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lutetium lu-177 psma-r2
- Development stage
- Phase 2
- Lead developer
- Advanced Accelerator Applications
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Lutetium Lu-177 PSMA-R2 is a radioconjugate composed of the PSMA-R2 ligand, which specifically targets human prostate-specific membrane antigen (PSMA), conjugated to the beta-emitting radioisotope lutetium 177. This agent is designed for targeted radioligand therapy in prostate cancer, delivering ionizing radiation directly to PSMA-expressing tumor cells and thereby inducing cytotoxicity. The molecule is urea-based and acts as a small molecule inhibitor targeting carboxypeptidase-II (the enzymatic function of PSMA). Lutetium Lu‑177 PSMA‑R2 was developed as a patent-protected alternative to 177Lu‑PSMA‑617, with similar intended use in advanced prostate cancer. Its primary indication has been metastatic castration-resistant prostate cancer (mCRPC) and other forms of advanced or hormone-refractory prostate cancer[1][2][3][4][7].
- Other names
- lutetium lu-177 psma-r2
02
Targets
PSMA (Prostate-specific membrane antigen)
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