Pharmaceuticals – Peptides

During ReGen’s discussions with potential licensing partners in 2004, it became apparent that a product based on the Colostrinin™ complex, as a whole, was more commercially attractive as a nutraceutical, rather than as a pharmaceutical.  It was decided, therefore, to develop the original formulation of Colostrinin™ as a nutraceutical.

ReGen did however continue to investigate the structure and properties of the individual peptides contained within the Colostrinin™ complex.

ReGen conducts its research through a number of scientific development collaborators worldwide, but much of the peptide research was carried out as part of our long-term relationships with the University of Texas Medical Branch in Galveston, Texas, USA (UTMB) and Roswell Park Cancer Institute of Buffalo, New York State in the USA. This work suggests that the peptides derived from Colostrinin™ may act in a number of ways that suggest utility in neurodegenerative diseases:

  • The reduction and/or prevention of oxidative stress
  • The reduction and/or prevention of apoptosis
  • The reduction and/or prevention of beta amyloid aggregation
  • The encouragement of neuronal cell production

Oxidative stress is a general term for the build-up of harmful reactive oxygen species (ROS) as a result of normal/abnormal cell metabolism. This age-related build-up gradually overwhelms the normal processes, in which ROS are neutralised, leading to the modification of important molecules (e.g. enzymes) and the impairment of their function, ultimately leading to disease. Oxidative stress has recently been implicated as a key feature in the development of many age-related disorders, including neurodegenerative diseases such as Alzheimer’s disease and Parkinson’s disease or multiple sclerosis.

Apoptosis, known as programmed cell death, is the mechanism by which cells are caused to die when they reach the end of their life expectancy. However, premature apoptosis is often triggered by many pathological conditions including inflammation. In Alzheimer’s disease, a particular example of brain inflammation, apoptosis is an important factor in progression of the disease.

Alzheimer’s disease is characterised by the accumulation of abnormal protein fibrils, including senile plaques, causing selective neuronal loss in the central nervous system. The primary components of senile plaques are insoluble aggregates of a peptide called amyloid beta. In addition, an abnormally high level of iron is witnessed in the brains of Alzheimer’s disease patients. This is thought to stimulate oxidative stress in the brain, giving rise to free radicals which then go on to damage cells and cause subsequent brain inflammation.

As a result of the actions described above, it has been shown that Colostrinin™ and its peptides encourage the production of neuronal cells and increase the life span of cells in general.In April 2005 ReGen announced that Colostrinin™ and a nine amino acid synthetic homologue of a Colostrinin™ derived peptide showed neuroprotection in a cell line model predictive of Parkinson’s disease. The Company is evaluating the activity of all the peptides derived from the Colostrinin™ complex. Our prime target remains the treatment of Alzheimer’s disease, particularly in view of the clinical results obtained from our trial RG 010 in Poland, but it is hoped that the continuing peptide-activity work will also show that there is efficacy in the treatment of other diseases such as Parkinson’s disease, Multiple Sclerosis, Amyotrophic Lateral Sclerosis and Huntingdon’s Chorea.  The Company has already announced that one of the peptides has shown in-vitro and in-vivo activity in Alzheimer’s disease and another in-vitro activity in Parkinson’s disease.

In December 2007, ReGen announced that the peptide programme had presented some interesting compounds for further development to a pre-clinical stage.  The Company’s scientists have, so far, selected three candidates, two of which may have potential utility in Alzheimer’s disease and a further candidate with potential utility in obesity.The Company seeking industry partners to take development of these peptides forward.