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225Ac-PNT2001 (actinium (225Ac) ancelvotide guraxetan, LY4181530) is a next-generation, prostate-specific membrane antigen (PSMA)-targeted radioligand therapy. It consists of the alpha-emitting radioisotope actinium-225 conjugated to PSMA-62, a small-molecule PSMA inhibitor, via a novel linker technology designed to enhance cellular internalization, improve biodistribution, and reduce off-target toxicities (such as xerostomia and renal toxicity) compared to first-generation PSMA radioligands. Originally developed by Scintomics and licensed to POINT Biopharma (subsequently acquired by Eli Lilly), the drug was evaluated in the Phase I/II ACCEL trial (NCT06229366) for metastatic castration-resistant prostate cancer (mCRPC) and oligometastatic hormone-sensitive prostate cancer (OmHSPC). However, in February 2026, Eli Lilly announced the termination of its development due to efficacy concerns.
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