A61K51/088

COMPOSITIONS AND METHODS OF TARGETING AND IMAGING AGED MICROGLIA WITH Aß PEPTIDE AMINO ACID RESIDUES FOR V-DOMAIN BINDING OF RAGE
20230181770 · 2023-06-15 ·

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).

METHODS OF DETECTING AND TREATING LUNG DAMAGE IN RESPIRATORY-RELATED VIRAL INFECTIONS

Provided herein are methods for detecting, monitoring, diagnosing and treating respiratory-related viral infections, including SARS-CoV-2 infected individuals and subjects that are infected with or suspected of having been infected with the virus, or that have come in contact with COVID-19 suffering individuals.

PSMA binding ligand-linker conjugates and methods for using

Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

Peptide therapies for reduction of macular thickening

Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH.sub.2—SO.sub.3H)COOH or Arg-Gly-NH—CH(CH.sub.2—SO.sub.3H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, stereoisomers, multimers, cyclic forms, linear forms, drug-conjugates, pro-drugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibiting integrins including but not necessarily limited to α.sub.5β.sub.1-Integrin, α.sub.vβ.sub.3-Integrin and α.sub.vβ.sub.5-Integrin, inhibiting cellular adhesion to RGD binding sites, preventing or treating viral or other microbial infections, inhibiting angiogenesis in tumors, retinal tissue or other tissues or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.

CYCLIC PEPTIDES AND THEIR CONJUGATES FOR ADDRESSING ALPHA-V-BETA-6 INTEGRIN IN VIVO

The invention provides conjugates of cyclic peptides as ligands for cellular surface receptors, in particular, as ligands for αvβ6-integrin. The conjugates further contain effector moieties and are suitable for use as therapeutic agent, diagnostic agent, agent for imaging, targeting moiety and as biomolecular research tool. The invention specifically relates to the use of conjugates with signalling moieties or radionuclides for in-vivo addressing of αvβ6-integrin.

GRP-R agonistic 177-lutetium-labeled bombesin derivatives for diagnosis and treatment of prostate cancer

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.

Spatial mapping of kidney functions
11666671 · 2023-06-06 · ·

A molecular imaging agent including a detectable moiety, a chelation moiety, and a carrier moiety is provided. In one embodiment, the detectable moiety is coupled to the chelation moiety and the chelation moiety is linked to the carrier moiety. In another embodiment, the detectable moiety is .sup.99mTc; the chelation moiety includes HYNIC; and the carrier moiety includes from N-terminus to C-terminus: a His6 purification tag, a human VEGFA polybasic tag sequence, and a human Fc stabilization segment.

VISUALIZATION OF HER2 EXPRESSION IN HUMAN PATIENTS

There is provided an imaging agent for use in a method of visualization of HER2 expression in a human patient, said method comprising administering the imaging agent to the patient in a dose of 400-700 μg and subsequently a scanning of the patient to visualize HER2 expression, wherein the imaging agent is a conjugate comprising a radionuclide and a HER2-binding protein (HBP) of a certain amino acid sequence. Further there is provided a unit dose comprising the imaging agent in an amount of 400-700 μg.

[161Tb]-BASED RADIOPEPTIDES

A radiopeptide is provided which comprises (a) a radionuclide, wherein the radionuclide is terbium-161, (b) a chelator coordinating terbium-161, and (c) a peptide or peptide analogue, which is a somatostatin receptor (SSTR) antagonist. The radiopeptide is suitable for use in the treatment of tumor diseases.

PET IMAGING WITH PD-L1 BINDING POLYPEPTIDES

Provided herein are novel .sup.10Fn3 domains which specifically bind to PD-L1, as well as imaging agents based on the same for diagnostics.