The new antiepileptic drug valrocemide, developed at the Hebrew University of Jerusalem by Meir Bialer, the David Eisenberg Professor of Pharmacy, will undergo phase three clinical trials in the U.S. under a new agreement between Teva Pharmaceutical Industries of Israel and Acorda Therapeutics of the U.S.

Teva acquired the rights to the drug from the Hebrew University's Yissum Research Development Company for the production of a treatment for epilepsy and other neurological and psychiatric diseases.

Epilepsy is a widespread neurological disease. Approximately one percent of the world's population suffers from it, and annual sales of antiepileptic drugs in the U.S. amount to more than $2 billion per year.

There are several existing drugs on the market for patients with epilepsy. However, some one-third of the patients do not react positively to these treatments, and as a result they continue to suffer periodic epileptic seizures. There is a need, therefore, to develop new 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 activating or inhibiting 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 activating (excitatory) amino acids or a reduction in the level of the inhibitory acids.

Glycine is one of the inhibitory 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 cannot penetrate the blood-brain barrier that prevents medications from reaching their target sites.

Prof. Bialer's research team, which included his former doctoral student, Dr. Salim Hadad, worked to develop a glycine derivative which 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).

The new drug, valrocemide, is a combination of a known antiepileptic drug, valproic acid, and a glycine derivative, glycinamide. Valrocemide has been shown to be one of the most effective drugs among a large, analogous series of molecules which are being developed in Prof. Bialer's laboratory.

The drug's patent is owned by the Hebrew University's Yissum Research Development Company, which awarded the production rights to Teva Pharmaceuticals.

The drug has successfully passed the first phase of clinical trials, and Teva has completed a 13-week, phase two clinical trial in Europe with therapy-resistant epileptic patients, in which valrocemide was administered together with other medications.

The agreement signed between Teva and Acorda Therapeutics will permit the initiation of large-scale clinical testing (phase three clinical trials) involving hundreds of epileptic patients. Additionally, the drug is also to be tested for its possible beneficial effects on patients suffering from manic-depression, as well as for treatment of neuropathic pain.

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Contact: Jerry Barach, jerryb@savion.huji.ac.il, 972-2-588-2904, Hebrew University of Jerusalem

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