guardianactual
MuscleChemistry Registered Member
Pharmaceutical companies Acceleron Pharma and Shire have put the myostatin inhibitor ACE-031 on hold. They made an announcement about this in a joint press release recently [acceleronpharma.com May 2, 2013]. A strange development, as a few weeks previously Muscle & Nerve published a study that shows that ACE-031 is stuff that anyone who considers themself to be a chemical bodybuilder would be happy to be able to afford.
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</br>Injectable ACE-031 – an underground example is shown above – is a synthetic activin receptor type IIB. Muscle cells have this receptor too: it's intended for proteins like myostatin, GDF11 and activin A and B. If myostatin attaches itself to an activin receptor type IIB, then the growth of muscle fibres is inhibited. Under the 'right' conditions myostatin actually breaks down muscle.
</br>
</br> If you inject ACE-031 this doesn't happen at all. The synthetic activin receptor type IIB filters out the muscle inhibiting proteins and deactivates them.
</br>
</br> In 2007 Acceleron Pharma still had high expectations for ACE-031. At that point the company only had animal studies to back them up. But in 2013 they published the results of a human study, in which 48 healthy women aged from 45-75 had been given a single injection containing 0.02, 0.05, 0.1, 0.3, 1 or 3 mg ACE-031 per kg bodyweight. The substance remained in circulation in the body for a number of weeks: the half-life was 10-15 days.
</br>
</br> But the single injection did lead to muscle growth. The 3-mg/kg dose led to an increase in muscle of volume of 5 percent, it boosted lean body mass by 3 percent [just over a kilogram], and seemed to also reduce fat mass. (3mg per kg! What this stuff cost $150 per 1 mg!!!!)
</br> The injection reduced the leptin concentration and boosted that of adiponectin. This would suggest that ACE-031 breaks down fat mass. Moreover, the myostatin inhibitor boosted the concentration of bone specific alkaline phosphatase [BSAP] in the blood and reduced that of C-terminal type 1 collagen telopeptide [CTX]. This would suggest that ACE-031 strengthens bones. Acceleron has demonstrated these effects in animal studies using RAP-031, the mouse variant of ACE-031.
</br>
</br> If you read the article in Muscle & Nerve you wonder why Acceleron has put the development of ACE-031 on hold. And why it doesn't declare war on the web-shop owners who happily ignore Acceleron's patents and sell ACE-031 for prices that no ordinary pharmaceuticals company can compete with.
</br>
</br> The answer is in a post on the website of the Muscular Dystrophy Association. [quest.mda.org May 2, 2013] This describes a trial [NCT01099761] performed in 2011 in which researchers gave ACE-031 to children with muscular dystrophy. During the trial side effects emerged and the researchers had to stop the study.
</br>
</br> "The adverse events that the trial participants experienced — minor nose and gum bleeding and dilation of blood vessels in the skin — were not, in and of themselves, considered dangerous. However, the companies and regulatory agencies involved say they need to fully understand these events before continuing clinical studies of ACE-031."
</br>
</br> Some other strange side effects also came to light in the study published in Muscle & Nerve. ACE-031 caused the concentration of FSH in the women subjects to plummet. How this happened, and what the effects of this might be, the researchers don't know.
</br>
</br>Injectable ACE-031 – an underground example is shown above – is a synthetic activin receptor type IIB. Muscle cells have this receptor too: it's intended for proteins like myostatin, GDF11 and activin A and B. If myostatin attaches itself to an activin receptor type IIB, then the growth of muscle fibres is inhibited. Under the 'right' conditions myostatin actually breaks down muscle.
</br>
</br> If you inject ACE-031 this doesn't happen at all. The synthetic activin receptor type IIB filters out the muscle inhibiting proteins and deactivates them.
</br>
</br> In 2007 Acceleron Pharma still had high expectations for ACE-031. At that point the company only had animal studies to back them up. But in 2013 they published the results of a human study, in which 48 healthy women aged from 45-75 had been given a single injection containing 0.02, 0.05, 0.1, 0.3, 1 or 3 mg ACE-031 per kg bodyweight. The substance remained in circulation in the body for a number of weeks: the half-life was 10-15 days.
</br>
</br> But the single injection did lead to muscle growth. The 3-mg/kg dose led to an increase in muscle of volume of 5 percent, it boosted lean body mass by 3 percent [just over a kilogram], and seemed to also reduce fat mass. (3mg per kg! What this stuff cost $150 per 1 mg!!!!)
</br> The injection reduced the leptin concentration and boosted that of adiponectin. This would suggest that ACE-031 breaks down fat mass. Moreover, the myostatin inhibitor boosted the concentration of bone specific alkaline phosphatase [BSAP] in the blood and reduced that of C-terminal type 1 collagen telopeptide [CTX]. This would suggest that ACE-031 strengthens bones. Acceleron has demonstrated these effects in animal studies using RAP-031, the mouse variant of ACE-031.
</br>
</br> If you read the article in Muscle & Nerve you wonder why Acceleron has put the development of ACE-031 on hold. And why it doesn't declare war on the web-shop owners who happily ignore Acceleron's patents and sell ACE-031 for prices that no ordinary pharmaceuticals company can compete with.
</br>
</br> The answer is in a post on the website of the Muscular Dystrophy Association. [quest.mda.org May 2, 2013] This describes a trial [NCT01099761] performed in 2011 in which researchers gave ACE-031 to children with muscular dystrophy. During the trial side effects emerged and the researchers had to stop the study.
</br>
</br> "The adverse events that the trial participants experienced — minor nose and gum bleeding and dilation of blood vessels in the skin — were not, in and of themselves, considered dangerous. However, the companies and regulatory agencies involved say they need to fully understand these events before continuing clinical studies of ACE-031."
</br>
</br> Some other strange side effects also came to light in the study published in Muscle & Nerve. ACE-031 caused the concentration of FSH in the women subjects to plummet. How this happened, and what the effects of this might be, the researchers don't know.
