DOTAGA-substance P

DOTAGA-substance P is a synthetic peptide-drug conjugate consisting of the neuropeptide substance P (SP) linked to the chelator DOTAGA (a derivative of DOTA), which enables stable radiolabeling with therapeutic radionuclides such as yttrium-90 (^90Y), bismuth-213 (^213Bi), or actinium-225 (^225Ac). The compound specifically targets the neurokinin-1 receptor (NK1R), which is highly and consistently overexpressed in glioblastoma multiforme (GBM) and other malignant gliomas. Upon local intratumoral or intracavitary injection, the radiolabeled conjugate binds to NK1R-expressing tumor cells and neovasculature, delivering cytotoxic radiation directly to malignant tissue while sparing surrounding healthy brain. This targeted alpha or beta therapy has shown feasibility, low toxicity, and promising efficacy in early-phase clinical studies for recurrent or inoperable GBM. The approach leverages both direct tumor cell kill via high-linear energy transfer radiation and potential ablation of infiltrative tumor margins[1][2][6][8].

Other names

[90Y]-DOTAGA-substance P[213Bi]-DOTAGA-substance P[225Ac]-DOTAGA-substance Pradiolabeled DOTAGA-SP