The mk-677 had arrived on Daniel’s doorstep in a plain brown box and was as dark as urine. Daniel stood in his bathroom, drawing the serum into an oral syringe, investigating its color and consistency. Once it checked out, he let the liquid fall onto his tongue. It bludgeoned his taste buds with an acrid, sinus-scorching flavor. The next day, he went to the gym.
Daniel is a 39-year-old surgeon. In college, he was an athlete—lean, muscled. But four years of med school left him 50 pounds heavier, and he had little time to sweat it off. Lifting brought him some solace, but the gains came slowly. Frustrated, Daniel sought an edge. Steroids were out of the question: “I could lose my license,” he says. But then, whilecombing the Web for an alternative, he discovered MK-677, a chemical originally intended for Alzheimer’s patients. In an ill-considered health gamble that would rightly horrify most medical professionals, he did a little “research” on anonymous online forums and started taking MK-677 along with another chemical. Five weeks into his trial run, he deadlifted 335 pounds three times; a month ago he could barely bring that weight off the ground. It didn’t end there. He began strapping 55 pounds to his waist for dips (up from 25) and banging out three sets of 10. He tacked on 15 pounds to his overhead press, too.
“My wife was like, ‘Hey, your arms look bigger,’” he says.
Daniel is part of a community of hormonal hobbyists looking to get cut—and cut corners doing it. Risking their long-term health on a largely untested and powerful substance in order to obtain what they consider an ideal masculine physique, they’re experimenting with selective androgen receptor modulators, or SARMs. Originally designed to strengthen cancer patients and to combat the withering of old age, these chemicals in low doses seem to enhance growth receptors without affecting testosterone levels. On bodybuilding forums and black-market sites, the drugs are being positioned as a cutting-edge alternative to steroids: no strict regimen of injections; no man boobs, anger issues, or acne. Best of all, the muscle appears to stick around after the dosing stops.
But you won’t find them on the shelves at GNC; SARMs are chemicals developed for critical medical interventions. None of the compounds have ever made it out of clinical trials or been studied in the amounts taken by men like Daniel. Their long-term effects are unknown. One study was aborted after test mice began bleeding from the rectum. But due to a loophole in federal law, SARMs can be purchased from secondhand pharmacological Web sites—that is, if buyers affirm that the drugs are being bought for “research purposes” for use on “laboratory animals.”
One evening while driving home from work, Daniel noticed his vision had gone green—as though food coloring had been dropped onto his pupils. His eyes were hazy, unable to focus under bright lights. Despite the obvious dangers to patients he operated on, Daniel didn’t seem to worry. “It’s one of the effects recorded in trials,” he reasons. “At least I know I’m getting the real deal.”
Like so many pharmaceutical breakthroughs, sarms were created accidentally. In 1997 doctors James Dalton and Duane Miller were searching for ways to block testosterone from aggravating receptors in the prostate. Along the way they inadvertently created compounds that activated certain muscle pathways while leaving others alone.
Known as the mother of all steroids, testosterone increases protein synthesis. Take it in excess and you’ll fill out your shirt until you can’t button the collar. Same with oral anabolics, which are liver toxic and frequently used with testosterone to build mass. But both are nonselective and carpet bomb the body, triggering receptors that prompt not only cellular growth but also hair loss, skin problems, and excess estrogen. When castrated mice were given an early SARM, however, muscle enlargement was far more significant than any other mild effect.
Dalton and Miller licensed their compound to pharmaceutical company GTx, Inc. and began developing the drugs as a treatment for muscle loss. GTx moved ahead with MK-2866, dubbing it Ostarine. Ligand Pharmaceuticals invested in another formulation, LGD-4033. Merck’s MK-677, a SARM-like chemical, was designed to counteract growth deficiencies; GlaxoSmithKline’s GW-501516 resulted in extreme endurance, with test rodents running 92 percent longer than average.
Dalton knew what would follow. Bodybuilders are always first in line for any drug with the potential to accelerate muscle growth, and it wasn’t long before profit-hungry labs supplying U.S. dealers began copying formulas out of journals. Drugs unsanctioned by the FDA are illegal to sell for human consumption, so most SARMs come in foul-tasting liquid form under the label of “research chemicals.” Several dozen Web sites peddle them. They accept all major credit cards; a few even traffic in bitcoin.
According to Rick Collins, an attorney specializing in steroid-related cases, both seller and buyer often know there’s no animal research. “The only one in the dark is the agency that’s supposed to be supervising the situation—the FDA,” he says. The Food and Drug Administration didn’t respond to requests for comment.
Most sites don’t list dosing instructions, so a thriving community of self-experimenters has emerged on online forums to swap tips and horror stories. One user who started taking SARMs at 17 claimed they wrecked his hormones. Others fretted about organ toxicity and liver damage.
Ed, a 223-pound data analyst and part-time bodybuilder, isn’t worried. “I’m absolutely a guinea pig,” he says.
For Ty, who has less than 10 percent body fat, testimonies on the forums “tend to convince me I won’t be killing myself,” he says. He guesses he’s used Ostarine nine times. Each multiweek cycle resulted in six pounds of mass and additional definition.
Ed added eight pounds during one cycle. Sure, anabolics could tack on roughly 10 to 15 in the same period, but the schedule can be exhausting: twice-weekly or daily injections, pills to avoid breast-tissue growth, and increased likelihood of a cardiovascular event. What’s more, with anabolics, “wet” gains—those that result in water retention—are often urinated away after cycles stop. SARM gains are said to be “dry,” with the muscle staying intact. But to Dalton, there are still too many unanswered questions.
“Quite honestly,” he says, “it scares me to death.”
As their name suggests, sarms are quite selective about what receptors they stimulate. But that’s only proved to be true in therapeutic doses. Bodybuilders’ early hopes that large amounts of SARMs wouldn’t turn off natural testosterone production were unfounded, and many have had to add other drugs to kick-start low-functioning testicles. Some have also reported bleeding gums and muscle spasms.
Ed tried 50 milligrams of Ostarine because he “wanted to see what would happen.” It was no more effective than the 25 recommended by forum advisers, but his liver enzymes shot up. One study found that at high amounts, GW-501516 induced tumors in mice. Both it and S-4 are no longer being developed but are still in use among gym rats.
It can be difficult to tell when adverse effects are due to the drug itself or tainted batches. Black-market labs aren’t known for sterility. After scanning a secondhand Ostarine bottle, Dalton noticed a missing ingredient. “The compound wouldn’t build muscle,” he says. “It could be safe or dangerous. Nobody knows.”
The lack of research has led many users to become amateur biochemists. Ed routinely pores over endocrinology journals; guys like Ty, who’s taken Ostarine for up to 16 weeks in a cycle and also saw his vision yellow on S-4, get blood work done before and after dosing to make sure they haven’t loosened a cellular bolt. “If I feel it becomes too much, I’ll stop,” he says.
On one forum, a user suggested eating more fiber to offset “the squirts”; another theorized the polyps risk would be reduced with an anti-inflammatory pill.
Some amateur reports are sophisticated, admits Abraham Morgentaler, M.D., a hormonal-therapy specialist. “But these are medications that change hormones, and they’ve never been studied adequately in humans. It’s hard to know the risks.”
For muscle chasers, risk is rarely an issue: Anabolic use surged in the 1970s, helping create the Gold’s Gym physiques. Testosterone was the base; anabolics were added to enhance effects. In the 1980s, lifters even began spiking and crashing their blood sugar with insulin to augment gains.
“Guys were going into comas and flirting with death,” says Randy Roach, author of the history Muscle, Smoke & Mirrors. “Insulin was hugely dangerous, but they didn’t care.” Then came the growth hormone, and the cartoonish proportions it created.
Today, lean is the new large. Companies line shelves with supplements that follow the trend. Some are spiked with anabolics to ensure results. The occasional scare emerges—one was pulled after causing liver failure—but most users aren’t put off. The problem is that lifters are often more informed than those scolding them, having discovered high- protein, low-carb diets and other hacks before they were recommended.
The pursuit of muscle often trumps common sense. “In 10 years, I don’t know what this stuff will do,” says Ty. “But so far, it hasn’t hurt me.”
Masculinity tagged with a ups tracking number is becoming harder to come by. This past winter, Congress quietly enacted the Designer Anabolic Steroid Control Act. It gives the DEA authority to target sellers of designer drugs, the anabolics-in-disguise that have long flown under its radar. Web sites immediately offered significant markdowns.
But SARMs are getting a pass—for now. “The way the statute is written, we have to be able to demonstrate a substance is chemically and pharmaceutically similar to testosterone,” says DEA spokesman Joseph Moses. “That makes them incapable of being controlled under the term anabolic steroid.” Perversely, then, the ban may make SARMs even more popular.
Athletic regulators are taking action, however. Both the World Anti-Doping Agency (WADA) and the U.S. Anti-Doping Agency (USADA) have banned SARMs from sporting events. Meanwhile, Ostarine is still being developed in hope of getting FDA approval; newer SARMs are being nursed by GlaxoSmithKline. If any come to market, they will be classified as prescription drugs. For the underground, it’s better that SARMs remain in developmental limbo, where the selling of “research chemicals” can continue.
That legal fudge is opening up new possibilities. Ty has been injecting a new compound called ACE-083 into his calves and biceps. After three days, he claims, he measured three quarters of an inch of muscle growth.
“Fuck, if 1 milligram did this,” he asks, “what will 50 do?”
Good question. Maybe let the lab rats help answer it.
Photos by Photo: Graeme Montgomery / Trunk Archive