The present invention provides in certain embodiments a carcinoma-targeting conjugate comprising Formula I wherein T is a SST2R targeting ligand, L is a linker, and X is a chelator, for the therapeutic treatment of cancer, and methods of use thereof.

The present invention relates to formulations of radiolabeled compounds that are of use in radiotherapy and diagnostic imaging related to prostate specific membrane antigen (PSMA).

The disclosure provides multifunctional compounds for use in medical imaging and therapy, the compounds comprising two or more of (i) a chelating ligand moiety (CL); (ii) an optical probe moiety (OP); and (iii) a biological targeting moiety (BT). The disclosure further provides related compositions and methods.

The present invention relates to a compound of a pharmaceutically acceptable salt thereof of formula (I) wherein (A) is at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; (C) a dye moiety; x.sub.1 is a spacer or a chemical single bond covalently connecting (A) to the rest of the molecule; x.sub.2 is a spacer or a chemical single bond covalently connecting (C) to the rest of the molecule. The invention further relates to compositions comprising said compounds as well as a method for detecting neoplastic cells in a sample in vitro with the aid of the compounds or composition. ##STR00001##

The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A.sup.1 represents a chelate group; R.sup.1 represents a hydrogen atom or the like; R.sup.2 represents a hydrogen atom or the like; and Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4, and Z.sup.5 are the same or different and each represent a nitrogen atom or CR.sup.3 or the like wherein R.sup.3 represents a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group or the like; L.sup.1 represents a group represented by the formula (3) wherein R.sup.13, R.sup.14, R.sup.15, and R.sup.16 are the same or different and each represent a hydrogen atom or the like; L.sup.2 represents an optionally substituted C.sub.1-6 alkylene group; and L.sup.3 represents as optionally substituted C.sub.1-6 alkylene group.

##STR00001##

Low dose radiation, including conversion electron energy induces apoptosis in peripheral macrophages and CNS microglia. The transport of Sn-117m, a conversion electron emitter has been shown to be deliverable into the CNS across the blood-brain-barrier (BBB). The receptor for advanced glycation end products (RAGE) is a multi-ligand receptor member of the immunoglobulin super family which is able to bind A13 peptide and 13-sheet fibrils. It is expressed in endothelial cells, smooth muscle cells, microglia and neurons, and is implicated in the transport of A13 through the BBB, oxidative stress-mediated neurotoxicity, and adverse microglia inflammatory responses. The interaction between RAGE and its ligands is thought to result in pro-inflammatory gene activation. Enhanced levels of RAGE ligands in Alzheimer's disease are thought to contribute to the cause of this disorder. Embodiments of the invention use the RAGE multi-ligand site as an anchoring loci for a conversion electron emitting compound rather than as a receptor to intrinsically activate or block inflammation through the RAGE intracellular cascade through activation of the RAGE cytoplasmic tail (ctRAGE) and mammalian diaphanous 1 (DIAPH1).

The present invention relates to a ligand-SIF A-chelator conjugate, comprising, within in a single molecule three separate moieties: (a) one or more ligands which are capable of binding to a disease-relevant target molecule, (b) a silicon-fluoride acceptor (SIFA) moiety which comprises a covalent bond between a silicon atom and a fluorine atom, and (c) one or more chelating groups, optionally containing a chelated nonradioactive or radioactive cation.

The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of membrane type 1 metalloprotease (MT1-MMP). The invention also describes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups which have utility in imaging and targeted cancer therapy.

Provided is a novel compound capable of being usefully used to diagnose and treat prostate cancer by labeling a radioisotope on a bombesin derivatives capable of selectively targeting a target material over-expressed in tumor cells in order to develop an effective diagnose and treatment method of diseases associated with prostate cancer.

The radiopharmaceutical .sup.177Lu-PSMA I&T is provided, including in high purities with extended shelf life. Further provided are methods of synthesis of .sup.177Lu-PSMA I&T and pharmaceutical compositions and methods of treatment that comprise .sup.177Lu-PSMA I&T.