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Ac-225-PSMA-62
- Development stage
- Phase 1
- Lead developer
- Eli Lilly
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
- Administration
- Intravenous
01
Overview
[Ac-225]-PSMA-62 is a next-generation prostate-specific membrane antigen (PSMA)-targeting radioligand therapy. It consists of the alpha-emitting radioisotope actinium-225 (Ac‑225), a chelating moiety, an optimized linker, and PSMA‑62—a small peptide inhibitor of PSMA. This design enables high-affinity binding to PSMA on prostate cancer cells and promotes efficient internalization into tumor cells. The improved linker technology enhances cellular uptake and tumor retention while facilitating rapid renal clearance to reduce off-target toxicity. [Ac‑225]‑PSMA‑62 is being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC) and oligometastatic hormone-sensitive prostate cancer (OmHSPC). It is currently under investigation in phase Ia/Ib/II clinical trials to assess safety, tolerability, optimal dosing schedules, and efficacy compared with standard-of-care therapies[1][2][3][5].
- Other names
- Ac-225 PSMA 62Ac225 PSMA 62Ac 225 PSMA 62
02
Targets
PSMA (Prostate-specific membrane antigen)DNA
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