公开(公告)号：US20240216551A1

公开(公告)日：2024-07-04

申请号：US18288838

申请日：2021-10-14

申请人： Guillermina FERRO-FLORES ,  Blanca Elí OCAMPO-GARCÍA ,  INSTITUTO NACIONAL DE INVESTIGACIONES NUCLEARES

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

IPC分类号： A61K51/04

CPC分类号： A61K51/0455 ,  A61K51/0497 ,  A61K2123/00

摘要： This invention relates to new fibroblast activation protein (iFAP) inhibitory radiopharmaceuticals based on the molecule ((R)-1-((6-hydrazinylnicotinoyl)-D-alanyl)pyrrolidin-2-yl)boronic acid (HYNIC-iFAP), where the hydrazine nitrogens of HYNIC act as favorable chemical groups for the interaction of the HYNIC-iFAP molecule with phenylalanine (Phe-350 and Phe-351), glutamic acid (Glu-203 and Glu-204) and with serine (Ser-624) in the active center of fibroblast activation protein (FAP), coupled with the conventional use of HYNIC as a chelating agent for the radiometal 99mTc, where ethylenediamine diacetic acid (EDDA) is used to complete the coordination sphere of the radiometal. The new radiopharmaceutical from 99mTc-EDDA/HYNIC-iFAP (99mTc-HYNIC-iFAP) detects, with high affinity in vivo, FAP expressed in the microenvironment of malignant tumors of epithelial origin using nuclear medicine SPECT molecular imaging techniques. The object of this invention is to provide a new SPECT-specific radiopharmaceutical with high sensitivity for the detection of FAP protein expression in the tumor microenvironment, based on boronPro-type inhibitors (molecular target radiopharmaceutical).