darolutamide + lutetium (177Lu) vipivotide tetraxetan

Darolutamide + 177Lu-PSMA-617 is an investigational combination regimen being studied as a neoadjuvant (pre-surgical) treatment for high-risk localized prostate cancer. It pairs darolutamide, an oral androgen receptor inhibitor, with 177Lu-PSMA-617 (lutetium vipivotide tetraxetan), a radioligand therapy consisting of the beta-emitting radioisotope lutetium-177 conjugated to a ligand that targets prostate-specific membrane antigen (PSMA). Darolutamide works by competitively inhibiting androgen binding to the androgen receptor (AR), inhibiting AR nuclear translocation, and preventing AR-mediated transcription. 177Lu-PSMA-617 delivers targeted radiation directly to PSMA-expressing tumor cells, leading to DNA damage and cell death. The rationale for this combination is that androgen receptor pathway inhibitors like darolutamide may upregulate PSMA expression on prostate cancer cells, potentially enhancing the uptake and therapeutic efficacy of the radioligand therapy. This combination is currently being evaluated in a prospective, multi-center clinical trial sponsored by The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School.

Other names

darolutamide + 177Lu-PSMA-617darolutamide + lutetium Lu 177 vipivotide tetraxetan