Patent classifications
A61K2123/00
RADIOLABELED LIGANDS FOR TARGETED PET/SPECT IMAGING AND METHODS OF THEIR USE
The present disclosure provides compounds, complexes, compositions, and methods for the detection of cancer. Specifically, the compounds, complexes, compositions of the present technology include pH (low) insertion peptides. Also disclosed herein are methods of using the complexes and compositions of the present technology in diagnostic imaging to detect cancer in a subject.
Methods for low temperature fluorine-18 radiolabeling of biomolecules
New chelators such as H.sub.3L1, H.sub.3L2, H.sub.3L3, H.sub.3L26 and derivatives were synthesized for the complexation of {Al.sup.18F}.sup.2+. These new chelators are able to complex {AI.sup.18F}.sup.2+ with good radiochemical yields using a labeling temperature of 37° C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and AI.sup.18F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and Al.sup.18F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and derivatives have been synthesized. We have explored the complexation of {AI.sup.18F}.sup.2+ with new chelators and obtained very favourable radiochemical yields (>85%) using a labeling temperature of 37° C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum at 37° C., where AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and Al.sup.18F-L26 showed high stability, since only very limited bone uptake—which would be an indication of release of fluorine-18 in the form of fluoride—was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestines due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and H.sub.3L26 demonstrated to be good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and several derivatives have been synthesized.
LIPID MICROBUBBLES AND PROCESS OF MAKING THEREOF
Disclosed is a suspension of gas-filled microbubbles in a physiologically acceptable liquid carrier comprising a lipid mixture of a first lipid having transition temperature of about 41° C. such as DPPC or DPPG, a second lipid having transition temperature of about 55° C. such as DSPC or DSPG, and a PEGylated DSPE such as DSPE-PEG2000, DSPE-PEG3000, or DSPE-PEG5000, and methods of preparation thereof.
8-hydroxyquinoline derivatives as diagnostic and therapeutic agents
The present application provides compounds useful in methods of treating neurological disorders such as Alzheimer's disease, and cancer such as prostate cancer. Also provided herein are radiolabeled compounds useful for imaging techniques, and techniques for diagnosis and monitoring of treatment of neurological disorders and cancer. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography or single-photon emission computed tomography. Methods for preparing radiolabeled compounds and methods for preparing unlabeled compounds are also provided.
RADIOPHARMACEUTICAL COMPOUND AND COMPOSITION FOR POSITRON EMISSION TOMOGRAPHY (PET) IMAGING OF INTERLEUKIN-2 RECEPTOR POSITIVE CELLS, PROCESS FOR THE PREPARATION THEREOF, RELATED KIT AND USES THEREOF
The present invention relates to a radiopharmaceutical compound or composition for Positron Emission Tomography (PET) imaging of interleukin-2 (IL2) receptor positive cells, in particular, .sup.68Ga-radiolabelled interleukin-2 such as a desalanyl-1, serine-125 human interleukin-2 (dsIL2) radiolabelled with a short-lived PET radioisotope (or radionuclide) gallium-68 (.sup.68Ga) by using tris-(hydroxypyridinone-maleimide) (THP-mal) as a chelator. The invention concerns also a kit comprising dsIL2 linked to THP-mal which can be added with .sup.68Ga in order to obtain the above mentioned radiopharmaceutical, at room temperature, suitable for PET imaging, a process for the preparation of the radiopharmaceutical and its use in medical and diagnostic field.
Dual mode radiotracer and—therapeutics
The present invention relates to a ligand-SIFA-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.
SOLVENT FREE GADOLINIUM CONTRAST AGENTS
Disclosed herein are complexes of gadolinium metal, ligand and meglumine that are substantially free of non-aqueous solvents. In particular, solvent-free complexes of 1) gadopentetate dimeglumine and 2) gadoterate meglumine are disclosed and methods of their preparation are disclosed. In addition, methods are disclosed for purifying reactants, monitoring and controlling pH, quantifying the free gadolinium content, quantifying the concentration of gadolinium-ligand complex in aqueous solution, and procedures for producing a drug product in one step. The one step process eliminates the need to dry the gadolinium-ligand complex, which is typically highly hygroscopic. The one step process includes purification steps that do not require the use of non-aqueous solvents.
Nanoparticle, contrast agent for magnetic resonance imaging containing same, and ligand compound
Provided is a novel nanoparticle, a contrast agent for magnetic resonance imaging containing the same, and a ligand compound used for production of the nanoparticle. The present invention relates to a nanoparticle including: a metal particle containing iron oxide; and a ligand which is bound to a metal atom on a surface of the metal particle and is represented by formula (3): ##STR00001## where m is an integer of 1 to 4, and a broken line represents a coordinate bond with a metal atom on the surface of the metal particle.
IMMUNOPET AND IMMUNOSPECT IMAGING TO IDENTIFY CYTOTOXIC T CELL ACTIVITY
Provided herein is a method for identifying cytotoxic T cell activity due to cancer immunotherapy in a subject. In some embodiments, the method comprises administering an effective amount of a tracer for positron emission tomography (PET) or single photon emission computed tomography (SPECT) to a subject receiving a cancer immunotherapy, wherein the tracer comprises an antibody or antigen-binding fragment thereof that specifically binds to a luminal domain of a lymphocytic granule-associated molecule (LGAM) labeled with a PET or SPECT detectable moiety, and detecting the signal of the tracer by PET or SPECT imaging to identify the cytotoxic T cell activity due to immune therapy for the cancer in the subject. In several embodiments, the antibody or antigen binding fragment specifically binds to the luminal domain of CD107a.
COMPOSITION FOR TARGETING MEDULLARY THYROID CANCER
Disclosed is a composition for targeting medullary thyroid cancer, the composition includes a diagnostic radionuclide-labeled ligand of the olfactory receptor OR51E2. The composition is internalized into parafollicular C cells by the olfactory receptor OR51E2 that is expressed on the parafollicular C cells of the thyroid gland and as such, can be advantageously used for diagnosing parafollicular C cell-derived medullary thyroid cancer and identifying whether or not parafollicular C cell-derived medullary thyroid cancer metastases are. In addition, a pharmaceutical composition includes an acetate-associated therapeutic radionuclide for treatment of medullary thyroid cancer can be used for treatment of medullary thyroid cancer because the composition is internalized into cancer cells through the binding of the acetate to the olfactory receptor OR51E2.