BioLineRx Announces Results of Clinical Receptor-Occupancy Study of BL-1020, a First in Class GABA-Enhanced Antipsychotic for the Treatment of SchizophreniaJERUSALEM--(BUSINESS WIRE)--Jul 16, 2007 - BioLineRx Ltd. (TASE:BLRX), Israel's leading drug development company, announced today the successful completion of a study determining the clinical binding properties of BL-1020 to the dopamine receptors in the human brain. The study has shown that BL-1020, the first GABA enhanced antipsychotic clinical candidate for the treatment of schizophrenia, blocks dopamine receptors in the human brain, providing direct evidence of antipsychotic efficacy. The study further supports the safety of BL-1020. In addition, this study provides evidence that the 32 mg will be clinically efficacious and that BL-1020 can be given once daily.
BioLineRx expects to initiate its Phase II maximum tolerated dose clinical trial for BL-1020 later this quarter. The Phase II trial sites have already been selected in Romania and the Company is currently awaiting final Romanian regulatory agency approval.
"We are very pleased with the promising results of this receptor occupancy study, which provides us with important information regarding the dosage, mechanism of action, safety and efficacy of BL-1020," stated Morris C. Laster, MD, chief executive officer of BioLineRx. "This study supports our belief that BL-1020 holds great potential as a next generation antipsychotic with the potential to be efficacious with minimal therapy-limiting side effects, and we are looking forward to the initiation of the Phase II trail."
The study's primary objective was to investigate receptor occupancy of BL-1020 in the human brain. The trial also supplies additional safety, tolerability and pharmacokinetic data. The study, conducted at Uppsala, Sweden, was designed as a single-center, randomized, open label clinical study performed on three cohorts, each with four healthy male subjects (age 21-35) receiving a single dose of 16, 24 or 32 mg of BL-1020. Receptor occupancy was assessed using PET scans at 1.5, 6, or 24 hours post dosing.
The PET data demonstrated a dose dependant increase in dopamine occupancy that supports the 32mg dose as being able to achieve clinically efficacious dopamine blockade. The efficacy of BL-1020 was also demonstrated by measuring the elevation in prolactin levels, an accepted marker for dopamine activity. There was a dose dependent change in prolactin level at 4 hours post dosing, further validating earlier Phase 1 results. Safety and tolerability data show that there have been no significant changes in ECG, vital signs or physical examination, clinical chemistry or hematology values.
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 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 from 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.
Schizophrenia is a serious mental disorder that affects about 1% of the world's population. It is a multifactorial disease characterized by delusions and hallucinations, emotional withdrawal and apathy, poor attention and disorganization. In 2002, the overall cost of schizophrenia in the United States was estimated at $62.7 billion, and the market for schizophrenia therapy in the U.S. is estimated to reach approximately $10 billion in 2012.
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
Posted: July 2007