¹⁷⁷Lu-Vipivotide tetratexan (¹⁷⁷Lu-PSMA-617) is a ¹⁷⁷Lu labeled peptide developed for the therapy of metastasized castrate resistant prostate cancer (mCRPC). This molecule is an IP protected molecule back-up of PSMA-11. Vipivotide tetraxetan is primarily developed as a therapeutic agent labeled with ¹⁷⁷Lu. Data published in December 2016 based on 145 patients with mCRPC who received treatment with ¹⁷⁷Lu-PSMA-617 for radioligand therapy and treated in 12 therapy centers show that 45% of patients had a positive response to treatment after receiving all treatment cycles, and 40% responded after one cycle.

Several new clinical trials involving ¹⁷⁷Lu-PSMA-617, among which a Phase I/II study in patients prior to prostatectomy (first line treatment), a comparative study with Enzalutamide, or studies in combination with Pembrolizumab or Olaparib. A first trial of treatment with ¹⁷⁷Lu-PSMA-617 in a single patient with glioblastoma proved to be efficient, opening a new era for the therapeutic use of this drug.

Target/Mechanism: PSMA

Carrier/Ligand: Vipivotide

Radiation Type: beta electrons (β^–)