Application in bodybuilding

Author: Yuri Bombela

It's not often that you can get your hands on the results of studies concerning peptides. Those very same peptides that are very popular in Ukraine and Russia. In this case, we are talking about one peptide, more precisely, a propeptide - ACE-031, which is a myostatin inhibitor.

It should be said that the company that synthesized ACE-031 - Acceleron Pharma - has stopped research on it. For how long or not, it is not yet known. But the propeptide is still being synthesized by outside labs and is on the market. Therefore, it is worth talking about it, especially since myostatin inhibitors are a rather vast and interesting topic. In this case, we will talk about a quite official study, the results of which were published in the March issue of the scientific journal Muscle & Nerve.

48 people took part in the study. All of them were women aged 45-75 years (women are usually selected for such experiments to minimize the influence of external factors, particularly testosterone). They were given only one injection of ACE-031, but in different amounts: 0.02, 0.05, 0.1, 0.3, 1 and 3 mg per kilogram of body weight. One injection in this case was quite enough, as the half-life of the drug is about 20 days. Plasma concentrations build up quite rapidly, reaching a maximum within about 3-4 days. After 8-10 days the concentration starts to decrease gradually.

It should be said that satisfactory results were obtained only with very large injections - 1 and 3 mg per kilogram of body weight. The other dosages did not give any special advantage compared to placebo injections. However, the "three-milligram" group got a significant increase in muscle volume - 5 percent. Dry muscle mass increased by 3 percent and some fat was lost. I emphasize: three percent for a 100 kg athlete is 3 kg of muscle, which "grows" in just two or three weeks.

But we are talking about MILLIGRAMS per kilogram of weight. ACE-031 is usually sold in bottles containing just 1 mg (1000 mcg). Can you imagine how many of these vials would be needed for just one injection? Finally, it is also worth mentioning why Acceleron Pharma has stopped research on its myostatin inhibitor for now.

The fact is that in a slightly earlier experiment on children, spontaneous bleeding from the nose and gums, as well as distension of blood vessels, were found in a number of subjects. In the above-mentioned experiment on women, almost all of the subjects had dramatically decreased FSH levels. Maybe there is nothing dangerous in these "side effects," but the specialists from Acceleron Pharma have decided to look into everything thoroughly - to be on the safe side. Those who still buy ACE-031 inject it at their own risk.

Other peptides

GHRP-2

GHRP-6 (Hexarelin)

GRF(1-29)

CJC-1295

Ipamorelin

HGH Frag (176-191)

Melanotan 2

TB500

ACE-031 Clinical Trials.

In A May 2, 2013, press release, Acceleron Pharma and Shire PLC announced that they have reached a conclusion about their collaboration on ACE-031 and related molecules, and that they will not embark on a restart of this program. John Knopf, CEO of Acceleron said: "While we express our dissatisfaction with the results of the ACE-031 program, at the same time we have gained valuable insights that can be used as Acceleron conducts the development of new compounds, also they may benefit our patients in the future."

In another development, dated May 2, 2013: when contacted by Jane Larkindale, AMD's vice president of research, Kenneth Atty of Acceleron and Lawrence Charles of Shire reported that the ACE-031 clinical trial had been suspended since February 2011. "Since that time," they continued, "we have submitted a number of additional preclinical and toxicology studies, but unfortunately, the results of those studies do not provide further development." They thanked AMD for its participation in the ACE-031 program and noted that: "Every company remains committed to developing new therapies for AMD and other rare diseases."

The following is the original story on the search - "ACE-031 clinical trial of Duchenne muscular dystrophy suspended for now," - published May 3, 2011.

On April 21, 2011, biopharmaceutical companies Acceleron Pharma and Shire announced that the AMD-supported ACE-031 clinical trial for Duchenne muscular dystrophy (DMD) has been suspended.

Work on the phase 2 dose-escalation study of ACE-031 in boys with DMD has been stopped, and the extension of the clinical trial for boys, which was completed as part of the original study, has been suspended based on preliminary safety-related data.

Both studies were conducted in Canada, and the plan was to open research centers in the United States sometime in the future.

The adverse events experienced by trial participants-significant bleeding from the nose and gums, and dilatation of blood vessels in the skin, both generally and in themselves-were not deemed dangerous. Nevertheless, the companies and regulators involved say they need a full understanding of these events before clinical trials of ACE-031 will proceed.

The development of ACE-031 was fully discussed in the April 2011 issue of AMD's health and quarterly research magazine Quest. The discussion was published under the title "A Distracting and Unwanted Protein." The companies hope to resume testing of ACE-031 once safety issues are fully investigated.

Acceleron and Shire are completing studies of ACE-031 in rats and monkeys. Researchers will analyze human and animal data to gain insight into the resulting, adverse events. The companies say they hope to restart human trials of ACE-031 after the results of these assays are received and reviewed by the U.S. Food and Drug Administration (FDA) as well as Health Canada.

Acceleron and Shire issued the following statement on April 21:

"In order to maintain a situation in which the Duchenne Muscular Dystrophy Association will be kept informed, Acceleron and Shire are going to provide updates on the status of the ACE-031 clinical program."

"In clinical trials in healthy adults and boys with DMD, some participants experienced minor nasal bleeding, bleeding gums and/or slight dilation of blood vessels in the skin. These phenomena were completely resolved after discontinuation of treatment."

"Minor bleeding and dilation of blood vessels themselves were not considered a serious safety concern in the context of this study."

"However, based on a review of this safety data with the FDA and Health Canada, Acceleron discontinued the A031-03 DMD study and suspended recruitment and dosing in the subsequent expanded A031-06 study."

"Acceleron and Shire remain associated with the international DMD clinical program as well as the ACE-031 development project. In pursuit of these goals, we express our intention to initiate new ACE-031 studies as part of our work with DMD, with appropriate monitoring of issues as well as follow-up discussions with regulatory authorities."

"In the coming months, we will provide new information to the MDD association, as we are expected to do."

Significance for families associated with Duchenne muscular dystrophy

The emergence of safety concerns associated with an experimental drug is never good news for families expressing hope for new therapies. Nevertheless, clinical trials of an experimental drug are inherently risky. And its benefit to patients, who could potentially experience serious side effects, must be considered in terms of side effects, which must be clarified before they pose a health or life threat.

"While we are disappointed by this turn of events in the development of ACE-031, it underscores the importance of properly designed and controlled studies," says Sanjay Bidichandani, MDA vice president of research.