Palmitic Acid-Conjugated Radiopharmaceutical for Integrin α_vβ₃-Targeted Radionuclide Therapy.

ABSTRACT: Peptide receptor radionuclide therapy (PRRT) is an emerging approach for patients with unresectable or metastatic tumors. Our previously optimized RGD peptide (3PRGD₂) has excellent targeting specificity for a variety of integrin α_vβ₃/α_vβ₅-positive tumors and has been labeled with the therapeutic radionuclide [¹⁷⁷Lu]LuCl₃ for targeted radiotherapy of tumors. However, the rapid clearance of [¹⁷⁷Lu]Lu-DOTA-3PRGD₂ (¹⁷⁷Lu-3PRGD₂) in vivo requires two doses of 111 MBq/3 mCi to achieve effective tumor suppression, limiting its further clinical application. Albumin binders have been attached to drugs to facilitate binding to albumin in vivo to prolong the drug half-life in plas

SUBMITTER: Yang G 

PROVIDER: S-EPMC9321335 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature