Current Status of PSMA-Targeted Agents Based on Small Molecules for Prostate Cancer in Preclinical Studies
link.springer.com/article/10…
PSMA is a validated target for
#ProstateCancer imaging and radioligand therapy (RLT), with urea-based small-molecule ligands showing favorable pharmacokinetics, tumor penetration, and radiolabeling properties.
Recent preclinical efforts aim to improve efficacy through ligand optimization, radionuclide selection, and pharmacokinetic enhancements.
Strategies such as albumin-binding moieties and linker modifications seek to increase tumor uptake while reducing off-target toxicity. Therapeutic radionuclides, including lutetium-177, actinium-225, astatine-211, and iodine-125, offer complementary mechanisms of tumor cell destruction.
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