01 August 2008

AICAR and GW1516: Exercise Pills of the Future

How would you like to reap the benefits of exercise without exercising, simply by taking 'exercise pills'?

I think many fitness fans would love the idea. The main obstacles versus exercise have been centered on finding the time for it and resisting the efforts involved. With the new development, it is now possible to imagine a future when we can just pop a pill or two and observe the effects of exercise in our bodies.

The most promising compounds recently being studied are AICAR and GW1516.
Researchers at the Salk Institute report they have found two drugs that do wonders for the athletic endurance of couch potato mice. One drug, known as AICAR, increased the mice’s endurance on a treadmill by 44 percent after just four weeks of treatment.

A second drug, GW1516, supercharged the mice to a 75 percent increase in endurance, but had to be combined with exercise to have any effect.

"It’s a little bit like a free lunch without the calories," said Dr. Ronald M. Evans, leader of the Salk group. ~ NYTimes, 1 Aug 2008

How did this come about?
Given that people cannot be improved in this way, Dr. Evans wondered if levels of the gene-controlling protein could be raised by drugs. Pharmaceutical companies have long tried to manipulate the protein because of its role in fat metabolism, and Dr. Evans found several drugs were already available, although they had been tested for different purposes.

In a report published in the Friday issue of Cell, he describes the two drugs that successfully activate the muscle-remodeling system in mice. One, GW1516, activates PPAR-delta but the mice must also have exercise training to show increased endurance. It seems that PPAR-delta switches on one set of genes, and exercise another, and both sets are needed for great endurance.

The second drug, called AICAR, improves endurance without any training. Dr. Evans believes it both mimics the effects of exercise and activates PPAR-delta, thus being able to switch on both sets of genes needed for the endurance signal.

AICAR works by mimicking a by-product of energy metabolism, signalling the cell that it has burned off energy and needs to generate more. The drug is “pretty much pharmacological exercise,” Dr. Evans said. ~ NYTimes, 1 Aug 2008

Should this come true, I can already predict that these exercise pills will be bestsellers. Everyone wants to get instant benefits from exercise. But fitness benefits, minus the exercise? It will be the coolest idea!

Also, a Nobel-Prize for Dr. Evans is not a far-fetched possibility.
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