|Mode of Action:||Gliadin Sequestering|
|Stage of Development:||Phase 1/2|
|Patent Status:||Patents granted or pending worldwide, 20 years expiration in 2026|
BL-7010 is a novel, high molecular weight, non-absorbable, orally available polymer intended for the treatment of celiac disease. It has a high affinity for gliadins, the immunogenic proteins present in gluten that cause celiac disease. By sequestering gliadins, BL-7010 effectively masks them from enzymatic degradation and prevents the formation of immunogenic peptides that trigger the immune system. This significantly reduces the immune response triggered by gluten. BL-7010 is excreted with gliadin from the digestive tract and does not get absorbed into the blood. BL-7010 is chemically stable at a wide pH range, non-biodegradable and is water soluble. It works by acting locally in the gastrointestinal tract and is not absorbed systemically; therefore, it has a very good safety profile as was demonstrated in pre-clinical studies.
A Phase 1/2 study with BL-7010 was successfully completed in 2014. The trial was a two-part (single and repeated), double-blind, placebo-controlled, dose escalation study in 40 patients. The primary objective of the study was to assess the safety of single and repeated ascending doses of BL-7010 in well-controlled celiac patients. Secondary objectives included an assessment of the systemic exposure, if any, of BL-7010 in the study patients. BL-7010 was found to be safe and well tolerated in both single- and repeated-dose administrations, and the optimal safe dose for future development was determined. In all single- and repeated-administration cohorts, pharmacokinetic analyses revealed no systemic exposure of BL-7010 in plasma and urine samples. BioLineRx expects to commence a randomized, placebo-controlled efficacy study towards the end of 2015 or the beginning of 2016, contingent on finalizing a regulatory pathway classification process of BL-7010 as a medical device in the EU.
In vitro, BL-7010 has been shown to specifically interact with gliadins and to prevent their toxic damage to the epithelial tissue. Experiments in vivo in a murine model of celiac disease have shown that BL-7010 prevents pathological damage to the small intestine, helps to preserve the integrity of the intestinal mucosa and reduces inflammation. In addition, it has been shown to have no toxic effects, even at high doses that are significantly higher than the expected clinical effective dose. Additional studies showed that BL-7010 is specific to gliadins, the immunogenic proteins present in gluten that cause celiac disease, and does not interact with various tested vitamins in the digestive tract. These results imply that BL-7010 will not affect the absorption of vitamins and therefore will not lead to malnutrition.
BL-7010 was invented by Prof. Jean-Christophe Leroux from the Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, ETH Zurich, Switzerland and is being developed by BioLineRx Ltd. under a worldwide exclusive license agreement with Univalor.
For more information: info@BioLineRx.com