What are myostatin inhibitors?
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The bottom line
Myostatin inhibitors block the activity of myostatin in the body resulting in increased muscle mass. Clinical trials are investigating if they will benefit patients with muscle wasting illnesses. It is unclear if they work. They are not yet FDA-approved. Potential side effects include weakened tendons, reduced bone density, muscle spasm, bleeding disorders, and both vascular and cardiac damage.
Prevention Tips
If participating in a clinical trial, be aware of potential adverse effects and who to contact if you think you are experiencing toxicity.
Do not use myostatin inhibitors such as follistatin that can be purchased online.
Use non-pharmaceutical methods of inhibiting myostatin.
Do high intensity resistance training.
Participate in aerobic exercise (cycling, running, swimming).
Be sure your diet includes adequate protein.
Avoid overtraining.
Use supplements as directed that inhibit myostatin (cocoa, dark chocolate, green tea, black tea, vitamin D, creatine).
Speak with your physician before beginning a new exercise routine or taking any supplements.
This Really Happened
Eleven adult male body builders experienced decreased visual acuity and were admitted to a clinic. All patients had injected a high dose (1 mg) of follistatin-344 subcutaneously into the abdomen. They were diagnosed with central serous chorioretinopathy (CSCR) which is an eye condition where fluid leaks under the retina at the back of the eye. It was determined that this was due to follistatin. In the eight patients who had injected follistatin only once, symptoms improved and the fluid disappeared in an average of 2 months. The 3 patients with multiple follistatin injections developed recurrent CSCR.
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What are myostatin inhibitors?
Myostatin inhibitors are drugs that block the activity of myostatin. Myostatin is a protein in the body that limits the growth and development of muscle. There is research on using these drugs for muscle wasting conditions such as muscular dystrophy and sarcopenia. They are also being studied for cancer related muscle loss and along with GLP-1 drugs for weight loss without concomitant loss of muscle mass. They are usually given by intravenous infusion or subcutaneous injection. Examples of myostatin inhibitors include ACE-O31, bimagrumab, domagrozumab, landogrozumab, stamulummab, and trevogrumab.
There are naturally occurring myostatin antagonists such as follistatin (FST) that are available online; however, they may have other biological effects which makes their safety and efficacy uncertain. There are no approved pharmaceutical formulations of follistatin.
How do myostatin inhibitors work?
By inhibiting myostatin’s activity, myostatin inhibitors increase muscle mass and strength. Many are monoclonal antibodies that bind and neutralize myostatin. Others act as a decoy receptor that trap myostatin, which prevents it from binding with its natural muscle receptors.
Are myostatin inhibitors safe?
Clinical trials suggest that these drugs are generally safe, although there are potential risks with their use. They are not yet FDA-approved. They are banned by the World Antidoping Agency.
Do myostatin inhibitor supplements actually work?
It is unclear whether myostatin inhibitor supplements actually work. There are animal studies that showed efficacy. However, some clinical trials did not show benefits or were stopped early for safety reasons.
Side effects of myostatin inhibitors
Based on their mechanism of action, it is possible these drugs will weaken tendons and reduce bone density. Muscle spasms may occur. Some of these drugs cause bleeding disorders (nosebleeds, bleeding gums), and vascular damage. The thickness of the heart’s wall my increase due to an increase in the mass of cardiac muscles. There is a risk that increasing muscle mass may lead to fibrosis and blood supply issues that will affect muscle function.
Do myostatin inhibitors interact with other medications or supplements?
There is very limited information available on interactions, as myostatin inhibitors are still in clinical trials.
Of note, some supplements such as dark chocolate and cocoa that contain epicatechin naturally inhibit myostatin. Green tea, black tea, vitamin D, and high-dose creatine also inhibit myostatin. A potentially positive interaction being investigated is whether the combination of myostatin inhibitors and GLP-1 agonist can result in reduced body fat while preserving muscle mass.
What should you do if you have a bad reaction to a myostatin inhibitor supplement?
If you are participant in a clinical trial of a myostatin inhibitor and you are having a bad reaction, contact the clinical trial coordinator. If the adverse reaction is due to a myostatin inhibitor you purchased online, seek medical advice from a health care professional.
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