Meldonium: The Latest Performance Enhancing Drug

By Floyd Arthur

The World Anti-Doping Agency has a new drug in its sights -- meldonium. Also known as  Mildronāts, Quaterine, MET-88, THP and trimethylhydrazinium propionate, meldonium is manufactured by the Latvian pharmaceutical company Grindeks and sold under the brand name Midronate.

It is widely used in Eastern Europe and Central Asia for the treatment of angina, heart attacks and ischemic stroke, but is not approved for use in the United States.

Meldonium was banned by the WADA in 2016. But after dozens of elite athletes tested positive for the drug earlier this year, the anti-doping agency determined that any athlete who failed a drug test for meldonium prior to March 2016 may still compete.

What is Meldonium?

Meldonium is a fatty-acid oxidation inhibitor that alters the metabolic pathway for carnitine. Developed by chemist Ivar Kalvins, chair of the scientific board of the Latvian Institute of Organic Synthesis, the drug was first used to improve sexual performance and sperm motility in boars.

Meldonium’s first known use in humans occurred between 1979 and 1989, when it was given to Soviet troops in Afghanistan to improve their endurance in the country’s mountainous terrain.

According to the a study published in Drug Testing and Analysis in December 2015, meldonium “demonstrates an increase in endurance performance of athletes, improved rehabilitation after exercise, protection against stress and enhanced activations of central nervous system functions."  The WADA classifies it as a metabolic modulator, similar to insulin.

Meldonium Use in Athletes

Meldonium first came to the attention of antidoping officials in 2015, when the Partnership for Clean Competition funded a study to test for meldonium in athletes worldwide. The group, which includes representatives from the U.S. Anti-doping Agency, the U.S. Olympic Committee and various professional sports leagues, looked at 8,300 anonymous urine samples from athletes in different sports. It found meldonium in 182 samples, a rate of 2.2 percent. According to Larry Bowers, chair of the PCC Scientific Board, that is more than twice the rate for any other banned substance on the WADA list.

Then, meldonium hit the headlines when tennis star Maria Sharapova tested positive for the banned drug at the Australian open in January 2016. Since then, dozens of athletes, including Olympic gold-medalist Semion Elistratov and world champion speedskater Pavel Kulizhnikov, both of Russia, have tested positive for the drug.

According to a study published in the British Journal of Sports Medicine in March 2016, a total of 490 athletes tested positive for meldonium at the Baku 2015 European Games.

Do Meldonium Work?

There is little evidence that meldonium actually enhances athletic performance. According to Mark Stuart, a pharmacist in London who is on the medical and antidoping commission of the European Olympic Committees, “The evidence around whether it is a performance-enhancing drug is quite thin.”  

In fact, there is almost no available scientific evidence on the effects of meldonium on performance at all, other than the fact that it appears to inhibit the synthesis of carnitine, which the body uses to burn fat. This might force the body to burn glucose, which produces more energy under conditions of low oxygenation than fat, said Dr. William R. Hiatt, a cardiologist and professor at the University of Colorado School of Medicine, in an interview with the N.Y. Times. 

This hypothesis is borne out by a Grindeks’ funded randomized controlled trial  which demonstrated marginal but significant improvement in exercise tolerance in patients with stable angina who were given meldonium for a period of 12 months. It may also be why athletes believe the drug will improve their performance when they are exercising at peak capacity.

Meldonium is Latvia’s leading medical export, with sales of over 56 million euros ($64 million) in 2013. It cannot be obtained legally in the United States except with approval from the FDA. It is not known how Sharapova, who has lived in Florida since she was 7 years old, obtained the drug.