摘要:
Novel methods, processes and metal complexes attached to a hypoxia-localizing moiety comprising a metal, preferably radionuclide of rhenium or technetium; a hypoxia-localizing moiety; and, a complexing ligand, wherein said ligand and said radionuclide combined have cell membrane permeabilities greater than that of sucrose, are disclosed.
摘要:
Novel methods, processes and metal complexes attached to a hypoxia-localizing moiety comprisinga metal, preferably radionuclide of rhenium or technetium;a hypoxia-localizing moiety; and,a complexing ligand, wherein said ligand and said radionuclide combined have cell membrane permeabilities greater than that of sucrose, are disclosed.
摘要:
Boronic acid adducts of technetium-99m and radioactive rhenium dioxime complexes, each of which include biochemically active groups, are useful as diagnostic and therapeutic agents, respectively.
摘要:
A new and improved method for extending the half life of pharmaceutical compounds for use in diagnostic imaging or therapy uses a novel linker to attach a diagnostic or therapeutic moiety to a targeting peptide or another diagnostic or therapeutic moiety. The resulting compound may have the general formula M-N—O—P-Q, wherein M is the diagnostic or therapeutic moiety, N—O—P is the linker of the present invention, and Q is the targeting peptide. In another embodiment the compounds may have the formula M-N—O—P-M, wherein M is independently a diagnostic or therapeutic moiety and N—O—P is the linker of the invention. Methods for imaging or treating a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound are further provided. Methods for radiotherapy of a patient using the compounds are further provided, as are methods for preparing a radiotherapeutic agent from the compounds.
摘要:
Methods and compositions for diagnosing, staging disease, monitoring therapeutic effect of drugs and imaging a patient are provided, including radiopharmaceutical formulations. Compositions comprising Ga-AMBA complexed with a radioactive isotope are provided; as are methods of imaging Gastrin Releasing Peptide receptor (GRP-R) bearing tissue and methods of diagnosing or staging disease in patients suspected of having disease associated with aberrant GRP-R function. Further, methods of monitoring therapeutic effect of a drug targeted to a receptor that crosstalks with GRP-R are provided; as are methods of pre-dosing/co-dosing non-target tissues containing GRP-R. Particularly, methods of monitoring activity of receptors and receptor pathways in vivo/in vitro by using a ligand that binds to the GRP-R are provided; as are methods of measuring the activity of a receptor or group of receptors and their associated pathways that exhibit crosstalk with the GRP-R by using such a ligand which is also detectable by external means.
摘要:
A new and improved method for extending the half life of pharmaceutical compounds for use in diagnostic imaging or therapy uses a novel linker to attach a diagnostic or therapeutic moiety to a targeting peptide or another diagnostic or therapeutic moiety. The resulting compound may have the general formula M-N-O-P-Q, wherein M is the diagnostic or therapeutic moiety, N-O-P is the linker of the present invention, and Q is the targeting peptide. In another embodiment the compounds may have the formula M-N-O-P-M, wherein M is independently a diagnostic or therapeutic moiety and N-O-P is the linker of the invention. Methods for imaging or treating a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound are further provided. Methods for radiotherapy of a patient using the compounds are further provided, as are methods for preparing a radiotherapeutic agent from the compounds.
摘要:
Methods wherein the concentration of NMR-detectable xenobiotic compounds may be determined in living subjects by in vivo measurement of one or more magnetic resonance signals. In preferred embodiments, the present invention provides a method for evaluating, in vivo, the clearance rate of a xenobiotic compound from a living subject, thereby providing a noninvasive method for determining the status of the excretory organs of the subject, and a method for determining the proper dosing regimen of a pharmacologically active compound to be administered to the subject.
摘要:
Methods wherein the concentration of NMR-detectable xenobiotic compounds may be determined in living subjects by in vivo measurement of one or more magnetic resonance signals. In preferred embodiments, the present invention provides a method for evaluating, in vivo, the clearance rate of a xenobiotic compound from a living subject, thereby providing a noninvasive method for determining the status of the excretory organs of the subject, and a method for determining the proper dosing regimen of a pharmacologically active compound to be administered to the subject.
摘要:
Boronic acid adducts of technetium-99m dioxime complexes are useful for imaging the myocardium, hepatobiliary system, brain and blood pool in humans and other mammalian species.
摘要:
Methods and compositions for diagnosing, staging disease, monitoring therapeutic effect of drugs and imaging a patient are provided, including radiopharmaceutical formulations. Compositions comprising Ga-AMBA complexed with a radioactive isotope are provided; as are methods of imaging Gastrin Releasing Peptide receptor (GRP-R) bearing tissue and methods of diagnosing or staging disease in patients suspected of having disease associated with aberrant GRP-R function. Further, methods of monitoring therapeutic effect of a drug targeted to a receptor that crosstalks with GRP-R are provided; as are methods of pre-dosing/co-dosing non-target tissues containing GRP-R. Particularly, methods of monitoring activity of receptors and receptor pathways in vivo/in vitro by using a ligand that binds to the GRP-R are provided; as are methods of measuring the activity of a receptor or group of receptors and their associated pathways that exhibit crosstalk with the GRP-R by using such a ligand which is also detectable by external means.