"We are pleased to be presenting these promising results for BL-1020 at the APA Annual Meeting and look forward to the imminent initiation of the Phase II trial for this compound," commented Morris C. Laster, M.D., chief executive officer of BioLineRx.
The results of this trial were as follows:
1. BL-1020 demonstrated dopamine blockade by dose dependant elevation in serum prolactin levels which serves as a surrogate marker for dopamine antagonism. Dopamine hyperactivity is implicated in schizophrenia, and is the mechanism of action for various antipsychotic drugs.
2. In this trial BL-1020 appeared to be protective against extrapyramidal symptoms, a severe side effect of many antipsychotic medications. BL-1020 was extremely well tolerated in that no ECG psychiatric or neurological abnormalities were seen at any of the doses tested.
About the BL-1020 Phase I Clinical Trial
The Phase 1 trial of BL-1020 was a randomized, double blind, placebo-controlled, dose-escalation, single center study in healthy adult males (ages 21-45). 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.
48 volunteers participated in the Phase I trial. They were randomized and enrolled into 6 dose cohorts at a ratio of 6:2 (BL-1020: placebo). 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 ECG parameters, clinical lab data and neurological assessments.
BL-1020 is an orally available GABA enhanced antipsychotic clinical candidate for the treatment of schizophrenia. Data from preclinical and phase I studies demonstrated that the compound may retain the efficacy of currently available typical and atypical antipsychotic drugs while achieving a much higher safety profile as evidenced by a lack of metabolic or extrapyramidal side effects.
BL-1020 is designed to simultaneously target the dopamine hyperactivity and GABA hypoactivity of schizophrenia. Exogenously administered GABA is ineffective as a therapeutic agent due to its inability to cross the blood brain barrier. Pharmacokinetic studies demonstrate that BL-1020 provides effective transport of GABA into the brain, overcoming this challenge. Receptor binding studies indicate that BL-1020 has a high affinity to dopamine and specific GABA-A agonist activity. This unique clinical profile may explain the reduction in side effects observed in animals and may contribute to improving cognitive function in schizophrenia.
BL-1020 is being developed by BioLineRx, Ltd. under a worldwide exclusive license from Ramot at Tel Aviv University Ltd. and Bar-Ilan Research and Development Company Ltd., the technology transfer arms of Tel Aviv University and Bar-Ilan University respectively. BL-1020 was discovered by Professor Abraham Nudelman fro m the Department of Chemistry, Bar-Ilan University; and Ada Rephaeli, Ph.D., Professor Abraham Weizman, MD, and Irit Gil-Ad, Ph.D. from the Sackler Faculty of Medicine, Tel Aviv University.
BioLineRx, a clinical stage drug development company traded on the Tel Aviv Stock Exchange (TASE:BLRX), is dedicated to building a robust pipeline of promising therapeutics for unmet medical needs. The Company's leading programs are for schizophrenia and treatment of damaged heart tissue post-myocardial infarction. Additional products under development include compounds for the treatment of cancer and CNS, cardiovascular, metabolic, infectious and autoimmune diseases.
BioLineRx advances projects from early stage discovery and lead generation to advanced clinical trials, regulatory approval and marketing. Partnering with researchers, universities and biotech companies to further the commercialization of promising compounds, BioLineRx seeks to enrich the pipeline of large pharmaceutical companies seeking their next blockbuster drugs. The Company was founded in 2003 by leaders in the Israeli life science arena including Teva Pharmaceuticals Ltd, Giza, Pitango, Hadasit and the Jerusalem Development Authority. For more information, please visit www.biolinerx.com.
This press release contains "forward-looking statements." These statements include words like "may," "expects," "believes," "scheduled" and "intends," and describe opinions about future events. These forward-looking statements involve known and unknown risks and uncertainties that may cause the actual results, performance or achievements of BioLineRx to be materially different from any future results, performance or achievements expressed or implied by such forward-looking statements.
Yuri Shoshan, +972-2-548-9100
VP Finance and Corporate Development
Tsipi Haitovsky, +972-52-598-9892
Stern Investor Relations, Inc.
Melanie Friedman, 212-362-1200