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24 results about "Radioligand" patented technology
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A radioligand is a radioactive biochemical substance (in particular, a ligand that is radiolabeled) that is used for diagnosis or for research-oriented study of the receptor systems of the body. In a neuroimaging application the radioligand is injected into the pertinent tissue, or infused into the bloodstream. It binds to its receptor. When the radioactive isotope in the ligand decays it can be measured by positron emission tomography (PET) or single photon emission computed tomography (SPECT). In in vivo systems it is often used to quantify the binding of a test molecule to the binding site of radioligand. The higher the affinity of the molecule the more radioligand is displaced from the binding site and the increasing radioactive decay can be measured by scintillography. This assay is commonly used to calculate binding constant of molecules to receptors.
18 F and 11 C labeled MCHR1 PET ligands
PendingCN122122117AIsotope introduction to heterocyclic compoundsIn-vivo radioactive preparationsDiseaseClinical study
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.
Owner:RICHTER GEDEON NYRT
Radioligand compounds and uses thereof
PCT designated stageWO2026098519A1Radioactive preparation carriersAntineoplastic agentsRadioactive Therapeutic AgentCancer cell
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.
Owner:CHENGDU NEW RADIOMEDICINE TECH CO LTD
Methods of treating cancer
PendingCN122074048AReduce risk of deathReduce the risk of progressionRadioactive preparation carriersAntineoplastic agentsSomatostatin receptorPharmacology
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.
Owner:NOVARTIS AG
EPHA2 targeting radioligand compounds and methods thereof
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.
Owner:RGT UNIV OF CALIFORNIA +2
Radioactive ligand compounds and uses thereof
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.
Owner:CHENGDU NEW RADIOMEDICINE TECH CO LTD
N-(5-substituted-[(1,3,4-thiadiazolyl) or (1,3-thiazolyl)](substituted)carboxamide compounds, pharmaceutical compositions, and methods of preparing the amide compounds and of their use
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.
carboxamide compounds, pharmaceutical compositions, and methods of preparing the amide compounds and of their use](https://images-eureka.patsnap.com/patent_img/4079ac85-80be-417c-854d-89b674ab9300/US20260022114A1-D00000.png "N-(5-substituted-[(1,3,4-thiadiazolyl) or (1,3-thiazolyl)](substituted)carboxamide compounds, pharmaceutical compositions, and methods of preparing the amide compounds and of their use")
Owner:GILEAD SCIENCES INC
Combinations of inhibitors of ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) with radiation for cancer therapy
PCT designated stageWO2026136237A1Organic active ingredientsOrganic chemistryPhosphodiesteraseNucleotide
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.
Owner:STINGRAY THERAPEUTICS INC
Chimeric radiopharmaceuticals targeting proton sensing receptor GPR4
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).
Owner:AMPHILIX AG +1
Anti-CTLA-4 antibody for treatment of patients with prostate cancer and combination therapy with a radioligand therapeutic agent
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.
Owner:ONCOC4 INC +1
UCK2-targeting compound for use in detecting and treating UCK2 positive cancers
PCT designated stageWO2026055591A1In-vivo radioactive preparationsHeterocyclic compound active ingredientsPharmaceutical medicineOncology
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.
Owner:CASE WESTERN RESERVE UNIV
Radioligand therapeutic regimens targeting PSMA
PendingCN121604981ARadioactive preparation carriersAntineoplastic agentsRadioactive drugPharmaceutical drug
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.
Owner:NOVARTIS AG
Targeted radioligand therapy for treating cancer
PCT designated stageWO2026096948A1Radioactive preparation carriersAntineoplastic agentsCell surface moleculesCancer research
Owner:TWOSTEP THERAPEUTICS INC
Combination therapies with ar-degrading agents and PSMA-targeting radioligands
PCT designated stageWO2026088112A1Inorganic active ingredientsRadioactive preparation carriersAntigenRadioactive drug
Described herein are combination therapies featuring a Prostate- Specific Membrane Antigen (PSMA)-targeting radiopharmaceutical, in particular [177Lu]Lu-PSMA-617, and an Androgen Receptor (AR) -degrading agent, in particular luxdegalutamide, and their use in treating cancers, such as, e.g., PSMA-expressing cancers.
Owner:NOVARTIS AG
Cleavable radioligands for targeting cell surface receptors and uses thereof
PendingEP4436979A4Dipeptide ingredientsPharmaceutical delivery mechanismReceptor degradationCell biology
The present application relates to a compound or a pharmaceutically acceptable salt and / or solvate thereof comprising one or more circulation enhancing groups, one or more target binding groups, one or more chelating groups, at one least cleavable linker and at least one branching group that is at least trivalent. The application further includes a radionuclide complex or a pharmaceutically acceptable salt and / or solvate thereof, comprising a compound of the application or a pharmaceutically acceptable salt and / or solvate thereof, and one or more radionuclides, and to compositions comprising the compound or the complexes. The present application also includes methods of using the compounds, complexes and compositions for targeting and / or killing target cells. For example, the compound includes a compound of Formula I
Owner:FULL-LIFE TECHNOLOGIES UK LTD
Synthesis of a precursor of radiopharmaceutical products
PCT designated stageWO2026027442A1Group 5/15 element organic compoundsIn-vivo testing preparationsRadioactive drugProstate cancer
The present disclosure is directed to a method for synthesizing a precursor of radiopharmaceutical products, CTT1298. CTT1298 is a precursor of [18F]CTT1057, a radioligand imaging (RLI) agent useful in the diagnostic of prostate cancer, and a key intermediate in the synthesis of other radiopharmaceutical products useful in the treatment of prostate cancer, like [177Lu]Lu-CTT1401, and [177Lu]Lu-CTT1403 which are radioligand therapeutic (RLT) agents.
Owner:NOVARTIS AG
FAP targeting compounds and conjugates thereof
Described herein are compounds targeting fibroblast activation protein (FAP), 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 FAP-implicated diseases and disorders.
Owner:NOVARTIS AG
Cleavable radioligands for targeting cell surface receptors and uses thereof
The present application relates to a compound or a pharmaceutically acceptable salt and / or solvate thereof comprising one or more circulation enhancing groups, one or more target binding groups, one or more chelating groups, at one least cleavable linker and at least one branching group that is at least trivalent. The application further includes a radionuclide complex or a pharmaceutically acceptable salt and / or solvate thereof, comprising a compound of the application or a pharmaceutically acceptable salt and / or solvate thereof, and one or more radionuclides, and to compositions comprising the compound or the complexes. The present application also includes methods of using the compounds, complexes and compositions for targeting and / or killing target cells. For example, the compound includes a compound of Formula I
Owner:FULL-LIFE TECHNOLOGIES UK LTD
FAP-targeting cyclic peptides and conjugates thereof
Cyclic peptides targeting fibroblast activation protein (FAP), and incorporation of these cyclic peptides into compounds for radioligand imaging and therapy, and methods and / or uses of such compounds for imaging, treatment and / or prevention of diseases and conditions involving FAP are described herein.
Owner:NOVARTIS AG
Methods of treating prostate cancer
The present disclosure relates to a method of treating prostate specific membrane antigen (PSMA) positive oligometastatic prostate cancer (OMPC) that progresses after decisive treatment of a primary tumor thereof, the method comprising administering a therapeutically effective amount of a PSMA binding radioligand therapeutic (RLT) agent, preferably [177Lu] Lu-PSMA-617 (lutetium (177Lu) vepivopeptide Tailaracetam). Furthermore, the disclosure relates to radioligand therapy for early stage prostate cancer patients to control recurrent tumor progression to fatal metastatic disease while maintaining quality of life by delaying treatment with androgen deprivation therapy (ADT).
Owner:NOVARTIS AG
Combination therapy consisting of phenoxythiamine and / or oxythiamine and radionuclide therapy
In the treatment of patients with tumors (especially malignant tumors), the substances phenoxythiamine (B-OT) and / or oxothiamine (OT) are administered as active ingredients concurrently with ongoing radionuclide therapy (RNT) (particularly radioimmunotherapy (RIT) and / or radiopeptide or radioligand or radiopeptide ligand therapy (RLT)). B-OT and / or OT administration is cyclical, meaning that dosing phases of B-OT and / or OT (“B-OT / OT dosing cycles”) alternate with treatment intervals (dosing intervals). During each B-OT / OT dosing cycle, B-OT and / or OT are administered at a predetermined dose (mg / kg patient body weight) for one or more consecutive days. This is followed by a treatment interval during which neither B-OT nor OT is administered, before the next B-OT / OT dosing cycle begins.
Owner:TAVARGENIX GMBH
FAP targeting compounds and conjugates thereof
Described herein are compounds targeting fibroblast activation protein (FAP), 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 FAP- implicated diseases and disorders.
Owner:NOVARTIS AG
Sigma-1 compounds, radioligands, and related methods of use
Among the various aspects of the present disclosure is the provision of sigma-1 compounds, their radioligands, and related methods of use. The present teachings include compositions for compounds that target the sigma-1 receptor, as well as their radioligands. The present teachings also include a method to assess treatment efficacy of a sigma-1 modulator in a subject in need, which can include acquiring medical images after administration of a sigma-1 radioligand, characterizing sigma-1 expression from the acquired images, and assessing treatment efficacy of a sigma-1 modulator in the subject based on the assessed sigma-1 expression. The methods can assess treatment efficacy in neurological diseases, including but not limited to Alzheimer's disease.
Owner:WASHINGTON UNIV IN SAINT LOUIS
How to treat prostate cancer
This disclosure relates to a method for treating prostate-specific membrane antigen (PSMA)-positive oligometastatic prostate cancer (OMPC) that has progressed after curative treatment for the primary tumor, comprising a therapeutically effective amount of a PSMA-binding radioligand therapy (RLT) agent, preferably [ 177 Lu]Lu-PSMA-617(Lutetium( 177 The present disclosure relates to a method comprising administering (Lu) bipivotide tetraxetan. Furthermore, the present disclosure relates to radioligand therapy for early prostate cancer patients to control the progression of recurrent tumors to lethal metastatic disease while maintaining quality of life by delaying treatment with androgen deprivation therapy (ADT).
Owner:NOVARTIS AG
Radioligands for imaging the LPA1 receptor
PendingUS20260068185A1Organic chemistryIn-vivo radioactive preparationsRadiologyPharmaceutical medicine
The present invention relates to radiolabeled LPA1 receptor antagonists of Formula (I):or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein, which are useful for the quantitative imaging of LPA1 receptors in mammals.
Owner:BRISTOL MYERS SQUIBB CO