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[67Cu]Cu-LLP2A is an experimental radiopharmaceutical consisting of the high-affinity peptidomimetic ligand LLP2A, which targets the integrin α4β1 (very late antigen-4, VLA-4), radiolabeled with the beta- and gamma-emitting therapeutic radionuclide copper‑67 for targeted radionuclide therapy of VLA‑4–expressing malignancies. LLP2A binds VLA‑4 with picomolar affinity and has been shown to selectively accumulate in VLA‑4–positive tumors and lymphoid tissues, enabling delivery of cytotoxic radiation to a broad range of pediatric and adult solid tumors and hematologic cancers that overexpress this integrin.[3][6] Preclinical studies demonstrate favorable biodistribution, dose-dependent tumor control, and an acceptable toxicity profile in mice, with primary off‑tumor uptake in lymphoid organs and limited long‑term organ toxicity at therapeutically relevant administered activities.[3]
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