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177Lu-rhPSMA-10.2
- Development stage
- Discontinued
- Lead developer
- Blue Earth Therapeutics
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
177Lu-rhPSMA-10.2 is a radiohybrid prostate-specific membrane antigen (PSMA)-targeted radiopharmaceutical developed for the radioligand therapy of prostate cancer. It is a DOTA-based ligand complexed with the beta-emitting radioisotope lutetium-177. As a radiohybrid (rh) molecule, it was designed with the aim of optimizing human serum albumin binding and charge reduction to accelerate kidney excretion while maintaining high tumor uptake. Preclinical evaluations compared 177Lu-rhPSMA-10.2 with its stereoisomer, 177Lu-rhPSMA-10.1. Although both isomers demonstrated high tumor uptake, 177Lu-rhPSMA-10.2 exhibited slower kidney clearance kinetics and less favorable tumor-to-organ ratios than 177Lu-rhPSMA-10.1. Consequently, 177Lu-rhPSMA-10.2 has been deprioritized in favor of its stereoisomer for clinical development.
- Other names
- 177Lu-radiolabeled rhPSMA-10.2
02
Targets
PSMA (Prostate-specific membrane antigen)
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