Patent classifications
A61K51/0478
RADIOACTIVE ANTITUMOR AGENT
This radioactive antitumor agent comprises a radioactive dithiosemicarbazone-copper complex as an active ingredient, and is characterized by being used in such a way that the radioactive dithiosemicarbazone-copper complex is administered multiple times to an organism requiring tumor treatment, at a radioactive dose that avoids dose-limiting toxicity, as determined on the basis of hematological parameters. The multiple administration preferably consists of intermittent administration at time intervals allowing the hematological parameters to return to a normal range.
NANOPARTICLE IMMUNOCONJUGATES
Disclosed herein are nanoparticle immunoconjugates useful for therapeutics and/or diagnostics. The immunoconjugates have diameter (e.g., average diameter) no greater than 20 nanometers (e.g., as measured by dynamic light scattering (DLS) in aqueous solution, e.g., saline solution). In certain embodiments, the conjugates are silica-based nanoparticles with single chain antibody fragments attached thereto.
Evaluation of presence of and vulnerability to atrial fibrillation and other indications using matrix metalloproteinase-based imaging
The invention provides, in some embodiments, methods relating to assessing increased risk of developing atrial fibrillation (AF), and/or the likelihood of responding to particular AF therapies using imaging agents comprising an MMP inhibitor linked to an imaging moiety. The invention further provides methods for evaluating the presence of the risk of developing other cardiovascular conditions and assessing the effectiveness of treatment or other intervention for such conditions by determining MMP levels.
Compositions for therapeutics, targeted PET imaging and methods of their use
Described herein is a chelator for radiolabels (e.g., .sup.89Zr) for targeted PET imaging that is an alternative to DFO. In certain embodiments, the chelator for .sup.89Zr is the ligand, 3,4,3-(LI-1,2-HOPO) (HOPO), which exhibits equal or superior stability compared to DFO in chemical and biological assays across a period of several days in vivo. As shown in FIG. 1, the HOPO is an octadentate chelator that stabilizes chelation of radiolabels (e.g., .sup.89Zr). A bifunctional ligand comprising p-SCN-Bn-HOPO is shown in FIG. 4 and FIG. 5. Such a bifunctional ligand can eliminate (e.g., .sup.89Zr) loss from the chelate in vivo and reduce uptake in bone and non-target tissue. Therefore, the bifunctional HOPO ligand can facilitate safer and improved PET imaging with radiolabeled antibodies.
MULTINUCLEAR COMPLEXES AND THEIR PREPARATION
Multinuclear complexes and methods for preparing them are provided. The discrete multinuclear complexes include a one or more transition metals and a radioisotope having the same coordination geometry as the transition metal. A bridging ligand is coordinated to the transition metal and the radioisotope to link the transition metal and the radioisotope and pendent ligands are coordinated to each of the transition metal and the radioisotope to stabilise the complex. The multinuclear complexes may include a radioisotope or radioelement that can be detected by medical equipment and may find use in therapy and/or the diagnosis of disease in patients.
IMAGING AND RADIOTHERAPEUTICS AGENTS TARGETING FIBROBLAST-ACTIVATION PROTEIN-ALPHA (FAP-ALPHA)
Imaging and radiotherapeutics agents targeting fibroblast-activation protein- (FAP-) and their use in imaging and treating FAP- related diseases and disorders are disclosed.
COPPER-CONTAINING COMPLEX AND USES THEREOF
Complexes comprising a coordinated Cu(II) ion are described herein, which are capable of binding to an extracellular portion of Ctr1 such that the complex with the Cu(II) ion is transported through the Ctr1. The complexes may comprise a Cu(II) ion coordinated to a ligand and to a peptide, wherein the peptide is released upon contact of the complex with an extracellular portion of Ctr1, thereby forming a second complex comprising the ligand, the copper ion and the extracellular portion of Ctr1. Further described herein are uses and methods utilizing the complex, in imaging, in radiation therapy, and for determining a redox state of cells.
BIOAVAILABLE DITHIOCARBAMATE-METAL COMPLEX PARTICLES, METHOD OF PREPARATION AND USE THEREOF
A particulate form of dithiocarbamate-metal complex and at least one blood protein. The particulate form is obtained by a process having a sequential or simultaneous addition of individual components, resulting in their self-assembling. The aqueous dispersion of the particulate form is suitable for parenteral, oral and topical administration and for therapy and visualization of cancer.
Radiopharmaceutical compositions
The present invention relates to .sup.99mTc-maraciclatide radiopharmaceutical compositions, which are stabilised with a radioprotectant. Also described are kits for the preparation of the radiopharmaceutical compositions, as well methods of preparing such compositions from the kit. The invention also includes methods of imaging the mammalian body using the radiopharmaceutical compositions.
Compounds, compositions and associated methods using zirconium-89 in immuno-positron emission tomography
Disclosed are novel compounds, complexes, compositions and methods using Zirconium-89 combined with azamacrocyclic chelators in connection with PET. The compositions and methods should provide better diagnostic, prognostic and therapeutic oncology treatments relative to the presently available chelator compositions due to a variety of superior properties of the disclosed compositions. The present invention also relates to a superior method of making these compounds, complexes, compositions that allows one to make compounds/complexes (and thus, compositions) that were previously unattainable.