Drug intelligence / Profile preview

actinium (225Ac) ancelvotide guraxetan

Development stage
Discontinued
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Peptides
Administration
Intravenous
01

Overview

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.

Other names
actinium (225Ac) ancelvotidum guraxetanumactinium Ac 225 ancelvotide guraxetanancelvotide guraxetan
02

Targets

PSMA (Prostate-specific membrane antigen)

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