A<unk>  is a substance which blocks the<unk>  receptor and prevent its activation. Blocking the receptor stops the receptor's ligand, CXCL12, from binding which prevents downstream effects.<unk> s are especially important for hindering cancer progression because one of the downstream effects initiated by<unk>  receptor activation is cell movement which helps the spread of cancer, known as metastasis. The<unk>  receptor has been targeted by antagonistic substances since being identified as a co-receptor in HIV and assisting the development of cancer. Macrocyclic ligands have been utilised as<unk> s. Plerixafor is an example of a<unk> , and has approvals (e.g. US FDA 2008) for clinical use (to mobilize hematopoietic stem cells). BL-8040 is a<unk>  that has undergone clinical trials (e.g. in various leukemias), with one planned for pancreatic cancer (in combination with pembrolizumab). Previously called BKT140, it is a synthetic cyclic 14-residue peptide with an aromatic ring. In a 2018 mouse tumor model study, BL-8040 treatment enhanced anti-tumor immune response potentially by increasing the CD8+ T-cells in the tumor microenvironment.
CXCR4 antagonist
C-Met inhibitor
RET inhibitor
TNF inhibitor
Tissue factor pathway inhibitor
CCR5 receptor antagonist
MEK inhibitor
CDK inhibitor