177Lu-Pentixather is the therapeutic analogue of 68Ga-Pentixafor, to be used in metastasized patients showing tumors expressing CXCR4. 177Lu-Pentixather was tested in priority in patients with multiple myeloma. However, 177Lu-Pentixather could find applications in all cancer types that have already shown high expression of CXCR4 including lung cancer, squamous cell carcinoma, pancreas cancer, rectal and colon cancer.

The first clinical data in multiple myeloma patients were published in 2016. Patients are selected on the basis of Imaging with 68Ga-Pentixafor and were treated either with 177Lu-Pentixather or 90Y-Pentixather. Additional data were published in extramedullary relapsed multiple myeloma patients treated with 177Lu-Pentixather. The drug induced high response rate. Further studies have been initiated.

Target/Mechanism: CXCR4

Leading Emitter: beta electrons (β)