Daewoong Pharmaceutical has said it would promote sarpogrelate, which reportedly has a lower risk of bleeding than aspirin and prevents cardiovascular disease, to fight the popular notion that aspirin is synonymous with an antiplatelet drug.

The company also plans to market it as a preventive therapy for high-risk groups with cardiovascular diseases such as elderly diabetic patients, it added.

Sarpogrelate acts on the serotonin receptors in the blood vessels to suppress vasoconstriction, improving the limping symptoms in patients with peripheral arterial disease. Other antiplatelet medicines, clopidogrel and aspirin, irreversibly bind to platelets, while sarpogrelate binds reversibly.

With a short half-life of four hours, sarpogrelate’s antiplatelet effect disappears within a short time when the administration is discontinued. So, the agent can reduce the risk of bleeding. However, clinicians tend to associate an antiplatelet drug with aspirin. Plus, sarpogrelate lacks strong evidence by a large-scale trial.

Daewoong, which sells antiplatelet drug Anpl-One with the ingredient of sarpogrelate, said it plans to release the results of a trial on the drug’s secondary effect to prevent cardiovascular disease in diabetic patients in October. The study was a large-scale one, testing the drug on 2,000 patients. Daewoong released Anpl-One in 2015. Selling about 18 billion won ($14.6 million) a year, the drug tops the local sarpogrelate sustained-release market.

Korea Biomedical Review has recently met with Professor Park Jung-hwan of the Endocrinology and Metabolism Department of Hanyang Univerisity Hospital to learn the clinical value of sarpogrelate and challenges.

Question: What are the merits of sarpogrelate, compared to aspirin?
Answer: Patients with peripheral artery disease suffer a lot from claudication. Therefore, it is necessary to improve these symptoms as well as to earn the antiplatelet effect in such patients. However, aspirin and clopidogrel reportedly have little effect in improving these symptoms. Sarpogrelate is effective for inhibiting vasoconstriction by acting on the serotonin receptors of the blood vessels, so it can improve the symptoms of claudication and show the antiplatelet effect in patients with peripheral arterial disease. Besides, increased serotonin levels raise the risk of atherosclerosis, major pathophysiology of peripheral arterial disease, and sarpogrelate has shown its effect to inhibit atherosclerosis in related studies.

Q: For which patient groups do you recommend to use sarpogrelate?
A: When a vascular disease occurs while the serotonin level is high, it often leads to polyvascular disease. Diabetes and peripheral arterial disease cause high serotonin levels. Sarpogrelate is very effective in these patients. Among patients with diabetes and peripheral arterial disease, elderly patients, in particular, may find it helpful to use sarpogrelate because of the high risk of bleeding and complications associated with antiplatelet agents.

Q: What are the merits of Anpl-One sustained-release among sarpogrelate-using drugs?
A: For sarpogrelate to show additional effects such as antiplatelet effect and improvement in red blood cells’ ability to deform, patients must take the recommended dose of 300mg per day. To do so, they should take the existing sarpogrelate three times a day. However, increasing the number of doses weakens drug compliance. On the other hand, patients can take sarpogrelate sustained-release once a day, which can enhance drug compliance significantly.

Q: What are the limitations of sarpogrelate?
A: Sarpogrelate lacks data from a randomized and controlled clinical trial (RCT), as much as conventional antiplatelet drugs such as aspirin have. However, through several studies, sarpogrelate has proved not only the antiplatelet effect but an ability to suppress atherosclerosis, improvement in red blood cell deformability, better insulin resistance in diabetes, better proteinuria, and safety. In other words, we have the minimum evidence for selecting sarpogrelate in clinical practice. Therefore, physicians can consider prescribing sarpogrelate for patients with diabetes or peripheral arterial disease or those with suspected micro blood flow abnormalities.