Complex of bifunctional chelating agent and mannosyl human serum albumin

摘要

The present invention is about bifunctional chelating agents (BCA) conjugated mannosyl human serum albumin (MSA) and its radioisotope labeled compounds for imaging immune system such as macrophages, Kupffer cells, reticuloendothelial system (RES), and lymphatic system. The present invention comprises BCA-MSA conjugates, their radiolabeled compounds, and kits for radiolabeing. The present invention improved radiolabeling procedure, showed higher lymphatic system uptake, and enabled image by positron emission tomography (PET).

主权项

1. A sterile and apyrogenic kit of liquid, frozen or lyophilized state for preparation of a pharmaceutical composition labeled with a metallic radioisotope comprising:
(a). 10 ng˜100 mg of a conjugate of the following Formula 1;
(Man-L1)n-A-(L2-BCA)m  [Formula 1]wherein, Man is mannosyl group;L1 and L2 are independently linker(s) or direct conjugation(s);A is human serum albumin;BCA is 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA); andm and n are independently integers from 1 to 58; and (b). 0.01 mL˜10 mL of 1 μM˜10 M buffer (pH 1˜9); wherein the buffer solution is a mixture of acids selected from the group consisting of acetic acid, phosphoric acid, citric acid, fumaric acid, lactic acid, succinic acid, tartaric acid, carbonic acid, glucoheptonic acid, gluconic acid, glucuronic acid, glucaric acid and boric acid, and sodium or potassium salts thereof.