Angina: New Drug Gets Right To The Heart Of The Problem

Main Category: Heart Disease
Also Included In: Cardiovascular / Cardiology
Article Date: 07 Jan 2009 - 4:00 PDT

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A compound designed to prevent chest pains in heart patients has shown promising results in animal studies, say scientists. In the second issue of the British Journal of Pharmacology to be published by Wiley-Blackwell, researchers from the Centre de Recherche Pierre Fabre in France, show that the novel compound F15845 has anti-angina activity and can protect heart cells from damage without the unwanted side effects often experienced with other drugs.

Because F15845 does not interfere with heart function, as some conventional drugs such as beta blockers do, it could be given as part of a combination therapy. "It's completely different from other anti-angina drugs which directly interact with the function of the heart. So the idea is to do a co-administration with conventional heart drugs such as beta blockers," says lead author of the study, Bruno Le Grand from the Centre de Recherche Pierre Fabre in Castres, France.

The drug works by blocking excess influxes of sodium into heart cells through 'gate' proteins called sodium channels. High levels of sodium in heart cells are associated with low oxygen levels, which cause angina and can in turn lead to the build up of toxic concentrations of calcium that are lethal to cells. A number of drugs that target sodium channels can block the influx, but they act universally on heart cells and can sometimes cause further heart irregularities.

F15845 specifically targets the sodium channels that are thought to cause the most damage, those responsible for what is known as the persistent sodium current, which causes a permanent excess sodium influx.

The study confirmed the drug's anti-angina activity in laboratory animals. The researchers say the drug is absorbed well when given orally and represents a novel therapeutic opportunity for treating angina and possibly other cardiac pathologies.

"We know that in animals, we have acceptable bioavailability, but with the data that we have in human volunteers following phase I clinical trials we are very confident that it is above 70 per cent," says Le Grand.

Wiley-Blackwell is proud to publish the British Journal of Pharmacology as of 1st January 2009.

Full citation: Vacher B, Pignier C, Létienne R, Verscheure Y, Le Grand B; F15845 inhibits cardiac persistent sodium current and prevents angina in animals models; British Journal of Pharmacology

About the Author: Bruno Le Grand is based at the Centre de Recherche Pierre Fabre in Castres, France. To arrange an interview, please contact Dr. Le Grand on bruno.le.grand[at]pierre-fabre.com.

The British Journal of Pharmacology is a broad-based journal giving leading international coverage of all aspects of experimental pharmacology. Its scope includes: molecular and cellular pharmacology, neuropharmacology, cardiovascular and pulmonary pharmacology, pharmacokinetics, drug metabolism, toxicology, gastrointestinal pharmacology, cancer pharmacology, inflammation and immunopharmacology, genitourinary and renal pharmacology, endocrine pharmacology, drug discovery, biopharmaceuticals and methods and techniques. BJP's 2007 Impact Factor is 3.767 (Journal Citation Reports, Thomson Reuters, 2008). The British Journal of Pharmacology can be accessed here.

The British Pharmacological Society is the professional association for pharmacologists in the UK and is one of the leading pharmacological societies in the world. The history of the Society originates in 1931 when a group of pharmacologists met in Oxford and decided to form a learned society. Since those small beginnings the Society has grown to exceed 2500 members and on 1 January 1994 the Society became a Company Limited by Guarantee. It is also a registered charity. The object of the Society is to promote and advance pharmacology, including clinical pharmacology. For more information, please visit http://www.bps.ac.uk.

Wiley-Blackwell was formed in February 2007 as a result of the acquisition of Blackwell Publishing Ltd. by John Wiley & Sons, Inc., and its merger with Wiley's Scientific, Technical, and Medical business. Together, the companies have created a global publishing business with deep strength in every major academic and professional field. Wiley-Blackwell publishes approximately 1,400 scholarly peer-reviewed journals and an extensive collection of books with global appeal. For more information on Wiley-Blackwell, please visit http://www.wiley-blackwell.com or http://interscience.wiley.com.

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