2024年10月20日星期日

Recent Advances in Antianginal Drugs


Recent Advances in Antianginal Drugs

The field of antianginal drug therapy has seen significant developments in recent years, with researchers and pharmaceutical companies focusing on novel mechanisms of action and improved formulations. These advancements aim to enhance efficacy, reduce side effects, and provide better outcomes for patients with angina pectoris. Here's an overview of some of the most notable recent advances in antianginal drugs:


Novel Sodium Channel Inhibitors:

Building on the success of ranolazine, researchers have been exploring new sodium channel inhibitors. These drugs target specific sodium channel subtypes to reduce intracellular sodium and calcium overload in cardiac cells. Some promising candidates in development include:



GS-6615: A more potent and selective late sodium current inhibitor

ATI-2042: A novel compound showing potential in both angina and atrial fibrillation


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Improved Nitrate Formulations:

To address the issue of nitrate tolerance, new formulations and delivery systems have been developed:



Transdermal nitroglycerin patches with novel polymer technologies for better drug release control

Oral nitrate preparations with modified-release properties to maintain therapeutic levels while minimizing tolerance


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Metabolic Modulators:

Following the success of trimetazidine, research has focused on other metabolic modulators:



Perhexiline: A carnitine palmitoyltransferase inhibitor that shifts myocardial metabolism from fatty acids to glucose oxidation

Etomoxir: Another fatty acid oxidation inhibitor showing promise in preclinical studiesassium Channel Openers:

These drugs aim to improve coronary blood flow by opening ATP-sensitive potassium channels:

Nicorandil: Already used in some countries, it combines potassium channel opening with nitrate-like effects

Novel compounds with more selective potassium channel opening properties are in development


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Rho-Kinase Inhibitors:

Rho-kinase plays a role in coronary artery spasm and atherosclerosis. 

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