Inventors:
Martin W. Brechbiel - Annandale VA, US
Robert A. Star - Bethesda MD, US
Hisataka Kobayashi - Nishinomiya, JP
Assignee:
The United States of America as represented by the Secretary of the Department of Health and Human Services - Washington DC
International Classification:
C07F005/00
US Classification:
534 15, 424 111, 424 91, 424 936
Abstract:
Small dendrimer-based MRI contrast agents are disclosed to accumulate in renal tubules. The accumulation enables visualization of renal structure and function, permitting assessment of structural and functional damage to the kidneys. In a disclosed embodiment, six, small dendrimer-based MRI contrast agents were synthesized, and their pharmacokinetics, whole body retention, and renal MRI images were evaluated in mice. Surprisingly, despite having unequal renal clearance properties, all of the dendrimer agents clearly visualized the renal anatomy and proximal straight tubules of the mice better than Gd-[DTPA]-dimeglumine. Dendrimer conjugate contrast agents prepared from PAMAM-G2D, DAB-G3D, and DAB-G2D dendrimers were excreted rapidly and may be acceptable for use in clinical applications.