公开(公告)号：US20210015949A1

公开(公告)日：2021-01-21

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： A61K51/04

摘要： The invention relates to a new lutetium-177 therapeutic radiopharmaceutical as an inhibitor of prostate-specific membran 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 over

公开(公告)号：US20210187132A1

公开(公告)日：2021-06-24

申请号：US17135424

申请日：2020-12-28

申请人： INSTITUTO NACIONAL DE INVESTIGACIONES NUCLEARES

发明人： Guillermina FERRO FLORES ,  Blanca Elí OCAMPO GARCÍA ,  Clara Leticia SANTOS CUEVAS ,  Myrna Alejandra LUNA GUTIÉRREZ ,  Erika Patricia AZORÍN VEGA ,  Nallely Patricia JIMÉNEZ MANCILLA

IPC分类号： A61K51/04 ,  A61P35/04

摘要： The invention relates to a novel radiopharmaceutical that inhibits the prostate-specific membrane antigen (iPSMA), containing hydrazinonicotinamide (HYNIC) as a critical chemical group in increasing in the lipophilicity of the molecule for binding to the hydrophobic sites of the PSMA, combined with the conventional use of HYNIC as a chelating agent for radiometal 99mTc, in which the ethylenediaminetetraacetic acid (EDDA) is used to complete the coordination sphere of the radiometal. The novel radiopharmaceutical 99mTc-EDDA/HYNIC-iPSMA detects, with high affinity and sensitivity in vivo, the overexpressed PSMA protein in prostate cancer cells using SPECT molecular imaging techniques in nuclear medicine. The aim of the invention is to provide a novel specific radiopharmaceutical (radiopharmaceutical for molecular targets) for SPECT, with high sensitivity for the detection of tumours with overexpression of PSMA.