Patent classifications
A61K51/121
Stabilized compositions of radionuclides and uses thereof
Provided herein are radiopharmaceutical compositions and uses thereof. The radiopharmaceutical compositions can comprise one or more stabilizing agents, an aqueous vehicle, and a conjugate that comprises a targeting ligand and a radionuclide bound to a metal chelator. The targeting ligand can be a small molecule compound or a peptide such as a monocyclic peptide. The targeting ligand can be configured to bind with a tumor target. The stabilizing agent can comprise a radiolysis stabilizer, a free metal chelator, and/or a pH stabilizer. Further provided herein are methods of preparing the radiopharmaceutical compositions and methods of treating cancer by administering the described radiopharmaceutical compositions.
STABLE, CONCENTRATED RADIOPHARMACEUTICAL COMPOSITION
The present disclosure relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.
METHODS FOR RADIOLABELLING GRPR ANTAGONISTS AND THEIR KITS
The present invention relates to methods for radiolabelling GRPR antagonists such as NeoB, and their kits. In particular, the invention to a method for labeling a gastrin-releasing peptide receptor (GRPR) antagonist with a radioactive isotope, preferably .sup.68Ga, .sup.67Ga or .sup.64Cu, said method comprising the steps of: i. providing a first vial comprising said GRPR antagonist in dried form, ii. adding a solution of said radioactive isotope into said first vial, thereby obtaining a solution of said GRPR antagonist with said radioactive isotope, iii. mixing the solution obtained in ii. with at least a buffering agent and incubating it for a sufficient period of time for obtaining said GRPR antagonist labeled with said radioactive isotope, and, iv. optionally, adjusting the pH of the solution.
Trivalent Radioisotope Bio-Targeted Radiopharmaceutical, Methods Of Preparation And Use
A targeted radiopharmaceutical comprising a targeting species chemically-bonded to a PCTA-chelated Q.sup.+3 trivalent radioactive ion of Formula I
##STR00001##
is disclosed. Six of R.sup.1 through R.sup.7 are H and the seventh is a reacted functionality, Z, that forms the chemical bond with the targeting species, T. “g” is a number whose average value is 1 to about 12. X.sup.1, X.sup.2, and X.sup.3, are substituent groups that can coordinate to the Q.sup.+3 ion and/or help neutralize the ionic charge. Anion Y.sup.− is optionally present to balance the ionic charge. A pharmaceutical composition comprising a theranostic effective amount of a targeted radiopharmaceutical of Formula I in a pharmaceutically acceptable diluent is also contemplated, as are a method for treating and/or diagnosing a mammalian host having a disease, disorder or condition characterized by undesired angiogenesis, tumor growth and/or tumor metastasis.
Stabilized compositions of radionuclides and uses thereof
Provided herein are radiopharmaceutical compositions and uses thereof. The radiopharmaceutical compositions can comprise one or more stabilizing agents, an aqueous vehicle, and a conjugate that comprises a targeting ligand and a radionuclide bound to a metal chelator. The targeting ligand can be a small molecule compound or a peptide such as a monocyclic peptide. The targeting ligand can be configured to bind with a tumor target. The stabilizing agent can comprise a radiolysis stabilizer, a free metal chelator, and/or a pH stabilizer. Further provided herein are methods of preparing the radiopharmaceutical compositions and methods of treating cancer by administering the described radiopharmaceutical compositions.
STABILIZER FOR RADIOPHARMACEUTICALS AND RADIOPHARMACEUTICAL COMPOSITION COMPRISING THE SAME
The present invention relates to: a composition for stabilizing a radiopharmaceutical, the composition comprising a vitamin B compound as an active component; and a radiopharmaceutical composition comprising the same. Due to the inclusion of the vitamin B compound, it is possible to stabilize the radiochemical purity of the radioactive compound by inhibiting the radioactive degradation thereof at room temperature as well as at high temperature.
Apparatus of producing nuclide using fluid target
The disclosure provide an apparatus for producing a nuclide by using a liquid target which can perform the nuclear reaction process and can discharge the radioactive gas such as Radon within the vial. As described above, an apparatus for producing a nuclide by using a liquid target according to the present disclosure can minimize quantitative loss of a reactant by performing the nuclear reaction process using a target of a liquefied state and reusing a liquefied target on which the nuclear reaction process has not been performed, and can improve safety by enabling the radioactive gas generated to be disposed.
STABILIZED COMPOSITIONS OF RADIONUCLIDES AND USES THEREOF
Provided herein are radiopharmaceutical compositions and uses thereof. The radiopharmaceutical compositions can comprise one or more stabilizing agents, an aqueous vehicle, and a conjugate that comprises a targeting ligand and a radionuclide bound to a metal chelator. The targeting ligand can be a small molecule compound or a peptide such as a monocyclic peptide. The targeting ligand can be configured to bind with a tumor target. The stabilizing agent can comprise a radiolysis stabilizer, a free metal chelator, and/or a pH stabilizer. Further provided herein are methods of preparing the radiopharmaceutical compositions and methods of treating cancer by administering the described radiopharmaceutical compositions.
Astatine solution and method for producing same
The invention provides a method for producing a solution containing .sup.211At.sup.− (astatide ion) at a high radiochemical purity by using .sup.211At obtained by a nuclear reaction as a starting material, including a step of adding a reducing agent to a solution containing an impurity derived from .sup.211At. The invention also provides a solution containing .sup.211At.sup.− (astatide ion) at a radiochemical purity of not less than 30%.
Composition Containing a Somatostatin Analogue for Radiopharmaceutical Use
The present invention relates to a somatostatin analogue composition for radiopharmaceutical use, in particular for diagnostic or therapeutic use. More specifically the somatostatin analogue is a receptor-selective somatostatin peptide antagonist.