The Novel Drug PAI-039 Prevents Blood Vessel Blockage
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According to a recent study, a new drug called PAI-039 could prevent heart problems like stroke, heart attack and other diseases by avoiding blockages in blood vessels. The study revealed that this drug acts as a protein inhibitor and could be a novel therapeutic approach to prevent cardiac diseases related to blockage of blood vessels. When there is a blockage in blood vessels, they could not effectively deliver oxygen and nutrients to the heart and brain, which consequently leads to stroke or heart attack.
“Arteries are living tubes that contract and expand in order to normalize blood flow to organs and muscles,” explained William Fay, M.D., senior author of the study, who works as a research scientist at the Harry S. Truman Memorial Veterans’ Hospital in Columbia, Missouri. “Soft muscle cells in the artery control blood flow by narrowing and expanding. But, when chronic inflammation happens in a blood vessel because of diabetes, high cholesterol and cigarette smoking, the soft muscle cells in the walls of arteries alter their activities. They slowly accumulate within the artery and narrow the blood vessel. On coronary arteries, which deliver blood to heart muscle cells, this activity creates blockages that can result in a heart attack.”
Efficiency of PAI-039 Drug
Plasminogen activator inhibitor-1, or PAI-1, is a naturally occurring protein inside blood vessels that regulates cell migration. Because of diseases such as diabetes and obesity, PAI-1 over-accumulates in blood vessels. This increases blockage formation. This activity happens not only in arteries, but also in vein grafts in patients who have undergone coronary artery bypass graft surgery.
Fay’s research team examined PAI-039, also called as tiplaxtinin, an experimental drug not yet used to treat humans. The researchers discovered that PAI-039 blocked the migration of cultured human coronary artery smooth muscle cells, and avoided the formation of blockages in arteries and bypass grafts in mice.
“We discovered that PAI-039 reduced blockage development by about 50 percent, which is a potent result in the models we used,” noted Fay. “Other than reducing vascular blockages, inhibiting PAI-1 also creates a blood thinning effect that avoids the blood clots that induce most heart attacks and strokes.”
Fay anticipates that if further studies are successful, PAI-039 or same kind of drugs could be used to avoid blockages in arteries and bypass grafts.
“I don’t believe there will be any single ‘magic pill’ that avoids arterial diseases, particularly for those with other high-risk conditions,” Fay said. “But, possibly someday a PAI-1 inhibitor can be used together with other approaches such as right diet and exercise, aspirin and cholesterol medicines to avoid blood vessel blockages and decrease heart attack and stroke risk.”
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