{"entity":{"id":"cxcr4","kind":"target","name":"CXCR4","aka":[],"tldr":"A chemokine receptor that anchors blood cells in the marrow and helps cancer cells home to it; mutated in a third of Waldenström patients and targeted by plerixafor for stem-cell mobilisation.","summary":"CXCR4 binds CXCL12 (SDF-1) to retain haematopoietic stem cells in the marrow niche and guides metastasis of solid tumours to bone. Plerixafor (2008) blocks it to mobilise stem cells for autologous transplant; motixafortide (2023) does the same in myeloma. WHIM-like CXCR4 mutations in ~30-40% of Waldenström macroglobulinaemia slow BTK-inhibitor response; mavorixafor is in trials. CXCR4 is also imaged with Ga-68 pentixafor and treated with Lu-177 pentixather in marginal zone lymphoma and myeloma (theranostic, experimental). Balixafortide and ulocuplumab failed in solid tumours.","asOf":"2026-09-08","wikipedia":"https://en.wikipedia.org/wiki/CXCR4","links":[{"label":"CXCR4 in WM (Blood 2014)","url":"https://doi.org/10.1182/blood-2014-01-550905"}],"tags":["gap-fill"],"related":["ga-68","lu-177"],"indications":[],"sections":[],"technologies":["radioligand-therapy"],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":["theranostics"],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"symbol":"CXCR4","hgnc":"HGNC:2561","ensembl":"ENSG00000121966","uniprot":"P61073","entrez":"7852","biology":"G-protein-coupled receptor; CXCL12 binding activates Gαi, PI3K/AKT and MAPK, promoting chemotaxis, survival and retention in stromal niches; truncating C-terminal mutations impair receptor internalisation (WHIM syndrome).","whereFound":["Waldenström macroglobulinaemia (30-40% mutation)","Myeloma, lymphoma, AML (expression)","Breast, prostate and other solid tumours (metastatic homing)"],"targetClass":"other","prevalence":[]},"route":"/targets/cxcr4/","neighbours":{"isotope":[{"id":"ga-68","kind":"isotope","name":"Gallium-68","route":"/isotopes/ga-68/"},{"id":"lu-177","kind":"isotope","name":"Lutetium-177","route":"/isotopes/lu-177/"}],"technology":[{"id":"radioligand-therapy","kind":"technology","name":"Radioligand therapy (beta emitters)","route":"/technologies/radioligand-therapy/"}],"term":[{"id":"theranostics","kind":"term","name":"Theranostics","route":"/terms/theranostics/"}],"indication":[{"id":"primary-aldosteronism","kind":"indication","name":"Primary aldosteronism","route":"/indications/primary-aldosteronism/"}],"opportunity":[{"id":"opp-cxcr4-primary-aldosteronism","kind":"opportunity","name":"CXCR4 imaging instead of adrenal vein sampling","route":"/opportunities/opp-cxcr4-primary-aldosteronism/"}],"drug":[{"id":"ga-68-pentixafor","kind":"drug","name":"Gallium-68 pentixafor","route":"/drugs/ga-68-pentixafor/"}]}}