CHELANTS WITH ENHANCED BLOOD RETENTION

摘要

The present invention is a pharmaceutical composition that exhibits enhanced IP blood retention, the composition comprising: a biotargeting molecule; and a chelating agent conjugated to the biotargeting molecule; wherein the composition exhibits a half-life in the bloodstream of from 15 minutes to 24 hours. The present invention is also directed to the use of functionalized chelants to modify the pharmacokinetics of radiopharmaceuticals. Compared with non-functionalized chelants, chelants functionalized with bulky and/or lipophilic groups can slow down the renal clearance and enhance the blood retention of metals complexed therewith. This enhanced blood retention leads to increased uptake of metal in target tissue.