公开(公告)号：US12128114B2

公开(公告)日：2024-10-29

申请号：US16980252

申请日：2019-03-07

申请人： INSTITUTO NACIONAL DE INVESTIGACIONES NUCLEARES

发明人： Guillermina Ferro Flores ,  Blanca Elí Ocampo García ,  Myrna Alejandra Luna Gutiérrez ,  Clara Leticia Santos Cuevas ,  Erika Patricia Azorín Vega ,  Nallely Patricia Jiménez Mancilla ,  Tania Hernández Jiménez ,  Flor de María Ramírez De La Cruz

IPC分类号： A61K51/00 ,  A61K51/04 ,  A61M36/14

CPC分类号： A61K51/041

摘要： The invention relates to a new lutetium-177 therapeutic radiopharmaceutical as an inhibitor of prostate-specific membrane antigen (iPSMA), wherein 1,4,7,10-tetraazacyclododecane-N,N′,N″,N″″-tetraacetic acid (DOTA) bonded to the heterocyclic molecule hydrazinonicotinamide (HYNIC), generates a rigid chemical structure that minimises the number of conformers and intramolecular hydrogen bonds, thereby producing a favourable spatial orientation of the active site (Lys(Nal)-NH—CO—NH-Glu) in the molecule, for biological recognition by the PSMA protein. The new 177Lu-DOTA-HYNIC-iPSMA radiopharmaceutical accumulates, with high affinity in vivo, in tumours that overexpress the PSMA protein, acting as a radiotherapeutic agent. The purpose of the invention is to provide a new specific radiopharmaceutical (molecular target radiopharmaceutical) for the treatment of tumours with PSMA overexpression.