The compound effectively stopped weight gain, lowered cholesterol, controlled blood sugar and minimized inflammation in mice, making it an excellent candidate for a rapid transition into human clinical trials.
Fexaramine, the new pill, doesn't dissolve into the blood like appetite suppressants or caffeine-based diet drugs, but remains in the intestines, causing fewer side effects unlike the other diet pills.
In the United States, more than a third of adults are obese and 29.1 million people have diabetes, according to the Centers for Disease Control and Prevention.
Farensoid X receptor (FXR), a protein that plays a role in how the body releases bile acids from the liver, digests food and stores fats and sugars.
The human body turns on FXR at the beginning of a meal and not only triggers the release of bile acids for digestion, but also changes blood sugar levels and causes the body to burn some fats in preparation for the incoming meal.
"When you eat, you have to quickly activate a series of responses all throughout the body. And the reality is that the very first responder for all this is the intestine" says Evans.
The group gave obese mice a daily pill of fexaramine for five weeks and the mice stopped gaining weight, lost fat and had lower blood sugar and cholesterol levels than untreated mice.
In addition, the mice had a rise in body temperature—which signals metabolism ramping up—and some deposits of white fat in their bodies converted into a healthier, energy-burning beige form of the tissue.
Evans says, "The body's response to a meal is like a relay race, and if you tell all the runners to go at the same time, you'll never pass the baton. We've learned how to trigger the first runner so that the rest of the events happen in a natural order."
The researchers hypothesize, since fexaramine doesn't reach the bloodstream, it is also likely safer in humans than other FXR-targeting drugs. They're already working to set up human clinical trials to test the effectiveness of fexaramine to treat obesity and metabolic disease.
Administration of the drug under a doctor's guidance, would work in conjunction with diet and lifestyle changes, similar to weight-loss surgeries or other obesity or diabetes drugs.
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