Artículo
Radiopharmacokinetics and uptake of 99m Tc-cRGD in av B3 integrins for imaging angiogenesis in induced malignant tumors in athymic mice
Autor
López Durán, Fred Alonso;#0000-0002-9316-3348
PEDRAZA LOPEZ, MARTHA; 25164
ARTEAGA PEREZ, CONSUELO; 7855
HERNANDEZ HERNANDEZ, DIANA EDITH; 47618
GARCIA BECERRA, ROCIO ANGELES; 36851
ORDAZ ROSADO, DAVID; 131365
López Durán, Fred Alonso
PEDRAZA LOPEZ, MARTHA
ARTEAGA PEREZ, CONSUELO
HERNANDEZ HERNANDEZ, DIANA EDITH
GARCIA BECERRA, ROCIO ANGELES
ORDAZ ROSADO, DAVID
Institución
Resumen
The multistep process of angiogenesis offers several targets for therapeutic interventions. One molecular target structure is the alfa five beta three (av b3 ) integrin which is expressed on vascular endothelial cells and over-expressed in cancer tumor angiogenesis. To image neoangiogenesis in athymic mice with induced pancreatic, breast and prostate malignant tumors a new radiopharmaceutical was developed. The 99mTc-EDDA/HYNIC-cyclic-Arg-Gly- Asp-D-Phe-Lys (99mTc-cRGD) targets integrin receptors av b3 and was prepared with an average radiochemical purity > 95 %. 99mTc-cRGD shows high in vivo stability, fast blood clearance and rapid renal excretion in mice. There are statistical differences between tumor/muscle ratios for the 3 tumors studied. The highest tumor/non-target ratio was found in breast cancer (7.2 after 24 h) and a representative dorsal SPECT image was obtained where the tumor showed up very clearly over the background tissue. The high resolution of the image implies that 99mTc-cRGD will be of great value in nuclear medicine as a potential radiopharmaceutical for av b3 integrins receptor uptake and for imaging neoangiogenesis in neoplastic tissue and to follow up cancer tumor progression.