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.

A compound represented by the following Formula 1 or a pharmaceutically acceptable salt thereof:

##STR00001##

where R.sub.1 is a chelating agent labeled with a metallic radioisotope. A thrombus imaging composition including the compound or the pharmaceutically acceptable salt thereof labeled with a metallic radioisotope as an active ingredient.

The present invention relates to ligands of Fibroblast Activation Protein (FAP) for the active delivery of various payloads (e.g. cytotoxic drugs, radionuclides, fluorophores, proteins and immunomodulators) at the site of disease. In particular, the present invention relates to the development of FAP ligands for targeting applications, in particular diagnostic methods and/or methods for therapy or surgery in relation to a disease or disorder, such as cancer, inflammation or another disease characterized by overexpression of FAP.

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 is directed to a composition comprising at least one fibronectin binding polypeptide (FnBP) linked to at least one diagnostic or therapeutic agent, a nucleic acid encoding a fusion polypeptide comprising at least one fibronectin binding polypeptide (FnBP) linked to at least one diagnostic or therapeutic polypeptide agent as well as a corresponding recombinant vector and host cell comprising such a nucleic acid and preferably expressing said fusion polypeptide. The invention also relates to a kit of parts comprising at least one fibronectin binding polypeptide (FnBP), at least one diagnostic or therapeutic agent, and optionally one or more chemical agents for linking the fibronectin binding polypeptide (FnBP) to the diagnostic or therapeutic agent. In addition, the present invention intends said composition, nucleic acid, vector, host cell and kit for use in the therapeutic or prophylactic treatment of a disease, preferably a disease associated with abnormal fibronectin accumulation such as cancer, fibrosis or immune diseases.

The present invention provides novel PSMA targeting urea-based ligands that binds to prostate-specific membrane antigen (PSMA) which is expressed 8-to-12-fold higher in prostate cancer cells when compared to healthy tissue. The PSMA targeting urea-based ligands comprises a chelating agent that may comprise a metal and a halogen radioisotope of fluorine, iodine, bromine or astatine. The invention further relates to a method for providing the PSMA targeting urea-based ligands of the invention, to precursors of the PSMA targeting urea-based ligands and to the PSMA targeting urea-based ligands use in radiotherapy, imaging and theranostic.

The present technology is directed to compounds, intermediates thereof, compositions thereof, medicaments thereof, and methods related to the imaging of mammalian tissue overexpressing PSMA. The compounds are of Formula I

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein one of R.sup.1, R.sup.2, and R.sup.3 is

##STR00002##

and of Formula IV

##STR00003##

or a pharmaceutically acceptable salt thereof.

A method for making a radiopharmaceutical cold kit without lyophilization, comprising (1) providing a labeling ligand, a reducing agent, and a bulking agent, and at least one of an antioxidant and an exchange ligand, wherein each of said labeling ligand, reducing agent, bulking agent, antioxidant and exchange ligand is provided in a dry form; and (2) combining and mixing the labeling ligand, the reducing agent, the bulking agent, and at least one of the antioxidant and the exchange ligand to produce a dry powder mixture, wherein the wherein the dry powder mixture is produced without the use of a lyophilization step. The radiopharmaceutical cold kit comprising the dry powder mixture may be stored, or combined with a radionuclide such as Technetium-99m (.sup.99mTc).

Conjugates derived from non-steroidal anti-inflammatory drugs (NSAIDs) and methods of use thereof are disclosed, useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The NSAID-based conjugates contain an imaging moiety. The conjugates concentrate at sites of increased cyclooxygenase expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections.

The invention relates to chemical compounds and complexes that can be used in therapeutic and diagnostic applications.