DOTA-[Thi8,Met(O2)11]-substance P

DOTA-[Thi8,Met(O2)11]-substance P is a modified peptide-based theranostic radiopharmaceutical designed for the targeted treatment and imaging of glioblastoma multiforme. It consists of a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) chelator conjugated to a stable analogue of the neuropeptide Substance P, featuring specific amino acid substitutions: thienylalanine at position 8 and oxidized methionine at position 11. These modifications enhance the peptide's stability and selectivity for the neurokinin-1 receptor (NK1R), which is highly overexpressed in glioblastoma cells. The compound can be radiolabeled with Gallium-68 for positron emission tomography (PET) imaging or with alpha-emitters like Bismuth-213 for targeted alpha-radionuclide therapy (TAT). Clinical studies, primarily conducted at the Medical University of Warsaw and in Switzerland, have focused on local injection for inoperable or recurrent high-grade gliomas, showing promising survival outcomes and high tolerability.

Other names

1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-[Thi8,Met(O2)11]-SP[213Bi]Bi-DOTA-[Thi8,Met(O2)11]SP[68Ga]Ga-DOTA-[Thi8,Met(O2)11]SPBismuth-213-DOTA-[Thi8,Met(O2)11]-substance PGallium-68-DOTA-[Thi8,Met(O2)11]-substance P