium channel blockers, are used in the treatment of angina pectoris. Here is the latest research on their use and their mechanism of action.

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.

Cardiac Conduction System

The cardiac conduction system is a specialized tract of myocardial cells responsible for maintaining normal cardiac rhythm. Discover the latest research on the cardiac conduction system here.

Cardiomyopathy

Cardiomyopathy is a disease of the heart muscle, that can lead to muscular or electrical dysfunction of the heart. It is often an irreversible disease that is associated with a poor prognosis. There are different causes and classifications of cardiomyopathies. Here are the latest discoveries pertaining to this disease.