BL-3040

BL-3040 (also known as BKT3040) is an orally bioavailable small molecule CXCR4 antagonist originally developed by Biokine Therapeutics and later licensed by BioLineRx. It was primarily investigated for the treatment of inflammatory bowel disease (IBD), including Crohn's disease and ulcerative colitis. The drug works by blocking the C-X-C chemokine receptor type 4 (CXCR4), which prevents the binding of its ligand, stromal cell-derived factor-1 (SDF-1/CXCL12). This interaction is known to play a critical role in the migration of inflammatory cells to the gut mucosa. By inhibiting this pathway, BL-3040 aimed to reduce the production of pro-inflammatory cytokines such as TNF-α and IL-6 while potentially inducing anti-inflammatory cytokines like IL-10. BioLineRx discontinued the development of BL-3040 in late 2011 following a strategic review of its pipeline and the completion of Phase 1 clinical trials.