Theranostic Study of PSMA-Targeted Radioligands Modified with Enhancer SNAC

Three novel PSMA-targeted radioligands (PSA3-1, PDA3-1, PDB3-1) were synthesized and evaluated for prostate cancer theranostics. PDB3-1 demonstrated high binding affinity (IC50 = 19.1 nM) and, in PC-3 PIP tumor-bearing mice, showed high tumor uptake with rapid renal clearance. Tao Zhang published this preclinical data on figshare in May 2026.

Use Cases

• Compare pharmacokinetic profiles of novel radioligands based on SNAC conjugation strategy.
• Evaluate tumor inhibition efficacy of [177Lu]Lu-PDB3-1 relative to [177Lu]Lu-PSMA-617.
• Analyze the relationship between ligand hydrophilicity and renal clearance rates.
• Correlate in vitro docking scores with in vivo tumor uptake from PET imaging.

Strengths

• High radiochemical purity (>98%) reported for all radiolabeled compounds.
• PDB3-1 showed a specific binding affinity (IC50 = 19.1 nM) and docking score (-12.3 kcal/mol).
• Therapy studies compared a reduced dose (9.25 MBq) and a high-tolerated dose (111 MBq) for safety assessment.

Limitations

• Row count is unknown, which may limit suitability assessment.
• Column-level documentation is absent; field semantics must be inferred after download.
• Data is limited to a single preclinical mouse model (PC-3 PIP).

Provenance

Source

figshare

Collection Method

Preclinical study involving synthesis, radiolabeling, affinity assays, PET imaging, biodistribution, and therapy in mouse models.

Freshness

Last updated 2026-05-28 08:05:44; freshness should be verified.