TE-1132 is an ARC, in which the antibody is derived from anti-CA19-9 monoclonal antibody, and the two site-specifically conjugated chelator bundles each carry 3 DOTA groups. TE-1132 is homogeneous, having 6 DOTA groups per molecule, and exhibits superior in vitro and in vivo stability.
The radiolabeling efficiency with 111In and 177Lu is over 90% in routine procedures. In mouse models with transplanted human pancreatic BxPC3 tumor cells, 111In-TE-1132 demonstrated excellent immuno-SPECT/CT imaging of tumor mass, with high tumor-to-blood ratio. 177Lu-TE-1132 could inhibit tumor growth with one single dose or multiple doses, suggesting that 177Lu-TE-1132 may be applied to treat human patients with pancreatic cancer.
The therapeutic effects of 177Lu-TE-1132 in patients will not be inhibited by the presence of CA19-9 antigen in the blood and the administration of 177Lu-TE-1132 can be accompanied by pre-dosing with large excess of unlabeled TE-1132
The molecular structure of radioisotope-labeled TE-1132.
The immuno-SPECT/CT imaging of an NU/NU mouse bearing a BxPC3 xenograft tumor by 111In-TE-1132.
Tumor suppression in NU/NU mice bearing BxPC3 tumor xenografts after three injections of 177Lu-TE-1132. (Dashed line: tumor volume reached 170 mm3 on day 22 post tumor cell implantation; green triangles: drug administered on day 22, 29 and 36).