The Unauthorized Biography

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The birth of metformin

When metformin was born to Dr. Jean Sterne at Aron Laboratories in Paris, France, in 1959, its proud father had no way to foresee how it would change the world. Initially (and still) sold under the trade name Glucophage, Greek for sugar eater, it would grow up to be a superstar, the most prescribed diabetes drug on the planet.

Like most drugs, metformin has its roots in a plant — in this case, the French lilac (Galega officinalis). Research into this plant’s potential as an antidiabetic agent dates back to the early 1920s, but major efforts were abandoned with the discovery and development of insulin. It wasn’t until 30 years later, in the search for oral drugs to control diabetes, that these efforts resumed. While the French lilac has long been known to have glucose-lowering properties, it has also long been known to be poisonous. Because it is dangerous to livestock, here in the United States it’s listed as a noxious weed in 12 states, including pretty much every state it grows in.

And just how does metformin lower blood glucose? No one knows, despite the fact that it is one of the most studied compounds in the world, having been the subject of over 13,000 clinical researchers and more than 5,600 published studies over the last 60 years. The leading theories on metformin hold that it limits glucose production in the liver, or that it helps muscle tissue take in glucose. Or that it helps with carbohydrate absorption. Or that it’s a mild insulin sensitizer. It’s probably a combination of all of these factors, although this is far from a definite answer.

But metformin does work, and it works fast, nearly from the first pill. It also carries little risk of overdoing its job; when used alone as a treatment, metformin rarely causes hypoglycemia (low blood glucose). It does not cause weight gain, and in many people it causes mild weight loss. It reduces the risk of heart attack, can be combined with other blood-glucose-lowering drugs, and has few harmful side effects. (Click here to learn more about the side effects of metformin.) Yet in the beginning, metformin was nowhere near as beloved as it is today.

Click on page 3, below, to learn about the early setbacks of metformin.

Originally Published June 4, 2013

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