Therapeutics: CXC chemokine receptor 4 (CXCR4; NPY3R); lymphocyte-specific protein kinase (LCK) Provisional patent application filed; available for licensing

In vitro studies suggest an antibody-drug conjugate (ADC) targeting CXCR4 and LCK could help treat autoimmune diseases. In a human cell line, a humanized antibody against CXCR4 bound T cells with a Kd of 2.1 nM and was internalized within 30 minutes, but had no activity against non-hematopoietic cells. In a human T cell line, an ADC of the anti-CXCR4 antibody conjugated to the LCK inhibitor dasatinib by an intracellularly cleavable linker decreased cell activation and cytokine secretion compared with the non-cleavable ADC or unconjugated antibody. Next steps include testing the ADC's efficacy in animal models of autoimmune diseases...