Santhera Licenses Melanocortin-4 Receptor Antagonist Program to BioLineRx

The preclinical activity spectrum of orally active MC-4R antagonists indicates beneficial efficacy in all key aspects of cachexia such as lack of appetite, increased resting energy expenditure and enhanced catabolism. The latest generation of compounds increased food intake 3- to 5-fold and inhibited the development of cachexia in a disease-relevant animal tumor model.

"We received considerable interest in this program and concluded that BioLineRx is the best partner for development of our selective, first-in-class MC-4R antagonists based on their excellent track record in developing similar stage assets to proof-of-concept in man," said Klaus Schollmeier, Chief Executive Officer of Santhera. "This agreement with BioLineRx fits well with Santhera's strategy to focus on its core late stage or marketed assets Catena®, fipamezole and omigapil."

About cachexia syndrome and MC-4R antagonists
Cachexia (Greek for "poor condition") is one of the most debilitating and life- threatening aspects of cancer and other severe diseases such as AIDS, chronic obstructive pulmonary disease (COPD), chronic kidney disease and chronic heart failure. The syndrome is associated with anorexia (lack of appetite), fat and muscle tissue wasting and consequently involuntary weight loss, psychological distress and/or depression and a progressively decreasing quality of life. Typically, weight loss due to cachexia cannot be compensated for by increased food intake, which results in wasting of both adipose and skeletal muscle tissue and poor physical performance. More than 50% of all cancer patients develop cachexia during the course of the disease, and cachexia is believed to be the cause of 20% of cancer deaths

Appetite-regulating peptides, pro-inflammatory cytokines and other regulatory peptides are considered to be major factors in the regulation of appetite and body weight. One pathway by which cytokines can induce anorexia is via an increase of pro- opiomelanocortin gene expression in hypothalamic feeding and energy regulating circuits, leading to an enhanced production of á-melanocyte stimulating hormone (á-MSH), a strong inhibitor of appetite. The MC-4R in the hypothalamus is a crucial target in the pathway through which á-MSH exerts its appetite inhibiting and energy wasting effects. The endogenous antagonist agouti- related protein (AGRP) as well as small molecule MC-4R antagonists increase food intake, reduce energy expenditure and catabolic activity. Accordingly, an interruption of this signaling pathway by means of MC-4R antagonists is seen as a promising treatment option for cachexia.

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About BioLineRx
BioLineRx Ltd. is a publicly-traded (TASE: BLRX) biopharmaceutical development company based in Jerusalem, Israel, with US offices in Rockville, Maryland. BioLineRx is dedicated to identifying, in-licensing and developing therapeutic candidates for unmet medical needs or that have advantages over currently available therapies. BioLineRx's current development pipeline consists of three clinical stage candidates as well as seven candidates in various pre-clinical development stages spanning a variety of indications, including central nervous system diseases, oncology, cardiovascular and autoimmune diseases. Two of BioLineRx's lead compounds have recently been out-licensed. BL-1040, an injected medical device developed for the prevention of cardiac remodeling in Acute Myocardial Infarction (AMI) patients was out-licensed in July 2009 to US company Ikaria Holdings Inc; and BL-1020, a New Chemical Entity indicated for the treatment of schizophrenia, was out-licensed (North America only), in July 2010 to Cypress Bioscience Inc. For more information about BioLineRx, please visit www.BioLineRx.com.


Catena® is a trademark of Santhera Pharmaceuticals.

For further information, contact
Santhera: Klaus Schollmeier, Chief Executive Officer Phone: +41 (0)61 906 89 52 klaus.schollmeier@santhera.com

Barbara Heller, Chief Financial Officer Phone: +41 (0)61 906 89 54 barbara.heller@santhera.com

Thomas Staffelbach, Head Public & Investor Relations Phone: +41 (0)61 906 89 47 thomas.staffelbach@santhera.com