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PIPELINE > TRIAL OVERVIEW

Trial Information
Molecule Overview
Prostate-Specific Membrane Antigen (PSMA)
[Ac-225]-PSMA-62
PSMA-62

Vito A, et al1; Jang A, et al2; Pomykala KL, et al3

Target

Prostate-specific membrane antigen (PSMA) is a type II transmembrane protein that is weakly expressed in normal prostate tissue but strongly upregulated in prostate cancer.4 PSMA expression increases with higher Gleason scores and further increases in metastatic disease and when resistance to androgen therapy emerges.5,6 Upon binding to its ligand, PSMA internalizes, thereby facilitating endocytosis and intracellular accumulation of PSMA-targeted compounds.7

Molecule
[Ac-225]-PSMA-62 is a next-generation PSMA-targeting radioligand comprised of the alpha-emitting radioisotope actinium-225, a chelating moiety, linker, and PSMA-62, a small peptide PSMA inhibitor. In nonclinical models, PSMA-62 showed high PSMA binding affinity, increased cellular internalization, and improved biodistribution, including high tumor retention and rapid renal clearance.1
Clinical Development

[Ac-225]-PSMA-62 is being studied in a phase I/II clinical trial for patients with metastatic castration-resistant prostate cancer (mCRPC) and patients with oligometastatic hormone-sensitive prostate cancer (OmHSPC).

References

  1. Vito A, et al. Eur J Nucl Med Mol Imaging. 2022;49(suppl 1):S440:EP-039.
  2. Jang A, et al. Ther Adv Med Oncol. 2023;15:1-12.
  3. Pomykala KL, et al. Ann Oncol. 2023;34(6):507-519.
  4. Silver DA, et al. Clin Cancer Res. 1997;3(1):81-85. 
  5. Kasperzyk JL, et al. Cancer Epidemiol Biomarkers Prev. 2013;22(12):2354-2363.  
  6. Meller B, et al. EJNMMI Res. 2015;5(1):66.
  7. Rajasekaran SA, et al. Mol Biol Cell. 2003;14(12):4835–4845.
For information on trial enrollment, locations, and more, call 1-800-545-5979.
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