Cancer Drug Trodusquemine can Help Prevent Heart Attack and Stroke

A drug trialed for breast cancer and diabetes has now shown cardiovascular benefits. Trodusquemine is a drug that can reverse the effects of atherosclerosis

Atherosclerosis - Causes, Symptoms, Prevention & Treatment
Atherosclerosis is a condition in which the arteries become hard and narrow, leading to restricted blood flow.

‘Trodusquemine is a drug that could reverse the build-up of cholesterol plaque and melt it away from the walls of the arteries.’

Highlights:

Trodusquemine, a drug to treat cancer and diabetes can protect against heart disease and stroke
The drug has been found to melt away the fat in the arteries
The study found that the drug also reverses the signs of atherosclerosis

A drug to treat breast cancer and diabetes has been found to melt away the fat inside arteries that can cause heart attack and stroke. A single dose of the drug Trodusquemine can reverse the effects of atherosclerosis. The findings of the study raise the prospect of new preventative medicines for heart attacks and strokes.

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Trodusquemine can Reverse the Effects of Atherosclerosis

A research team from the University of Aberdeen tested the effect of the drug Trodusquemine on mice with set-in atherosclerosis. For the study, mice were treated with a single dose of Trodusquemine after eight weeks of high-fat diet. After six weeks of treatment, mice treated with Trodusquemine had 20% reduction in body weight with greater than 50% reduction in fat mass compared to the control group.

The team found that the drug not only reduced fatty plaques inside the arteries, a single dose had the same effect as regular doses administered over time.

Trodusquemine works by blocking an enzyme called protein-tyrosine phosphatase 1B (PTP1B) which is increased in people with obesity and diabetes. PTP1B is also increased in other conditions that involve prolonged inflammation such as sepsis, inflamed diabetic foot ulcers, and allergic lung inflammation.

The research team also found that the drug activates a protective enzyme called AMPK ((acetyl-CoA carboxylase) kinase), which mimics exercise and actively reduces chronic inflammation.

The findings of the study suggest that the drug can significantly reduce deaths due to heart disease, which is the number one cause of death globally, claiming lives of 17.7 million people every year.

Professor Mirela Delibegovic from the University of Aberdeen’s Institute of Medical Sciences, who led the study, said, "Trodusquemine has already been trialed for treatment of diabetes and breast cancer, but this is the first time it has been used in models of atherosclerosis."

"These have only been tested at pre-clinical level, in mice, so far but the results were quite impressive and showed that just a single dose of this drug seemed to completely reverse the effects of atherosclerosis. The next step is to test the ability of this drug to improve outcomes in human patients with developed atherosclerosis and cardiovascular disease."

Inflammation plays a crucial role in atherosclerosis by thinning the connective tissue in plaques and causing them to rupture. Stopping the build-up of cholesterol plaques in the arteries can prevent heart attack and stroke. Professor Jeremy Pearson, Associate Medical Director at the British Heart Foundation, said, "This study shows Trodusquemine can also limit the build-up of fatty atherosclerotic plaques in mice. If we see the same effect in patients, the drug may prove even more useful than currently hoped for."

The research was published in the journal Clinical Science.

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Atherosclerosis

Atherosclerosis is the accumulation of cholesterol plaques that harden over time and narrow the arteries, leading to heart attacks, stroke, and peripheral vascular disease. The accumulation of plaque begins when an artery's inner lining called the endothelium becomes damaged. The causes of atherosclerosis are elevated levels of triglycerides, high blood pressure, smoking, high consumption of alcohol, physical inactivity, unhealthy diet, obesity, and diabetes. Lifestyle change is the main treatment for atherosclerosis.

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Tips to Prevent or Delay Atherosclerosis

Heart-Healthy Eating - A heart-healthy diet is low in sodium, added sugar and fats. Include whole grains, fruits and vegetables, seafood, lean meat, fat-free dairy products.
Exercise - Aerobic exercise helps reduce fat mass. Regular exercise helps improve fitness level and health. Exercising for at least 150 minutes per week can improve overall cardiovascular health.
Quit Smoking- Smoking can tighten blood vessels and increase the risk of atherosclerosis. Quitting smoking helps reduce the risk of atherosclerosis.

Reference:

Dawn Thompson, Nicola Morrice, Louise Grant, Samantha Le Sommer, Emma K. Lees, Nimesh Mody, Heather M. Wilson, Mirela Delibegovic. Pharmacological Inhibition of Protein Tyrosine Phosphatase 1B Protects Against Atherosclerotic Plaque Formation in the LDLR Mouse Model of Atherosclerosis. Clinical Science, (2017), 131 (20) 2489-2501; DOI: 10.1042/CS20171066
How Can Atherosclerosis Be Prevented or Delayed? - (https://www.nhlbi.nih.gov/health/health-topics/topics/atherosclerosis/prevention)

Source-Medindia