BL-8040

BL-8040, a 14-amino acid synthetic cyclic peptide, is a novel, best in class, high-affinity CXCR4 antagonist with long receptor occupancy (>48 hours) and extended CXCR4 inhibition. BL-8040 is developed for the treatment of solid tumors, hematological malignancies and indications requiring hematopoietic stem cell transplantation.

BL-8040 pipeline is based on the vital roles of CXCR4-CXCL12 (SDF-1) interactions in oncologic processes (growth, invasion, survival, angiogenesis and metastasis) in various cancer types and in the maintenance of hematopoietic stem cells, immune cells and hematopoietic cancer cells in their protective niche.

BL-8040

CXCL12 in bone marrow stromal cells binds to CXCR4 on HSCs and retain them in the protective bone marrow niche

BL-8040 blocks the interaction between CXCL12 and CXCR4 by binding to CXCR4 with a long receptor occupancy (>48 hours)

As a result HSCs are mobilized into peripheral blood, collected by apheresis and stored

HSCs are injected back into the patient (in autologous transplantations) or to a recipient patient (in allogeneic transplantations) to repopulate the bone marrow

Stem-cell mobilization

In March 2015, BioLineRx reported successful top-line safety and efficacy results from a Phase 1 safety and efficacy trial for the use of BL-8040 as a novel hematopoietic stem-cell mobilization treatment for allogeneic bone marrow transplantation.

In March 2016, BioLineRx initiated a Phase 2 trial using BL-8040 for hematopoietic stem cell mobilization for allogeneic and haploidentical stem-cell transplantation in various hematological malignancies, conducted in collaboration with the Washington University School of Medicine, Division of Oncology and Hematology. Initial results of this study announced in March 2017 showed that a single injection of BL-8040 mobilized sufficient numbers of CD34+ cells for transplantation. Topline results of this study are now expected in mid-2018.

In Dec 2017, BioLineRx presented data supporting BL-8040 as robust mobilizer of hematopoietic stem cells associated with long-term engraftment at the 59th American Society of Hematology (ASH) Annual Meeting and Exhibition in Atlanta, GA.

In December 2017, BiolineRX enounce the initiation of controlled Phase 3 registrational trial of BL-8040 for the mobilization of hematopoietic stem cells for autologous transplantation in patients with multiple myeloma.