Efficacy of heparinoid PSS in treating cardiovascular diseases and beyond-A review of 31 years clinical experiences in China.

Heparin is a life-saving drug with multiple molecular targets and mostly well known for its anticoagulant and antithrombotic pharmacological effects in treating cardiovascular diseases. All the heparin-like polysaccharides that mimic the biological activities of heparin are called heparinoids. However, heparin has no pharmacological effect if taken orally and has to be used by injection in hospital settings. Thus, heparinoids that can be taken orally are critically needed. Propylene glycol alginate sodium sulfate (PSS) is the world's first oral heparinoid used in treating cardiovascular diseases approved by Chinese Food and Drug Administration in 1987. PSS is produced by modifying partially hydrolyzed alginate, one of the most abundant marine polysaccharides isolated from brown algae, by epoxypropane esterification and by chemical sulfation. It is used for treating and preventing cardiovascular-related diseases. The low cost (US$1.29/100 tablets, ~4 tablets/day), remarkable clinical effects, and convenient oral administration make PSS an ideal long-term cardiovascular disease-prevention drug. PSS is also clinically trialed for treating diabetes and diabetes-associated complications, hepatitis, kidney, skin, and many other diseases in China. PSS is available in most drug stores in China, and millions of patients take PSS routinely during the past 31 years. The 24,089 reported clinical cases as well as the structure, preparation, clinical efficacy, adverse reactions, pharmacokinetics, pharmacodynamics, and future perspectives of PSS based on the results of peer-reviewed publications will be discussed. This review should bring the knowledge of PSS gained in China to the world to stimulate in depth academic and clinical studies of PSS and other heparinoids.