HPMA-RGDfK-DTPA

HPMA-RGDfK-DTPA is a **polymer-drug conjugate** composed of N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer, a cyclic RGD peptide (RGDfK: Arg-Gly-Asp-D-Phe-Lys), and DTPA or CHX-A''-DTPA as a chelating moiety. The RGDfK moiety targets the αvβ3 integrin, which is highly expressed on angiogenic endothelium and various tumor cells, enabling selective delivery to tumors. The conjugate can be radiolabeled via DTPA for imaging (e.g., with In-111 or other radionuclides) or for radiotherapy. This design aims to improve tumor accumulation and reduce off-target toxicity compared to untargeted therapies. HPMA copolymer-RGDfK-DTPA conjugates have shown **in vitro affinity for αvβ3 integrin**, rapid blood clearance in vivo, predominant renal accumulation, and variable tumor uptake depending on polymer structure and charge. Developed primarily in academic settings for preclinical evaluation in targeted oncology and radiopharmaceutical delivery[3][1][4].

Other names

HPMA copolymer-RGDfK-DTPAN-(2-hydroxypropyl) methacrylamide copolymer-RGDfK-DTPA