Vipivotide tetraxetan CAS# 1702967-37-0

Vipivotide tetraxetan (^177Lu-PSMA-617) is a radioligand targeting prostate-specific membrane antigen (PSMA) for selective delivery of β-emitting lutetium-177 to prostate cancer cells. In preclinical studies, PSMA-617 exhibited high binding affinity to PSMA (Kd ~1.2 nM) and strong internalization into PSMA-positive tumor cells. In mouse xenograft models, ^177Lu-PSMA-617 achieved high tumor uptake (>20% ID/g at 24 h) with rapid clearance from non-target tissues, resulting in favorable tumor-to-background ratios. Treatment significantly inhibited tumor growth and prolonged survival without marked toxicity to kidneys or salivary glands. These data supported its development as a targeted radioligand therapy for metastatic castration-resistant prostate cancer.