Bodybuilders Bulk Up Using... Cancer Drugs?
By Kristina Fiore
January 16, 2014
Noah Thomas' tattooed biceps are almost 18 inches around, to hear him tell it. His YouTube channel is full of advice for other weight lifters on how to build muscle. In at least one video, he demonstrates how he injects testosterone.
In another, Thomas talks about a side effect of having too much testosterone: high estrogen levels. Too much of this "female" hormone could lead to a host of well-known problems among bodybuilders -- gynecomastia, low sex drive.
But Thomas -- whom we couldn't reach for comment -- has a plan for fixing that.
"I heard Arimidex is useful," he says in the video. "I don't think I'm going to get any support from my endocrinologist. ... I do think my psychiatrist might be willing to get that for me."
Arimidex, also known by its chemical name anastrozole, is an aromatase inhibitor -- a breast cancer drug. While steroids and growth hormone make headlines when athletes abuse them, breast cancer drugs are a lesser-known staple of doping regimens, for athletes and "weekend warriors" alike. Star therapies of the breast oncology world -- like tamoxifen (Nolvadex) and exemestane (Aromasin) -- provide an easy, non-injectable means of cutting estrogen's unwanted side effects.
And bodybuilders are packing other little-known pharmaceuticals into their routines -- some of which, like ghrelin mimetics and selective androgen receptor modulators (SARMs), are still under investigation in clinical trials and are not available on any regulated market.
Demand for Breast Cancer Drugs
Weightlifters don't seem to have a preference for either class of anti-estrogens. There are the selective estrogen receptor modulators (SERMs) like tamoxifen, or the aromatase inhibitors like anastrozole. Both classes mitigate the effects of estrogen, which is metabolized from testosterone. When testosterone levels are high, estrogen levels also tend to increase as a natural byproduct.
"All they do is block estrogen," Fred Rowlett, president of the North American Natural Bodybuilding Federation, said of the nonchalant attitude weight lifters have about taking cancer drugs. "When you don't have estrogen, you gain nothing but muscle."
Rowlett's organization champions drug-free bodybuilding, and prescription anti-estrogens are on the group's list of banned substances, modeled on that of the International Olympic Committee. These breast cancer drugs are also on the prohibited performance-enhancing drugs lists from the U.S. Anti-Doping Agency and the World Anti-Doping Agency.
Abuse of breast cancer drugs isn't limited to top athletes. "Weekend warriors" and enthusiastic gym-goers are driving demand, as scores of YouTube videos attest. There are no data on how widely used anti-estrogens are in this community, but Rowlett says it's common practice.
Given that they're prescription drugs, the obvious question is how bodybuilders are getting their hands on them.
Rowlett says family practice physicians tend to write the scripts directly to those who are working out. There is also the potential for doctor shopping if one clinician refuses, as Thomas pointed out in his video.
And, of course, there's an underground market that anyone with Internet access can peruse. On its homepage, HardcorePeptides.com boasts tamoxifen and exemestane for under $40. Anti-Estrogens.com is a bit pricier, at $79 for a 30-pack of tamoxifen tablets.
It's unclear if the products are diverted, or if they're synthesized in a homegrown lab, à la Breaking Bad. Some may simply be scams to obtain credit card information, a common problem that many of the sites denounce and attempt to reassure potential buyers with customer service hot lines and other security measures.
A spokesperson for AstraZeneca, which makes Nolvadex and Arimidex, told MedPage Today that diversion and counterfeiting of its products for this purpose "isn't something we're aware of." Pfizer, maker of Aromasin, didn't comment on whether they were aware of the diversion or counterfeiting of the drug.
Then there are the specialized supplements -- which don't require a prescription -- that claim to target estrogen and aromatase, readily up for sale on Amazon.com and other sites. But like the rest of the unregulated supplement industry, there's no guarantee that these bottles contain what's on their labels.
Hungry for the Hunger Hormone
Researchers have been interested in ghrelin, called the hunger hormone for its ability to spark appetite, as a potential target for obesity treatment, but it's had more practical application in wasting disease. Ghrelin mimetics, such as GHRP6 and GHRP2, are still only in clinical trials, and none are commercially available on any market anywhere in the world.
They're readily for sale, however, on a vast amount of websites, along with other growth-hormone-releasing peptides such as ipamorelin and hexarelin. Ghrelin mimetics' potent stimulation of growth hormone secretion is the reason it's valued in muscle-building circles.
The hormones are all blatantly listed on sites like peptideboys.com and deboralabs.com, side-by-side with anabolic steroids and other performance-enhancing drugs. Some purport to be selling their peptides to scientists, but at the same time they tout "discreet shipping."
Jose Garcia, MD, PhD, of Baylor College of Medicine, who has been involved in studies of ghrelin mimetics, told MedPage Today that scientists would never acquire their active drugs that way.
"You would never go to a site like this because there is no quality control so you never know if these products are contaminated or if they contain what they're supposed to," Garcia said. "Not even for animal experiments."
It's likely that these drugs are being made in underground labs, he added.
The same goes for nonsteroidal selective androgen receptor modulators (SARMs), which are also still under investigation for wasting disease. A Google search of where to buy one of the most popular ones, enobosarm (Ostarine is the proposed trade name), returns plenty of results. As with ghrelin mimetics, most of the sites claim their products are for research purposes only and aren't intended for human consumption.
What's Regulated?
Since steroids make the Drug Enforcement Agency's list of controlled substances, inventive entrepreneurs have tried to get around legal issues by making supplements, prohormones, and designer steroids. There's much overlap between these categories, with prohormones being hormone precursors that can amplify the effect of existing hormones, while designer steroids are typically anabolic drugs that were never marketed for medicinal purposes.
Companies that produce these agents have been linked to top athletes, like Barry Bonds and BALCO, and, more recently, Biogenesis and several top baseball players including Alex Rodriguez and Ryan Braun.
Every now and then the FDA also cracks down on these agents -- typically after adverse event reports, as was the case with last month's consumer warning on the Mass Destruction supplement. A 28-year-old in North Carolina developed liver failure after weeks of using the product, which the FDA said contained at least one synthetic anabolic steroid.
Federal prosecutors have also gone after distributors of these supplements, with Bodybuilding.com -- the "largest Internet retailer of supplements in the world," according to a Department of Justice press release -- paying a $7 million fine in 2012 for selling drugs that were misbranded as supplements.
The feds had behind them the Designer Steroid Control Act, which updated the earlier Anabolic Steroid Control Act in order to bring these supplements under the umbrella of illegal steroids.
But anti-estrogens, ghrelin mimetics, and SARMs aren't included in any of that regulation, and they're not on the controlled substances list.
Joseph Moses, a spokesperson for the DEA, told MedPage Today that even though these drugs aren't controlled substances, they could be used in prosecution.
"If we seized them when we seized steroids that are controlled, we could bring them into court as evidence that the individual intended to use those substances or, if it's on a bulk level, to distribute them," Moses said.
Doctors who help weightlifters to obtain steroids via prescription can get in trouble with the law for illegal distribution, as was the case for a Pittsburgh Steelers doctor who falsely claimed his patients had hormonal disorders so they could get their drugs. He was also charged with healthcare fraud -- which covered the drugs prescribed to combat the side effects of steroid use.
Guidelines from both the American Association of Clinical Endocrinologists and The Endocrine Society state that testosterone therapy should be limited to men with testosterone deficiency. The American Academy of Family Physicians also has a policy statement against helping patients obtain performance-enhancing drugs.
"Our policy is very clear," Reid Blackwelder, MD, president of the AAFP, told MedPage Today. "We don't think anything should be prescribed for enhancing athletic performance," including prescription drugs that work against estrogen, he said.
"All of these medicines," he said, "should only be used for their intended medical purposes."
From http://www.medpagetoday.com/PrimaryC...eFitness/43839