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.
PSMA-617 is primarily developed as a therapeutic agent labeled with 177Lu. The development of the equivalent 68Ga-PSMA-617 seems on hold as the most developed analogue 68Ga-PSMA-11 targets exactly the same receptors. Also, in terms of side-effects, the use of 177Lu instead of 131I proved to be much superior.
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.
The drug is presently completing phase III trial and could reach the market by end of 2021. At least five new clinical trials involving 177Lu-PSMA-617 were initiated between mid-2019 and June 2020, 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.
Leading Emitter: beta electrons (β–)