Exercise in a pill

John DiTraglia M.D.


Exercise is so good for you. It improves blood pressure, blood cholesterol profiles, stress relief (like it did for Forest Gump) and ultimately longevity in a big way. It is more beneficial than not being obese but remember that of all the benefits of exercise, weight loss is not one of them. Exercise maybe can cause a small decrease in waist circumference and the new mantra is that it may help you maintain weight loss from dieting, though the evidence for help with weight loss maintenance is all observational (AKA bad evidence).

Lack of exercise should be considered a disease since it is so deadly but the Food and Drug Administration does not consider that a disease. For this reason, and also more especially because why or how exercise does all these wonderful things is still very poorly understood, there has been so far no treatment or medication that would duplicate the effects of exercise, except one.

An article in last week’s The New Yorker has an interesting article (1) about a drug to give you exercise in a pill. Developed by Ligand Pharmaceuticals and GlaxoSmithKline in the 1990’s and called GW501516 or just 516 or Cardarine it had reached the point of large scale human trials when it was given up on because it caused multiple cancers in mice and rats. But not before it was widely manufactured and used as a performance enhancer by lots of athletes. It is still available online as Ms. Tilley demonstrated by getting some sent to her. (She was afraid to take it.) It was banned by the International Olympic Committee and a urine test for it disqualified numerous athletes from the 2008 Beijing Olympics.

So far there have been no reports of adverse effect in these willing illegal guinea pigs but that use is obviously not well recorded or documented. A newer maybe safer version of 516 is currently in development under tight raps and still a ways off.

How this drug works by stimulating the peroxisome proliferator-activated receptor delta (PPARd) that turns on big energy expenditure and duplicates many of the effects of exercise is an improvement on our understanding of exercise effects.

In the meantime there is no substitute for the old fashioned painful and time consuming version of exercise. A pill that makes exercise feel more fun like it is naturally in kids and apparently in mice and rats would be another way. Mice and guinea pigs spontaneously put miles on the exercise wheels in their cages. Ms Twilley cites a study done in the Netherlands a few years ago where they put exercise wheels out in the woods and documented wild mice use them at length and repeatedly with motion-activated night-vision cameras.


John DiTraglia M.D.

John DiTraglia M.D. is a Pediatrician in Portsmouth. He can be reached by e-mail- jditrag@zoomnet.net or phone-354-6605.

John DiTraglia M.D. is a Pediatrician in Portsmouth. He can be reached by e-mail- jditrag@zoomnet.net or phone-354-6605.


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