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BIOLINERX COMPLETES STUDY OF GABA-ENHANCED ANTIPSYCHOTIC

February 19, 2007

BioLineRx has successfully completed Phase I clinical trials of BL-1020, the first antipsychotic enhanced with gamma-aminobutyric acid (GABA) for the treatment of schizophrenia. The study results showed that BL-1020 was well tolerated and showed an improved safety profile by reducing extrapyramidal symptoms that are experienced with currently available therapies.

The Phase I trial was a randomized, double-blind, placebo-controlled, dose-escalation, single-center study in healthy adult males. The primary objective was to evaluate the safety and tolerability of escalating doses of BL-1020. The secondary objectives were to determine the pharmacokinetics of BL-1020, and to assess its ability to block activity of the neurotransmitter dopamine, implicated in schizophrenia.

A total of 48 volunteers were randomized and enrolled into six dose cohorts. In each cohort, patients received a single dose or matching placebo (4, 8, 16, 24, 32 or 40 mg). The results demonstrate that BL-1020 was well tolerated following administration of a single dose up to 40 mg, with no adverse drug-related effects on electrocardiogram parameters, clinical lab data and neurological assessments.

Clinical activity of BL-1020 was assessed by its ability to antagonize dopamine activity. The effect of BL-1020 on dopamine levels was assessed by monitoring serum prolactin, a surrogate marker for dopamine antagonism. The pharmacokinetics of BL-1020 were linear across the range of doses studied, as assessed by the dose-dependent elevation of serum prolactin levels.

Currently available drugs, which also reduce dopamine activity, induce significant clinical side effects, thereby limiting patient compliance, according to the company. The results are that BL-1020 is protective against extrapyramidal symptoms. In addition to dopamine hyperactivity, schizophrenia is also associated with hypo-activity of the neurotransmitter GABA, and BL-1020 also acts as a GABA enhancer by delivering GABA to the central nervous system.