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-Anditixafortide. Additional data were published in extramedullary relapsed multiple myeloma patients treated with ¹⁷⁷Lu-Pentixather. The drug induced high response rate. Recent results have shown superiority of 90Y-Anditixafortide over 177Lu-Pentixather giving a lower priority to this 90Y-labeled drug.

Target/Mechanism: CXCR4

Carrier/Ligand: Pentixather

Radiation Type: beta electrons (β^–)