209 results about "Radioactive Label" patented technology

Methods for treating cancers and precancerous conditions by administering an effective amount of a radiolabeled agent that targets cell surface phosphatidylserine, alone or in combination with other therapies, are provided. The radiolabeled phosphatidylserine targeting agent delivers radiation to cells that externally present phosphatidylserine, such as tumor cells, depleting those cells and neighboring malignant cells to effect overall tumor reduction. Radiation delivered by the radiolabeled phosphatidylserine targeting agent itself increases the cell surface expression of phosphatidylserine, leading to a feed-forward mechanism that drives further accumulation of the phosphatidylserine targeting agent at target lesions to enhance its therapeutic effect.

The present disclosure provides a compound comprising a radiolabeling moiety, a targeting moiety, and a DNA intercalating agent and complexes thereof For example, the present disclosure provides a compound of Formula I or a pharmaceutically acceptable salt and / or solvate thereof. Methods of making and uses thereof, such as cancer theranostic applications, are also included. (I)

The present invention relates to MOFs for use in imaging and as radiolabeled tracers. More specifically, the present invention provides particles comprising MOFs, optionally at least one targeting moiety, and at least one short-lived radionuclide; compositions comprising the particles; the particles or compositions for use as imaging agents; the particles or compositions for use in methods for diagnosing proliferative diseases; the particles or compositions for use in methods for diagnosing chronic inflammatory diseases; and kits comprising particles comprising MOFs, optionally a targeting moiety, and a short-lived radionuclide cation.

The invention belongs to the technical field of radiopharmaceuticals, and particularly relates to a GPC3 targeted polypeptide probe and application thereof. According to the polypeptide probe targeting GPC3, non-natural functional groups are introduced to modify polypeptide ligands so as to enhance affinity, radiolabeling is carried out, and the polypeptide probe is used for PET molecular imaging diagnosis. The polypeptide probe shows good tumor targeting in vivo, the uptake of tumor tissues is remarkably different from that of normal liver tissues, the background of the normal liver tissues is clear, and a powerful tool and a theoretical basis are provided for noninvasive precise diagnosis of GPC3 positive liver cancer.

The 18F-labeling of unprotected peptides and sugars via thioarylation using a Au(III)-[˜F]fluoroaryl complex is reported. The chemoselective method generates 18F-labeled S-aryl bioconjugates in an aqueous environment in 15 min with high radiochemical yields and displays excellent functional group tolerance. This approach utilizes an air and moisture stable, robust organometallic Au(III) complex and highlights the versatility of designer organometallic reagents as efficient agents for rapid radiolabeling.

The invention relates to the technical field of sensing of magnetic nano photoelectric materials, in particular to a responsive microsphere based on a three-dimensional magnetic photonic crystal and a preparation method and application thereof, and the responsive microsphere is formed by arranging polyhydroxy compound modified magnetic nanoparticles in a spherical polymer into a non-close packing face-centered cubic or body-centered cubic structure. The responsive microsphere based on the three-dimensional magnetic photonic crystal is easy in color distinguishing, has no angle dependence, does not need to depend on a fluorescent dye or a radioactive label, can realize real-time and in-situ monitoring through own optical characteristics, breaks through the bottlenecks of sensitivity and resolution of a traditional sensor, realizes visual detection, simplifies the detection process, and is suitable for mass production. The cost is reduced. According to the responsive microsphere based on the three-dimensional magnetic photonic crystal, the substance diffusion path is shortened through the small size of the responsive microsphere, and the response speed is remarkably increased in combination with the high specific surface area.

The present application provides a synthetic process for production of lipoxin B4 and analogues thereof, which is modular and scalable, thus permitting synthesis of large quantities of LXB4 and analogues thereof, including radiolabeled analogues. Also provided are intermediate compounds that are useful in the synthetic process for production of lipoxin B4 and analogues thereof.

The present invention relates to novel, selective compounds with affinity to TDP-43, and to novel, selective radiolabelled TDP-43 ligands which are useful for imaging TDP-43 aggregates, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging TDP-43 aggregates in a tissue or a subject, in vitro or in vivo, and to precursors of said compounds.

The present invention relates to MSLN-specific binding constructs comprising a designed ankyrin repeat domain with binding specificity for MSLN and a chelator capable of bonding to a radionuclide, as well as to such MSLN-specific binding constructs comprising a half-life extending moiety with binding specificity for serum albumin. The invention further relates to methods of producing such radio-labelled MSLN-specific binding constructs, pharmaceutical compositions comprising such constructs, and the use of such constructs or pharmaceutical compositions in methods for treating, imaging or diagnosing diseases, such as cancer.

The present invention relates to radio- and fluorescence-labeled compounds, as well as their use as Diagnostics for Detecting Ecto-5′-Nucleotidase (CD73). The invention is further directed to a pharmaceutical composition comprising said compounds as well as to the compounds and the pharmaceutical composition for use in a method of diagnosis of a disease associated with increased or decreased CD73-expression as well as in the treatment of a disease associated with increased CD73-expression.

The present invention provides radiolabeled 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,7-α]indol-9-yl]pyridin-2(1H)-one derivatives of general formula (I) or salts thereof, as well as precursors of the radioligands of general formulae (II) and (III), processes for their preparation, and intermediates of the processes. The radiolabeled compounds enable visualization and quantification of melanin-concentrating hormone receptor 1 (MCHR1) in various target tissues, including monitoring MCHR1 in such target tissues. The compounds exhibit high binding affinity for MCHR1 and are able to cross the blood-brain barrier, thus facilitating diagnosis of various disease states in human clinical studies.

To provide a method of synthesizing 2-(3{1-carboxy-5-[(6-[18F]fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-pentanedioic acid ([18F]DCFPyL), which is a radiotracer for prostate-specific membrane antigen (PSMA) PET imaging for prostate cancer.SOLUTION: A synthesis method comprises the following steps: (i) radiofluorinating a DCFPyL precursor comprising ester moiety-protecting groups to form a radiofluorinated DCPFPyL precursor; (ii) deprotecting the ester moiety-protecting groups of the radiofluorinated DCPFPyL precursor of the step (i) with phosphoric acid to form [18F]DCFPyL in a reaction mixture; and (iii) purifying the [18F]DCFPyL from the reaction mixture of the step (ii) to provide [18F]DCFPyL.SELECTED DRAWING: Figure 5

The present invention provides a pharmaceutical composition comprising a radiolabeled complex comprising a radionuclide and a targeting moiety linked to a chelating moiety, and a stabilizer against radiolytic degradation of a radiolabeled complex comprising para-aminohippuric acid or a pharmaceutically acceptable salt or carboxylic derivative thereof. The pharmaceutical composition of the present invention is characterized by high stability of its radiolabeled complex against radiolytic degradation. The present invention also provides a method for preparing such a pharmaceutical composition, and use of para-aminohippuric acid or a pharmaceutically acceptable salt or carboxylic derivative thereof for the stabilization of the radiolabeled complex of such a pharmaceutical composition.

Radiolabeled liposomes can be used in the treatment of cancer. These local therapies can be used to treat cancers including, but not limited to, leptomeningeal metastases. In an embodiment, radiolabeled liposomes comprising (186Re) obisbemeda can be administered to a patient through an Ommaya reservoir. The therapies can include imaging the radiolabeled liposome concomitant or subsequent to administration.

This invention provides a combination for use in treating cancers that express prostate-specific membrane antigen (PSMA). [Solution] A combination comprising a PD-1 inhibitor, a CTLA-4 inhibitor, and a radiolabeled compound of formula Ia for use in treating PSMA-expressing cancer in the subject. JPEG2026049728000042.jpg45132 The aforementioned combination comprises one or more further anticancer agents, wherein the further anticancer agents are selected from octreotide, lanreotide, vapreotide, pasireotide, satreotide, everolimus, temozolomide, telotristat, sunitinib, sulfatinib, ribociclib, entinostat, and pazopanib.

Disclosed are radiopharmaceuticals with high stability and radiolabeling efficiency obtained by attaching a radionuclide to a pharmaceutical part with high stability that is obtained by attaching a chelating agent to a pharmaceutical specific to the receptors present in the tumor area, the radiopharmaceuticals enabling the imaging and / or the destruction of the cancer cells. Also disclosed is are a method for obtaining the radiopharmaceuticals and to a kit including the radiopharmaceuticals. The radiopharmaceuticals basically include at least one radionuclide, which enables the imaging and / or the destruction of the cancer cells, at least one pharmaceutical part, which includes at least one pharmaceutical agent targeting the receptor that causes the growth of the cancer cells, and at least one chelating agent enabling at least one radionuclide to be attached to the pharmaceutical agent.

The present invention relates to novel, selective compounds with affinity to TDP-43, and to novel, selective radiolabelled TDP-43 ligands which are useful for imaging TDP-43 aggregates, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging TDP-43 aggregates in a tissue or a subject, in vitro or in vivo, and to precursors of said compounds.

Radiolabelled binding agents that specifically bind to F-actin are provided. In particular, the radiolabelled binding agents of the invention exhibit preferential binding for F-actin over G-actin, which enables them to be used in medical and research settings. The invention provides radiolabelled binding agents, medical uses thereof, methods of generating radiolabelled binding agents and kits.

Disclosed are compositions and methods for the treatment of disease (e.g., cancer) using conjugates comprising a protein-binding moiety (e.g., an antibody or an antigen-binding fragment thereof) and one or more radiolabeled metalloporphyrin complexes. Also disclosed are conjugates that further include one or more chemotherapeutic agents.

Some embodiments relate to imageable radioisotope microspheres. In some embodiments, the imageable microspheres are radiolabeled with an imageable radioisotope. In some embodiments, the imageable radioisotope is directly chemically coupled to the surface of the microsphere matrix. In some embodiments, the imageable microspheres can be used as surrogate particles to predict the distribution of therapeutic microspheres containing radiotherapeutic isotopes.

There are provided fructose-based radiopharmaceuticals, pharmaceutical compositions comprising same, methods for preparing same, and methods of using same for biomedical imaging, particularly nuclear imaging using PET or PET / CT. (Compound 7)

The invention discloses a bisphosphonate radiomarker, and a precursor compound, a preparation method and application thereof, and belongs to the technical field of nuclear medicine. The structure of the precursor compound of the radioactive marker or the salt of the precursor compound is shown as a formula I; the structure of the radioactive marker or the salt thereof is shown as a formula II. The invention also discloses a preparation method of the precursor compound and the radioactive marker. The invention also discloses application of the precursor compound and the radioactive marker in preparation of a bone metastatic tumor targeted tumor imaging agent or / and a tumor therapeutic agent. The radioactive marker disclosed by the invention is relatively high in water solubility, relatively good in-vitro stability at room temperature and high in plasma protein binding rate, relatively high and relatively long-lasting skeleton uptake is shown in imaging and in-vivo distribution in mice, the imaging effect is superior to that of 99mTc-MDP, 68Ga-DOTA-ibandronic acid and 68Ga-labeled dithiophosphoric acid derivatives, and the radioactive marker has a wide application prospect. The compound is an excellent bone developer and a medicine for treating tumor bone metastasis.

The present invention provides a bivalent bispecific antibody targeting an EGFR and a c-MET and a radioactive label thereof. The research shows that the bivalent bispecific antibody provided by the present invention has good targeting affinity, and an antibody-radionuclide conjugate (taking 177Lu radioactive label as an example) of the bivalent bispecific antibody has an excellent SPECT imaging result, can be continuously accumulated in tumors over time, is more quickly removed in organs such as the liver and normal tissues, and can exhibit lower toxic and side effects. This also indirectly shows that the bivalent bispecific antibody provided by the present invention can clinically exhibit higher safety potential.

Disclosed are compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof. The variables of structural formula (I) are described herein. The compound of the invention can be attached to chelating groups for radionuclide binding and are therefore suitable for radioimaging and / or radiotherapy applications, for example the disclosed compounds can be radiolabeled with a positron emitter such as 18F, 68Ga or 64Cu, and used for positron emission tomography (PET). Alternatively, the compounds can be radiolabeled with an alpha particle emitter such as 223 Ac, a beta particle emitter such as 67Cu or 177Lu, or an Auger electron emitter (e.g. 111In, 67Ga, 99mTc, 195mPt, 125I, 123I and 161Tb) for use as a radiotherapeutic.

This radioactively labeled compound is represented by formula (1). In formula (1), M represents a radioactive metal ion. A represents a chelate moiety coordinated to the radioactive metal ion. B represents a first atomic group having a structure in which ethyleneimine is polymerized. C represents a second atomic group having a molecular weight of 5000 or less and capable of binding to a molecule expressed in a tumor cell. The second atomic group preferably includes a linear or cyclic peptide. The second atomic group also preferably includes 1-50 amino acid residues.

The present invention discloses a method for treating thyroid cancer using a radiolabeled cleavage-type Evans Blue degenerated fibroblast-activating protein inhibitor, said drug having excellent safety and tolerance in patients with thyroid cancer and having a very excellent therapeutic prospect in the treatment of thyroid cancer.