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Showing posts with label STX209. Show all posts
Showing posts with label STX209. Show all posts

Wednesday, 27 November 2013

Autism Clinical Trials, Arbaclofen (STX209), Curemark CM-AT and the Clever Chiropractor


 
In the world of clinical trials for drugs, judging success and failure can be highly subjective.  They try to make it as logical as possible and the method works pretty well for assessing things that you can measure objectively.




Primary and Secondary Endpoints
To quote Pfizer:

A trial endpoint of a clinical trial should fulfill three criteria: (1) be measurable and interpretable, (2) sensitive to the objective of the trial, and (3) clinically relevant. The endpoint can be either clinical or surrogate in nature.
If you are developing a drug to lower cholesterol or to increase survivability after a traumatic brain injury, it is pretty easy to define your endpoints.

When it comes to autism, one of the major hurdles is to define objective measurable endpoints.  As it stands today, none of the assessment tools are really fit for purpose, when Big Pharma is supposed to come along and invest hundreds of millions of dollars in some bright spark’s idea.

Arbaclofen, Seaside Pharma & Roche
The Swiss giant, Roche, recently had just such a problem.  They had partnered with a spinout company from MIT called Seaside Therapeutics.  One of the projects was to complete the trials of a fragile X targeted drug, called Arbaclofen (STX209).  During the 4+ years of trials Seaside had changed the primary endpoint.  Arbaclofen started out as drug to treat one aspect of behaviour, but by the time they got to phase 3  clinical trials this had been changed to lethargy and social withdrawal scores from the Autism Behavior Checklist (ABC).
Quite logically, Roche assessed the result of the stage 3 trial against its primary endpoint.  Based on the total cohort in the trial, Roche determined the drug to be a failure and pulled the plug on financing the drug further.
The owner and developer of the drug, Seaside, even though they have recently raised $90 million, said they could no longer continue to fund the trial and all those kids in the trial would have to be weaned of Arbaclofen ASAP.
It turns out that among the families involved in the trial there were many reports of wonderful improvements on Arbaclofen.  They even formed a group to lobby for a continuation of the trial.  There website is interesting.
It now appears that Seaside has had a rethink and will try again with a new trial with a new primary endpoint (mark 3).

Background on Arbaclofen
Some of the first studies of Arbaclofen were conducted in patients with Fragile X syndrome, a genetic condition caused by a change in a gene called FMR1, which normally is needed to make the brain grow properly. Fragile X is the most common form of inherited intellectual disability in boys and can be a cause of autism or related disorders. In those Phase 2 trials, Arbaclofen was shown to decrease social withdrawal and improve adaptive social function.

A  Phase 2a study conducted at 8 sites and involving 32 children showed significant positive behavioral outcomes, including improved scores on the Aberrant Behavior Checklist-Irritability Score (ABC-I) and on the ABC-Social Withdrawal Scale. The most common adverse events were agitation, irritability, fatigue, psychomotor hyperactivity, insomnia and diarrhea. Most resolved without dose changes, but one serious adverse effect did occur during down-titration of the medication.
In July 2011, Seaside Therapeutics, announced that 25 sites across the nation will be involved in a new clinical trial to involve approximately 150 ASD patients between the ages of 5 and 21.
STX209 is an orally-administered GABA-B agonist; the drug acts by stimulating the release of GABA, a neurotransmitter in the central nervous system. GABA inhibits the release of glutamate, an excitatory neurotransmitter, for which an overabundance negatively affects the ability of neurons to communicate with each other.

The GABA "A" receptor, is a chloride channel, while STX209 targets the GABA "B" receptor, which is a G-protein coupled receptor and regulates a different set of molecules from GABA "A".

The original basis for starting this blog was my success with bumetanide, which is affecting the GABA “A” receptor.  In the brain, bumetanide blocks the NKCC1 cation-chloride co-transporter and thus decreases internal chloride concentration in neurons.


Medicine as an art and a science
Mark Bear is a neuroscientist at MIT and he was the co-founder of Seaside Therapeutics.  He is clearly a very brainy guy.
There is a derivative of his Arbaclofen called Arbaclofen Placarbil.  I found it interesting that this substance was also being trialed as a therapy for Multiple Sclerosis and GERD.  GERD is the medical term for heartburn/indigestion.
Incidentally, Arbaclofen Placarbil failed both trials.


Now to the Clever Chiropractor and her Pancreatic Enzymes
People outside the US will find it very strange that in the US chiropractors and osteopaths have the same right to prescribe drugs as conventional medical doctors. 

Outside of the US, if you want to be a doctor you have to apply to medical school and in most countries the competition is very tough. There is no plan B if your exam grades slip.  In the US it is different, if your grades and resources are not taking you to the Harvard, you can opt to become an osteopathic physician or a chiropractic physician.
Rather than Harvard or MIT, Joan Fallon trained as a chiropractor at Palmer University.

Not surprisingly the scientific community is skeptical of her autism treatment, which is linked to pancreatic enzymes.  After all, how can a chiropractor know more than Ivy League neuroscientists?

Peter, on the other hand, thinks that Fallon is actually far more savvy than the very brainy people over at Seaside.  Her therapy may, or may not be effective, but her method of developing it is highly effective.
First she raised $6 million to start her company Curemark, then as trials progressed she very recently she raised another $18 million.
The reason I like what Fallon is doing is that she has figured out which sub-type of autism is helped by her therapy and she has identified a bio-marker for that subgroup.


Hallelujah, a street-smart autism researcher !
If you want to enroll in a clinical trial for Curemark’s CM-AT, first they will screen out the 50% that do not have the biomarker.  Fallon is making sure that her clinical trial results look as good as possible, by only including those subjects most likely to benefit.  This may sound like common sense, but in autism research this is a revolution.

CM-AT therapy and the biomarker
The reason the autism world are skeptical of Fallon, is that she is going on about Secretin and pancreatic enzymes.
Many years ago parents thought that Secretin was going to be the wonder cure for autism; it turned out not to be.  By reading her patents, it is clear that Fallon has some faith in the role of secretin, in addition to enzymes produced in the pancreas.

What impressed me was how she has screened the kids allowed into her clinical trials.


Eligibility
·         Inclusion criteria:
o    Child is 3-8 years old
o    Child has a diagnosis of autistic disorder
o    Child must have a low fecal chymotrypsin level (we will measure)

·         Exclusion criteria:
o    Child must have no dietary restrictions (other than for a nut allergy)
o    Child may not have an allergy to pork products
o    Child may not have a history of severe head trauma or stroke
o    Child may not have had a seizure within the past year
o    Child may not be diagnosed with: HIV, cerebral palsy, endocrine disorder or pancreatic disease
o    Child may not be taking any enzyme product, amino acids, secretin product or stimulant medication currently 

Low fecal chymotrypsin level” is a standard lab test available all around the world.  Over the years Fallon has found that it is a biomarker of the kids who benefit from her patented mix of enzymes sprinkled on their meals.
You actually can buy a very similar product called Creon, or Kreon, depending on which country you live in.  The reason why you cannot be in the trial if you have a pork allergy, is that they use the pancreas of dead pigs to make the enzymes.  This is bad news if you are Jewish, Muslim, a Seventh Day Adventist, or indeed the pig.

The active ingredient in Creon is Pancreatin. Pancreatin contains the pancreatic enzymes lipase, amylase and protease. These assist the digestion of fat, carbohydrates and proteins.

Update on trials of CM-AT
Here is a link to the always-helpful Simons Foundation, with the expected skeptical comments from experts:-

 https://sfari.org/news-and-opinion/news/2010/first-drug-for-autism-enters-final-stage-of-testing

Now Curemark have finished there phase 3 trial, and guess what? It met both primary and secondary endpoints and has been “fast-tracked” by the FDA.

Congratulations Joan !!!
One of the secrets of her success was to have the good sense to enroll herself in a course on clinical investigation run by Harvard/Massachusetts general hospital.
 
Curemark Begins NDA Submission for CM-AT Autism Treatment
CM-AT had previously been granted Fast Track status by the FDA, a designation given to drug candidates that treat serious or life-threatening conditions and demonstrate the potential to address unmet medical needs. The rolling submission process allows companies with a Fast Track designation to submit the NDA in sections to the FDA as they are completed.
“Initiating our ‘rolling NDA’ submission is a major step in the registration process for CM-AT,” said Dr. Joan Fallon, Curemark founder and CEO. “We have an extraordinary opportunity to help many children with autism improve the quality of their lives and we will continue to work closely with the FDA to make that happen.”
Curemark previously announced the successful completion of its Phase III multicenter clinical trial of CM-AT for autism. CM-AT met both primary and secondary endpoints in its double-blind, randomized, placebo-controlled study of children with autism at 3 to 8 years of age.



  
Conclusion

I would suggest those researchers who believe that diet can be an effective therapy in sub-types of ASD take good note of Joan Fallon's methods. You might indeed be right, but unless you can prove it, the skeptics will always hold sway.