52 results about "Radioligand" patented technology

A conjugate of the formula (I) wherein F is a ligand (radical thereof) that binds fibroblast activation protein alpha (FAPα); L is a functionalized linker that binds with F, A, and X; A is a pharmacokinetic extender that binds or associates or binds with a protein in the blood of an animal; and X is chelator; a method of imaging cancer-associated fibroblasts (CAFs) and activated myofibroblasts in a subject; and a method of treating a disease characterized by upregulation of FAPα, such as cancer, in a subject.

The present disclosure relates to a method of treating prostate specific membrane antigen (PSMA) positive progressive metastatic castration resistant prostate cancer (mCRPC) by administering a therapeutically effective amount of a PSMA binding radioligand therapy (RLT) agent, preferably [177Lu] Lu-PSMA-617 (lutetium (177Lu) vevovortitide Tailaracetam), to a taxane primarily treated patient whose disease progresses after receiving a second generation ARPI.

The present disclosure relates to stable compositions comprising a radiolabeled compound, and related pharmaceutical compositions and methods of manufacture. Such compositions are useful in both the diagnostic imaging of and the treatment of diseases (e.g., cancer).

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)

A precursor compound and a radioligand for cancer diagnosis and treatment comprises a high-affinity ligand PL for a cancer- associated protein conjugated to a covalent warhead CW for strong or covalent binding to an amino acid sidechain of the cancer-associated protein and a chelator Ch for complexation of a radioisotope or a leaving group LR for substitution with a radioisotope, wherein the covalent warhead CW is configured for quasi-covalent ionic binding using a sulfonic acid group or for covalent binding using a sulfur fluoride exchange (SuFEx) group, a benzotriazole or N-methyl-N- arylmethanesulfonamide leaving group or a malolactone group for strain-release alkylation.

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.

Provided herein are compounds for delivery of one or more radiotherapeutic or radiodiagnostic agents. In some embodiments, the compounds have a radioactive agent binding moiety (RBM) connected to a GRPR binding moiety (GBM) through a linker (RBM-L-GBM), wherein the at least one of L and GBM is optionally substituted with an albumin binding moiety (ABM). In some embodiments, the one or more therapeutic or diagnostic agents are delivered to cancer cells.

# imgabs0. The present invention discloses compounds of formula (I) and complexes thereof with radionuclides, which can recognize both the somatostatin type 2 receptor (SSTR2) and the cholecystoxin 2 receptor (CCK2R) and can be used in the diagnosis and treatment of diseases in which either or both receptors are overexpressed.

Described herein are cyclic peptides targeting human epidermal growth factor receptor 2 (HER2), and their incorporation into compounds for radioligand imaging and therapies, as well as methods and / or uses of such compounds for the imaging, treatment and / or prevention of HER2-implicated diseases and disorders (e.g., cancer).

The present invention relates to the fields of high molecular heterocyclic compounds and nuclear medicine imaging technology, and particularly relates to a PET probe obtained by coupling an SSTR agonist and an inhibitor, and a preparation method and application thereof. The PET molecular probe comprises a targeting molecule obtained by coupling an SSTR agonist and an inhibitor, a radioisotope, and a linker, and the linker connects the targeting molecule and the radioisotope. The heterodimer obtained by coupling the SSTR agonist and the inhibitor can improve the PET detection sensitivity by increasing the binding affinity with the target through a synergistic effect; has higher specificity and can specifically and efficiently target SSTR for in vivo imaging in a variety of tumor microenvironments; not only makes the distribution of the radioligand more uniform, but also can effectively improve the clinical effect of radionuclide therapy after labeling with therapeutic radionuclides such as <supgt;177< / supgt;Lu. Compared with the prior art, the molecular probe has stronger affinity, higher stability and higher target-to-background ratio; meanwhile, the preparation method of the PET molecular probe is simple and stable, and has good market promotion and application prospects.

The present disclosure relates to a method of treating highly differentiated G2 or G3 neuroendocrine neoplasms (NET) in a patient in need thereof, the method comprising administering to the patient a treatment of a radioligand therapy (RLT) agent comprising a therapeutically effective dose of a targeted somatostatin receptor (SSTR), in particular [177Lu] Lu-DOTA0-Tyr3-octoic acid, as a first-tier therapy.

Disclosed herein are EphA2 targeting compounds or pharmaceutically acceptable salt or radioactive metal complex thereof, and methods of their use in the treatment of EphA2 positive cancer. In certain embodiments, the compound is a Targefrin monomer or dimer compound complexed with a radiometal, such as lutetium-177. In certain embodiments, the compound is an irreversible covalent binder of EphA2. In certain embodiments, the compound is a cyclic compound.

Provided herein are compounds for the delivery of one or more radiotherapy or radiodiagnostic agents. In some embodiments, the compounds have a radioagent binding moiety (RBM) linked to a GRPR binding moiety (GBM) via a linker (RBM-L-GBM) wherein at least one of L and GBM is optionally substituted by an albumin binding moiety (ABM). In some embodiments, the one or more therapeutic or diagnostic agents are delivered to cancer cells.

The present application discloses specific compounds of Formula (I) and their use in therapy, in particular, their use as Polymerase Theta (Polθ) inhibitors for the treatment of cancer. The application further discloses the use of a combination comprising a compound of Formula (I) and a radiotherapy or a radioligand in therapy, in particular, the use of specific compounds of Formula (I) as a Polymerase Theta (Polθ) inhibitor in combination with a radiotherapy or a radioligand for the treatment of cancer.

The present application discloses specific compounds of formula (I) and their use in therapy, particularly their use as polymerase theta (Pol theta) inhibitors for the treatment of cancer. The present application further discloses the use of a combination comprising a compound of formula (I) and radiation therapy or a radioligand in therapy, in particular the use of a specific compound of formula (I) as a polymerase theta (Pol theta) inhibitor in combination with radiation therapy or a radioligand for the treatment of cancer. # imgabs0 #

The present invention provides combinations of inhibitors of Ectonucleotide Pyrophosphatase / Phosphodiesterase (ENPP1) with a radiation therapy or a radioligand for the purposes of treating cancer. The invention includes both methods of treatment of cancer with the provided combinations and pharmaceutical compositions comprising such combinations. A preferred ENPP1 inhibitor is SR-8541A; and a preferred radioligand is PluvictoTM.

Provided herein is a dendrimer complex comprising a 2-deoxyglucose (2DG) dendrimer and a neuroactive agent conjugated to an outer surface of the dendrimer. The dendrimer complex may further include one or more imaging agents and / or radioligands conjugated to an outer surface of the dendrimer. Such complexes are useful in methods for detecting or treating neurological diseases or disorders.

A precursor compound for a therapeutic, FAP-targeted radioligand comprises an FAP ligand that contains a covalent warhead.

The present invention relates to a compound of formula (0-a) or a pharmaceutically acceptable salt thereof. The compounds of the invention bind to proton sensing G protein coupled receptor type 4 (GPR4) and include a linker and a chelating agent, which may include a radioligand. These compounds of the invention are particularly useful in imaging and in the treatment of solid tumors. And (0-a).

Disclosed are methods of treating a cancer in a subject using at least one ATR inhibitor and a radionuclide-containing PSMA targeting agent such as 177Lu vipivotide tetraxetan, wherein the cancer has an over expression of PSMA on its cell membrane. The methods comprise contacting the cell with a therapeutically effective amount of a combination of at least one ATR inhibitor and 177Lu vipivotide tetraxetan.

Disclosed herein are radiolabeled compounds that can act as antagonists of the μ-opioid receptor, including methods of making and using the same. The selective mu opioid receptor antagonists disclosed herein can improve safety for subjects as well as enable studies of the μ-opioid receptor using agonist / antagonist radioligand pairs.

The invention provides an anti-CTLA-4 antibody or a nucleic acid encoding the anti-CTLA-4 antibody for use in treating prostate cancer in a subject, optionally in combination with a radioligand therapeutic agent such as lutetium (177LU) vipivotide tetraxetan. The invention further provides treatment methods for prostate cancer in a subject in need thereof, comprising administering the anti-CTLA-4 antibody or the nucleic acid encoding the anti- CTLA-4 antibody, optionally in combination with a radioligand therapeutic agent such as lutetium (177LU) vipivotide tetraxetan.

The present invention discloses compounds of Formula (I) and their complexes with radionuclides that can recognize both Somatostatin type 2 receptor (SSTR2) and cholecystokinin 2 receptor (CCK2R) and can be used in the diagnosis and treatment of diseases where either or both receptors are overexpressed.

A radionuclide labeled UCK2-targeting compound for use in radioligand therapy and imaging of UCK2 positive cancers, such as hepatocellular carcinoma (HCC) includes a compound having the structure of formula (I), (II), (III), (IV), (V) or a pharmaceutically acceptable salt thereof.

The present invention relates to the field of radiation oncology. Methods according to the present invention include using botulinum toxin and an anticholinergic drug to protect the gland from radiation damage and side effects caused by a radioligand. Methods according to the present invention also include using botulinum toxin to protect the gland from radiation damage caused by the radioligand. By using the methods according to the present invention, the present invention can provide effective protection of the gland from radiation damage.

The present disclosure is concerned with chemical release agents containing a release trigger (e.g., a benzisoxazole), a polymeric element, and an active agent such as, for example, a radioligand, a residue of a peptide, a residue of a protein, a residue of an oligonucleotide, or a residue of a small molecule therapeutic agent, containing the compounds, and methods for using the same. Also disclosed are intermediate compounds useful in the preparation of chemical release agents. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Described herein are radiopharmaceuticals for the treatment of PSMA-expressing cancers, and methods and / or uses of such compounds for the treatment of PSMA-expressing cancers, such as, for example, metastatic castration-resistant prostate cancer.

The present invention generally relates to the field of fluorescent probes comprising a cyanine dye with near-infrared (NIR) emission labelled with a PSMA-targeting moiety and their use in the targeting and imaging of cancer, in particular PSMA-expressing cancers, such as prostate cancer and metastases thereof. The fluorescent probes of the invention also include a different targeting ligand or a prosthetic group that can be radiolabeled, such as a radioligand, forming hybrid tracers that can be respectively used as heterobivalent agents or as bimodal agents in nuclear imaging and Fluorescence Guided Surgery. The invention also relates to methods for preparing these compounds, to pharmaceutical compositions and kits incorporating them and to methods of use them as diagnostic agents in imaging or therapy of diseases, particularly those associated with PSMA-overexpression.

Conjugates comprising an EETI-II based knottin peptide, comprising an engineered loop that binds to a cell surface molecule; and a chelator conjugated to the knottin peptide via a linker may be used for treating cancer in a patient. Conjugates may comprise a radionuclide-chelator complex.

The present disclosure relates to a method for treating prostate-specific membrane antigen (PSMA)-positive advanced metastatic castration-resistant prostate cancer (mCRPC) by administering a therapeutically effective amount of a PSMA-conjugated radioligand therapy (RLT) agent, preferably [177Lu]Lu-PSMA-617 (lutetium (177Lu) bipibotide tetraxetane), to taxane-naive patients who have progressed after receiving a second-generation ARPI.