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PIPELINE > TRIAL OVERVIEW

Molecule Overview
Prostate-Specific Membrane Antigen (PSMA)
[Ac-225]-PSMA-62
PNT2001

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

Target

Prostate-specific membrane antigen (PSMA) is a type II transmembrane protein with very limited expression in normal tissues and substantial upregulation in prostate cancer.4 Expression tends to increase with increasing pathological Gleason grades and is further upregulated with the emergence of androgen resistance.5,6 Upon binding to a 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 region, and PSMA-62, a small molecule 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 1/2 clinical trial for patients with metastatic castration-resistant prostate cancer and patients with biochemically recurrent prostate cancer.

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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