Scientists develop an improved pharmaceutical drug for the therapy of atrial fibrillation
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Scientists from the National University of Singapore (NUS) Department of Pharmacy have developed an improved pharmaceutical drug for the therapy of the commonest coronary heart rhythm disturbance – atrial fibrillation (AF). The 8-member analysis staff took 8 years to realize this technological breakthrough which may benefit hundreds of thousands of AF sufferers worldwide.

AF is a severe situation that may result in coronary heart failure, early mortality and stroke. For AF sufferers, there are presently medicines that are used to regulate AF and preserve regular rhythm. Ironically, these medicine while treating AF can promote a distinct sort of coronary heart rhythm disturbance within the decrease coronary heart chambers, often known as ventricular arrhythmia, which is probably extra harmful and even deadly. Some of those current AF medicines are additionally poisonous to different organs such because the liver, lungs and thyroid gland. Hence, there’s an unmet must develop efficacious and safer medicines to deal with AF.

Patents have been filed for the brand new drug candidate, termed as poyendarone. The analysis staff has examined poyendarone in laboratory research and the promising outcomes place the drug to be a gamechanger with larger security and efficacy for medical trials. It is noteworthy that there has not been a regulatory accredited AF drug since 2009.

The findings had been first printed within the journal Acta Phamaceutica Sinica B on 16 March 2022.

New efficient drug with decreased uncomfortable side effects

The analysis staff led by Professor Eric Chan from the NUS Department of Pharmacy found {that a} present drug for AF, referred to as dronedarone, causes the inactivation of a key coronary heart enzyme. Normally, the enzyme converts an unsaturated fatty acid to metabolites that facilitate coronary heart physiological features equivalent to regular beating and coronary heart muscle cell well-being. Dronedarone is metabolised by the center enzyme to kind a drug metabolite that may irreversibly bind to the enzyme’s energetic web site, therefore inactivating it. The inactivation of the enzyme in flip causes ventricular arrhythmia. Patients who expertise ventricular arrhythmia on account of dronedarone need to cease the remedy instantly whereas different therapy choices are thought-about.

Armed with this information, the NUS staff efficiently circumvented this probably deadly facet impact by modifying the chemical construction of dronedarone. This was performed via the delicate alternative of chosen hydrogen atoms current on the drug molecule with deuterium atoms, in a course of often called deuteration. Through this alteration, the reactivity of the metabolite is decreased and it’s now not in a position to inactivate the important thing coronary heart enzyme. Through laboratory research, the staff additionally discovered that the improved drug retained a number of beneficial drug-related properties equivalent to the way it treats AF efficaciously and may be processed by the physique effectively. Like dronedarone, the brand new drug molecule poyendarone is predicted to be administered as tablets.

The growth of an improved model of an current drug that’s each efficacious and safer is vital to deal with the unmet medical want in AF remedy. Prof Chan mentioned, “This is the first time deuteration as a drug discovery strategy is applied to optimise the efficacy while mitigating the side effects of a drug molecule. Our research findings demonstrate an innovative discovery platform that can enhance patient care via the development of efficacious and safe pharmaceuticals.”

There is a powerful must develop protected, efficacious and accessible anti-arrhythmic therapies to handle the ever-growing variety of AF sufferers world wide, which is presently estimated to be greater than 35 million. Poyendarone represents a paradigm shift in enhancing the traits of present medicine, selectively eliminating harmful uncomfortable side effects and organ toxicities while sustaining its potential to manage irregular coronary heart rhythm.”

Dr Pipin Kojodjojo, medical collaborator, heart specialist from the Asian Heart & Vascular Centre (AHVC) Singapore and Adjunct Associate Professor on the NUS Yong Loo Lin School of Medicine

Drug growth plans

The analysis staff is wanting into alternatives to conduct related medical trials that may set up drug security and efficacy, permitting for regulatory approval and business availability.


Journal reference:

Karkhanis, A.V., et al. (2022) Site-directed deuteration of dronedarone preserves cytochrome P4502J2 exercise and mitigates its cardiac opposed results in canine arrhythmic hearts. Acta Pharmaceutica Sinica B.

Posted in: Medical Research News | Medical Condition News

Tags: Arrhythmia, Atrial Fibrillation, Cell, Dronedarone, Drug Discovery, Drugs, Efficacy, Enzyme, Heart, Heart Failure, Laboratory, Liver, Lungs, Medicine, Metabolite, Metabolites, Molecule, Mortality, Muscle, Pharmaceuticals, Pharmacy, Research, Stroke, Thyroid, Vascular

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