Health and Fitness in a Bottle: Big Pharma Discovers their Holy Grail

I'm strong to the finish, cuz I eats me spinach....
I'm strong to the finish, cuz I eats me spinach....

Scientists from the Salk Institute’s Gene Expression Laboratory may have discovered Big Pharma‘s Holy Grail of Pharmaceuticals.

A pill that would allow you to reap all of the benefits of vigorous exercise while sitting on the couch watching re-runs of Seinfeld.

How about that!

Scientists from the Salk Institute’s Gene Expression Laboratory have reported (in the July 31 advance edition of the journal Cell) that they have discovered two drugs (GW1516 and AICAR) that were able to transform regular ole’ lab mice into freaky running machines.

AICAR increased the mice’s endurance on a treadmill by 44 percent after just four weeks of treatment.

GW1516 produced a 77%  increase in endurance, but sadly, had to be combined with exercise to have any effect.

The Study

Lead researcher, Ronald M. Evans, Ph.D, had previously discovered that by permanently activating a genetic switch known as PPAR delta, he could turn lab mice into miniature Olympic marathon champs.

In addition to their improvements in aerobic endurance, these super mice didn’t gain weight while being fed a diet high in pizza and beer. In addition to their ripped physiques, they experienced improved insulin sensitivity and lowered levels of blood sugar.

This led Dr. Evans to hypothesize whether a drug specific for PPAR delta would have the same beneficial effects.

So, they doped the mice with GW1516.
After four weeks, the researchers were in for a bit of a disappointment.
I've got the Eye of the Tiger...
I've got the Eye of the Tiger...

The mice were leaner, had an improved fatty acid profile, improved insulin sensitivity and lowered levels of blood sugar, but there was no effect on their exercise performance.

So, like a personal trainer, they upped the mice’s cardio and had them run up to 50 minutes on a treadmill.

And after a few more weeks, the GW1516 mice were lapping the non-doped mice.

In fact, the GW1516 mice improved their exercise endurance 77% higher than the control mice. They also saw a 38% increase in slow twitch muscle fibers.

But wait, the researchers weren’t finished yet. GW1516 looks pretty great, but they were looking for a drug that would provide the benefits of exercise without actually having to do the exercise.

Enter AICAR.

The researchers fed untrained mice AICAR, (a synthetic AMP analog that directly activates AMPK).

After four weeks, the AICAR mice were pushed onto the treadmill and boy did they perform. On average, they ran 44% longer than the control mice. According to the researchers, “That’s as much improvement as we get with regular exercise.”

So there we go, exercise in a pill.

So, How Does it Work?

Well, according to Dr. Evans,  “GW1516 activates the PPAR-delta protein, but the mice must also exercise to show increased endurance. It seems that PPAR-delta switches on one set of genes, and exercise another, and both are needed for endurance”.

AICAR however, “activates the PPAR-delta protein and mimics the effects of exercise, thus switching on both sets of genes needed for the endurance signal”. It “signals the cell that it has burned off energy and needs to generate more. It is pretty much pharmacological exercise”.

Conclusion

Theirs: “This is not just a free lunch,” Dr. Evans said. “It’s pushing your genome toward a more enhanced genetic tone that impacts metabolism and muscle function. So instead of inheriting a great set-point you are using a drug to move your own genetics to a more activated metabolic state.”

“The drugs’ effect on muscle opens a window to a world of medical problems,” he said. “This paper will alert the medical community that muscle can be a therapeutic target.”

Mine: I wonder if we are not straying a leeetle bit too far down the Eugenics path with this research.

Forgetting the potential moral argument of switching our genes on and off, my concern is purely medical. While it will take years and years of animal and human testing before a commercially viable GW1516 or AICAR is available on the market, I still think that I would prefer to improve my body the old fashioned way.

Thanks to EurekAlert! for the original source material.

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9 comments

  1. Interesting!

    Let’s start coming up with guesses for what fun, happy, descriptive names they will call these drugs:

    Endurovox
    Endurair
    Endartis
    Enduraicar

    DR, did you notice if a subject were to stop taking either of the drugs if the effects would be maintained?

  2. They have only released the abstract, so I don’t have all the details.

    That’s too funny about the names, I debated doing that in my post.

    When’s the next post?

  3. I agree with you. Exercise the old fashioned way seems to work great for me and most people. It feels good psychologically as well as physically after a long run or bike ride. Don’t know if a pill can do that!

  4. Just saw a story about this on Fox news.

    The man being interviewed said it would be meant more for people who are unable to exercise; like handicapped, or super morbidly obese people that have extreme trouble moving.

    But we both know a lot more people than that can’t wait to get their hands on them.

  5. Oh well, there goes one of the few remaining things it wasn’t possible to just walk into a shop and buy. Sigh. Assuming this stuff ever makes it to the market of course, it wouldn’t be the first announcement of a miracle drug that nobody ever heard of again.

    I wonder if it could lead to a cultural shift where exercising becomes viewed as something people only do if they can’t afford the appropriate pill? (Ha! Look at that poor sucker! He can’t afford a car or an exercise pill, so he’s CYCLING somewhere…! Ha! Pity the fool! Ha!*)

    Then again, suspending disbelief for a moment, if this stuff did turn out to have all the benefits of exercise why shouldn’t people who don’t enjoy exercise use it?** There’s no inherent superiority to doing something the old-fashioned way, just because that’s how it’s always been done. I think I’d probably hang on to my bike anyway because I enjoy it (and it saves me stacks of cash), but if there are people (and I’m sure there are) who’d be willing to buy “exercise in a pill” it’s not up to me to judge them or say they shouldn’t.

    My vote for the name – MAICAR. Any number of marketing puns available there! Can’t wait for the spam, “GeT MY-K4R oNL1nE 4 CHeaP $$$$!”

    *For the full effect, you have to imagine this being said through a mouthful of cheeseburger by a chemically-slim-and-toned guy driving a Hummer.

    **I’m assuming nobody has a problem with this for people who CAN’T exercise.

  6. I think it’s just scary and the secondary effects won’t be known before long but they will show up. You can’t play God without consequences.
    I prefer feeling my muscles aching.
    I understand it could be good for some disabled people but we all can figure already lots of other people will be interested in that stuff for many other reasons.
    What’s next?

  7. Thanks for making this topic so readable. I’ve read about this in other places, but your article put all the pieces in place for me. I agree that this would be wonderful for folks who really need it, and that there will always be folks who will try to abuse it (e.g., sports). As for me, I’m just the average person, who doesn’t like to go to the gym, but would love to have healthy ‘exercised’ muscles by pill.
    Austin
    http://drughealth.blogspot.com/

  8. It looks like many of the replies here are negative? I wonder why so many people automatically think negative when encountered with the unknown. It is the unknown that excites me, and keeps me going to college. It would seem that some people have the same attitude as Charles Duell in 1899 He was caught saying “Everything that can be invented – has already been invented”. Everyone knows that Charles Duell was a complete DUMB ASS in every sense of the word. So my advice to people is loose the fear, and don’t be a DUMB ASS! Imagine the possibilities of this drug and the ramifications it could have on the cost of health care, or the quality of your life. Keep an open mind, or you risk becoming a Charles Duell.

  9. 44% better cardio doesn’t necessarily mean they have improved hearts or lungs, does it? It sounds like this drug can increase muscle and therefore help reduce body fat, but that might be what accounts for the increased endurance on the treadmill. People whose hearts, lungs, and brains are sick will still be in trouble unless they adequately train their bodies with exercise and eat well. I think that’s what these companies want, too. If people take pills, get muscles & look better but eat pizza & drink beer& not much else, they may still have high cholesterol, heart disease, and depression & anxiety– those are the most profitable pharmaceutical diseases out there. This is hardly the holy Grail for humanity– just another huge moneymaker for drug companies.

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