Myostatin Propeptide ACE-031

The research towards the myostatin inhibitor ACE-031 was terminated - but it does work

The pharma companies Acceleron Pharma and Shire have put the myostatin inhibiter ACE-031 on ice. That have indicated. [Acceleronpharma.com May 2, 2013] And that's pretty weird. Them in a joint press release a few days ago

A few weeks earlier, Muscle & Nerve published a study showing that ACE-031 is a compound which a chemical bodybuilder would gladly add to his toolbox.

The injectable ACE-031  is a synthetic activin receptor type IIB. Muscle cells have that receptor too. It is intended for proteins as myostatin, GDF11 and activin A and B. If myostatin docks itself to the activin receptor type IIB, then the growth of muscle fibers reduces. Under the 'right' circumstances myostatin even breaks down muscle.

If you inject ACE-031, then that does not happen. The synthetical activin receptor type IIB captures the muscle inhibitory proteins away, and disable them.

In 2007 Acceleron Pharma had high expectations of ACE-031. Then the company had only performed animal studies. However, in March 2013 AP published a human study in which 48 healthy women aged 45-75 years received a single injection with 0:02, 0:05, 0.1, 0.3, 1 or 3 mg ACE-031 per kg body weight. The compound circulated a few weeks in the body. The half-life was 10-15 days.

However, this single injection did result in muscle growth. The dose of 3 mg / kg showed an increase of the muscle volume by 5 percent.  The lean body mass increased by three percent [just over a kilo], and also seemed to lessen. fat mass

The injection decreased leptin and increased concentration of adiponectin. That suggests that ACE-031 breaks down the fat.

In addition, increased the myostatin inhibiter the levels of bone specific alkaline phosphatase [BSAP] in the blood, and reduced that of the C-terminal type 1 collagen telopeptide [CTX]. This suggests that the ACE-031 makes bones stronger. In animal studies with RAP-031, the mouse version of ACE-031, Acceleron has been able to prove those effects.  [Endocrinology. 2010 Sep; 151 (9) :4289-300].

If you read the study in Muscle & Nerve, then you wonder why Acceleron has ceased the development of ACE-031.  And why it doesn’t take action against all the webshops and manufacturers, who wipe their butts with Accelerons patents - and sell ACE-031  for a price at which an ordinary pharmaceutical company can’t make any profit at all.

The answer to that is found in a message on the website of the Muscular Dystrophy Association. [Quest.mda.org May 2, 2013] That tells that in 2011 during a trial [NCT01099761], when researchers administrated ACE 031 to children with muscle disease, side effects came to light, that forced the researchers to stop the study.

"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 themelves, considered dangerous However, the companies and regulatory agencies Involved say they need to fully understand thesis events before continuing clinical studies of ACE-031. "

An other odd side effect was revealed in the study that was published in Muscle & Nerve. It showed that ACE-031 administration strongly decreased the FSH concentration in the female pwrticipants. The researchers do not know the cause, and what the consequences may be.

The study into MYO-029, the myostatinblokker from Wyeth, wasn’t succesfull either. In 2008 a disappointing study that showed that adults with muscular dystrophy, after administration with MYO-029,  did not get any stronger. [Ann Neurol. 2008 May, 63 (5) :561-71] And Wyeth discontinued the development of MYO-029..

Source:

Muscle Nerve. 2013 Mar; 47 (3) :416-23.