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(photo credit: Courtesy Photo)
A worldwide licensing arrangement for the development, production and marketing of an antiepileptic drug invented at the Hebrew University of Jerusalem has been signed by Shire Pharmaceuticals - a multinational firm with operations in North America, Europe and the Far East - with Yissum, HU's technology transfer company.
The efficacy of valrocemide as an antiepileptic drug has been demonstrated in a small clinical study, and Shire intends to study the drug as a candidate for application in a number of central nervous system conditions.
Valrocemide was discovered by a team led by Prof. Meir Bialer of the Hebrew University School of Pharmacy. Bialer, a leader in the discovery of antiepileptic agents, has authored over 180 publications in the area of pharmacokinetics, antiepileptics and central nervous system (CNS) drugs.
Epilepsy, a widespread neurological disease, affects approximately one percent of the world's population, and sales of antiepileptic drugs in the US alone are more than $3 billion annually.
There are several existing drugs on the market for patients with epilepsy. However, about one-third of the patients do not react positively to these treatments and they continue to suffer periodic epileptic seizures. There is a need, therefore, to develop new anti-epileptic drugs that will provide relief to patients who are not seizure-free or who suffer serious side effects from existing drugs.
The brain contains amino acids that serve as neurotransmitters, either excitatory or inhibitory neural transmissions within the central nervous system. Epilepsy is caused, among other reasons, by disturbances in the balance between these two functions: a rise in the level of the excitatory amino acids or a reduction in the level of the inhibitory acids. Glycine is one of the inhibitory amino acids, and increasing its concentration in the brain has an antiepileptic effect. However, it is impossible to administer it to patients in its natural state, because it does not penetrate the blood-brain barrier that prevents medications from reaching their CNS target sites.
Bialer's research team, which included his former doctoral student, Dr. Salim Hadad, worked to develop a glycine derivative that would penetrate the blood-brain barrier and would subsequently be cleared out of the body by a pre-designed elimination pathway in order to avoid undesirable side effects, which may be caused by toxic metabolic substances (metabolites).
Valrocemide is a combination of a known antiepileptic drug, valproic acid, and a glycine derivative, glycinamide. The new drug has been shown to be one of the most effective drugs among a large, analogous series of molecules that have been developed in Bialer's laboratory.