D-Pharm's Novel Drug-Candidate, DP-109, Reduces Amyloid-Beta Plaque Deposition In Models of Alzheimer's Disease.REHOVOT, Israel -- REHOVOT, Israel, March 13 /PRNewswire/ -- D-Pharm Ltd. announced today that it has received exciting new results from two independent studies. These studies demonstrate the clear effect of DP-109 on amyloid beta (A-beta) deposition in both in vitro and in vivo models of Alzheimer's disease Alzheimer's disease (ăls`hī'mərz, ôls–), degenerative disease of nerve cells in the cerebral cortex that leads to atrophy of the brain and senile dementia. . DP-109 is the second compound to emerge from D-Pharm's Membrane Active Chelator chelator A chemical–eg, EDTA that binds metal ions from solutions. See Chelation therapy. (MAC) drug discovery program, as a lead candidate for combating neurodegenerative disease Neurodegenerative disease
A disease in which the nervous system progressively and irreversibly deteriorates.
Mentioned in: Amnesia .
In the first study, DP-109 was tested in vitro in a rapid aging model recently developed by Thuris, in Irvine, California. In this rat hippocampal hip·po·cam·pus
n. pl. hip·po·cam·pi
A ridge in the floor of each lateral ventricle of the brain that consists mainly of gray matter and has a central role in memory processes. slice model, characteristics of Alzheimer's disease pathology emerge upon reaching critical intraneuronal accumulation of A-beta. DP-109 was found to significantly reduce uptake of A-beta by neurons, and this effect was accompanied by large decreases in microglial proliferation and activation
In a second study an in vivo transgenic mouse model for Alzheimer's disease, oral administration of DP-109 for 3 months was found to significantly decrease the insoluble A-beta, A-beta plaques and consequent amyloid amyloid /am·y·loid/ (am´i-loid)
1. starchlike; amylaceous.
2. the pathologic, extracellular, waxy, amorphous substance deposited in amyloidosis, being composed of fibrils in bundles or in a meshwork of polypeptide burden, compared to the vehicle treated group. This study was performed by Drs. J-Y Koh and J-Y Lee of the Department of Neurology at the, University of Ulsan The University of Ulsan was founded on February 19, 1969 as the Ulsan Institute of Technology. The University was promoted to a fully-fledged University on March 1, 1985. Located in Mu-guh dong (i.e. , Korea and involved using human mutant beta-amyloid precursor protein transgenic (Tg2576) mice.
Dr. Itzchak Angel, D-Pharm's Vice President for Research and Development said: "The results of these studies are significant and encouraging. We have clearly shown that DP-109 interferes with amyloid-beta deposition both in vitro and in vivo. This is important validation of D-Pharm's drug discovery platform as a generator of useful drug candidates for neurodegenerative and other diseases."
About the MAC technology
In many pathological conditions the ability of the membrane to control ion flux is disrupted, resulting in the loss of metal ion homeostasis homeostasis
Any self-regulating process by which a biological or mechanical system maintains stability while adjusting to changing conditions. Systems in dynamic equilibrium reach a balance in which internal change continuously compensates for external change in a feedback . Disrupted metal ion homeostasis is symptomatic of numerous diseases, ranging from inflammation, cardiac arrhythmia, myocardial infarction and acute stroke to chronic neuro-degeneration (e.g. Alzheimer's and Parkinson's diseases). D-Pharm's breakthrough was to recognize that many critical processes, involving metal ions, occur within the unique environment of the cell membrane itself, rather than in surrounding body fluids. Membrane Active Chelator (MAC) drugs are, therefore, designed to bind metal ions such as copper, zinc, calcium and iron selectively within cell membranes and membrane milieus, rendering the action localized and safe. MAC drug candidates are unique in that they operate at a number of different levels in the disease process, providing a broad base for protection. The company's most advanced MAC based products, DP-b99, has recently completed Phase IIa trials for acute stroke. The preliminary results of this trial were announced earlier this week.
Excessive metal dependent protein aggregation and impairment of metal homeostasis leading to cell damage and neuroinflammation is of particular relevance to neurodegenerative disease. DP-109, the second drug to emerge from D-Pharm's MAC drug discovery program, has been designed so that it selectively chelates calcium and transition metal ions in lipophilic lipophilic,
adj/n the ability to dissolve or attach to lipids.
adj 1. showing a marked attraction to, or solubility in, lipids.
2. environments, and thus may interfere with metal dependent pathological processes. DP-109 is under development as a safe, oral treatment for chronic neurodegenerative disease. DP-109 is currently in the preclinical development stage.
About Alzheimer's disease
Currently more than 2% of the population aged 55 and over in developed countries (the United States, Western Europe and Japan) is affected by Alzheimer's disease. Growth in the number of elderly in these markets is expected to increase the total prevalence to greater than 10 million within the next 5 years. No effective treatment is available to prevent or reverse the deterioration that results from Alzheimer's disease. With no truly neuroprotective drugs on the market, there is a huge unmet need for new therapies.
D-Pharm (http://www.dpharm.com/) is a biopharmaceutical company pioneering the development of lipid-based therapeutics. D-Pharm is engaged in both drug targeting and drug discovery based on the company's technological platforms: (i) Regulated Activation of Prodrugs (D-RAP(TM)); (ii) Membrane Activated Chelators (MAC); and (iii) LipidoMimetix(TM). This has enabled the company to generate a rich pipeline of innovative drugs for the treatment of CNS See Continuous net settlement.
See continuous net settlement (CNS). disorders, cancer, and autoimmune diseases. The company's business strategy is to develop its products through "proof of principle in man" and to seek partners for advanced clinical development and commercialization.
CONTACT: Israel - Andrea Klainer, +972-8-9300794, or Fax, +972-8-9300795, firstname.lastname@example.org, or US - Patricia Nasshorn, +1-215-598-7004, or Fax, +1-215-598-8959, or Mobile, +1-215-588-8484, email@example.com, both of D-Pharm Ltd.; Rachel Crossley, Senior Consultant of Global Consulting Group, Fax, +44-20-7724-5338, firstname.lastname@example.org, for D-Pharm Ltd.
Web site: http://www.dpharm.com/