29 results about "Prostate specific membrane" patented technology

An inhibitor of a prostate specific membrane antigen and a pharmaceutical use thereof. Specifically, the present solution belongs to the field of radiopharmaceuticals and relates to a compound represented by formula (IV) or a pharmaceutically acceptable salt thereof.

The present disclosure provides methods for treating prostate cancer or metastatic castration-resistant prostate cancer, reducing the severity of prostate cancer or metastatic castration-resistant prostate cancer, or inhibiting the growth of prostate cancer or metastatic castration-resistant prostate cancer. The methods of the present disclosure comprise administering to a subject in need thereof a therapeutically effective amount of a bispecific antibody, or antigen-binding fragment thereof, that specifically binds to prostate specific membrane antigen (PSMA) and CD28, as a monotherapy or in combination with an anti-PD1 antibody.

To provide new compounds that can be used for the treatment of various disease states of prostate specific membrane antigen (PSMA) expressing cancers.SOLUTION: For example, provided is a complex comprising a compound of Formula CA009 as shown in the Figures, or pharmaceutically acceptable salts or solvates thereof, and a radionucleide selected from 203Pb and 212Pb.SELECTED DRAWING: Figure 1-10

The present invention relates to polyplexes comprising linear conjugates of LPEI and PEG. The LPEI and PEG fragments of the linear conjugates are preferably linked by a [3+2]cycloaddition between an azide and an alkene or an alkyne to produce a 1, 2, 3 triazole or a 4,5-dihydro-1H-[1,2,3]triazole. The linear conjugates are further conjugated to a targeting fragment capable of binding to prostate specific membrane antigen (PSMA) to enable selective interaction with a particular cell type. The conjugates can form polyplexes with therapeutic agents such as nucleic acids to deliver the therapeutic agents to cells.

The present application provides a marker inhibitor for diagnosing or treating a cancer expressing prostate-specific membrane antigen, the inhibitor being a compound represented by general formula I or a compound represented by general formula II or a compound represented by general formula III or an optical isomer, a pharmaceutically acceptable salt and / or a solvate thereof, and the present application also provides a preparation method thereof and a pharmaceutical composition containing the compound. The present application also relates to the use of the compound and a pharmaceutically acceptable salt, a solvate or a prodrug thereof in treatment as a therapeutic agent for treating a cancer expressing PSMA.

The present invention is directed to a conjugate including: (i) an antigen-binding polypeptide having a specific binding affinity to prostate specific membrane antigen (PSMA); and (ii) a benzylguanidine prosthetic group including a radionuclide, wherein (i) and (ii) are covalently bound. Further provided are a composition including the conjugate, and use of same, such as in a theranostic method.

The present disclosure provides multispecific antigen-binding molecules that bind to prostate specific membrane antigen (PSMA) and 4-1BB (anti-PSMA x anti-4-1BB). In certain embodiments, the present disclosure provides a multispecific anti-PSMA x anti-4-1BB antigen-binding molecule or antigen-binding fragment thereof comprising a first antigen-binding domain that specifically binds PSMA, a second antigen-binding domain that specifically binds 4-1BB, and a third antigen-binding domain that specifically binds 4-1BB. In certain embodiments, the molecules are multispecific antibodies or antigen-binding fragments thereof. In certain embodiments, the multispecific antibodies disclosed herein bind PSMA expressed on tumor cells with the first antigen-binding domain and 4-1BB on immune cells (e.g., T cells) with the second and third antigen-binding domains. In certain embodiments, the antibodies of the present disclosure are useful in treatment of a cancer. In certain embodiments, the antibodies are useful for treating a PSMA-associated disease or disorder (e.g., prostate cancer).

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

The present invention relates to a dual antigen-targeting protein complex comprising an antibody or its antigen-binding fragment and an affibody. More specifically, the dual antigen-targeting protein complex comprises an EGFR (Epidermal Growth Factor Receptor) or PSMA (Prostate Specific Membrane Antigen) target site containing an antibody or its antigen-binding fragment, and a CD137 target site containing an affibody bound to the antibody or its antigen-binding fragment. When the dual antigen-targeting protein complex or a composition containing it is used, cancer can be effectively prevented or treated.

Provided herein, inter alia, are antigen-binding molecules having binding specificity for differentiation population 3T cell receptors (CD3); an antigen binding molecule having binding specificity for prostate specific membrane antigen (PSMA); a cleavable linker sequence; and a protease activatable bispecific fusion protein, such as a protease activatable T cell adapter; as well as uses and methods of treatment.

The present disclosure provides multispecific antigen-binding molecules that bind to prostate specific membrane antigen (PSMA) and 4-1 BB (anti-PSMA x anti-4-1 BB). In certain embodiments, the present disclosure provides a multispecific anti-PSMA x anti-4-1 BB antigenbinding molecule or antigen-binding fragment thereof comprising a first antigen-binding domain that specifically binds PSMA, a second antigen-binding domain that specifically binds 4-1 BB, and a third antigen-binding domain that specifically binds 4-1 BB. In certain embodiments, the molecules are multispecific antibodies or antigen-binding fragments thereof. In certain embodiments, the multispecific antibodies disclosed herein bind PSMA expressed on tumor cells with the first antigen-binding domain and 4-1 BB on immune cells (e.g., T cells) with the second and third antigen-binding domains. In certain embodiments, the antibodies of the present disclosure are useful in treatment of a cancer. In certain embodiments, the antibodies are useful for treating a PSMA-associated disease or disorder (e.g., prostate cancer).

The present disclosure provides methods for treating clear cell renal cell carcinoma (ccRCC) or metastatic ccRCC, reducing the severity of ccRCC or metastatic ccRCC, or inhibiting the growth of ccRCC or metastatic ccRCC. The methods of the present disclosure comprise administering to a subject in need thereof a therapeutically effective amount of a bispecific antibody or antigen-binding fragment thereof, the bispecific antibody or antigen-binding fragment thereof specifically binding to prostate specific membrane antigen (PSMA) and CD28.

The invention relates to a multi-target molecular ligand as well as a preparation method and application thereof. The multi-targeting molecular ligand disclosed by the invention aims at prostate cancer and bone metastasis thereof, and the ligand simultaneously contains a polypeptide chain Glu-urea-Lys (ACUPA) capable of being recognized by a prostate specific membrane antigen (PSMA), is used for targeting diphosphoric acid of hydroxyapatite nanocrystals in bones, and is also combined with an anisidine fragment which is specifically combined with a Sigma-1 receptor. The multi-target molecular ligand can efficiently mark radionuclide and has excellent radiation stability, cell and animal experiments prove that the multi-target molecular ligand can be efficiently taken by PSMA positive prostate cancer RM-1 cells, RM-1 subcutaneous tumor models and RM-1 tibial metastatic tumor models, and can be used for developing diagnosis and treatment of PSMA positive prostate cancer and bone metastasis thereof, and diagnosis and treatment integration is achieved.

The invention relates to the field of nuclear medicine, in particular to a prostate specific membrane antigen small-molecule inhibitor and preparation and application of a radionuclide complex of the prostate specific membrane antigen small-molecule inhibitor. The prostate specific membrane antigen small-molecule inhibitor has a structure as shown in a general formula (I). The invention also provides a radionuclide complex containing radionuclide and the prostate specific membrane antigen small-molecule inhibitor. On the basis of a prostate specific membrane antigen small-molecule inhibitor, various medical radionuclides, such as a complex formed by 68Ga or 177Lu, are marked, and the complex can be respectively used for PSMA specific SPECT / CT (Single Photon Emission Computed Tomography / Computed Tomography), PET / CT (Positron Emission Tomography / Computed Tomography) imaging or prostate cancer treatment. The complex has the characteristics of high labeling rate, good stability, good tumor tissue targeting property and the like, provides a new idea for diagnosis and treatment integration of prostate cancer, and has a wide application prospect.

The invention belongs to the technical field of radiopharmaceutical chemistry and clinical nuclear medicine, and particularly relates to a glutamic acid-ureido-lysine compound containing an L-proline derivative as well as a preparation method and application of the glutamic acid-ureido-lysine compound. A radioactive preparation obtained by labeling the glutamic acid-ureido-lysine compound containing the L-proline derivative with radionuclide can be specifically combined with a prostate specific membrane antigen target spot, has high uptake at a tumor site with high expression of a prostate specific membrane antigen, has a good tumor / non-target ratio, and can be used for preparing a prostate specific membrane antigen. The medicine is a novel tumor radiopharmaceutical with popularization and application values.

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

The invention relates to the field of nuclear medicine, in particular to a prostate specific membrane antigen small-molecule inhibitor and preparation and application of a radionuclide complex of the prostate specific membrane antigen small-molecule inhibitor. The prostate specific membrane antigen small-molecule inhibitor has a structure as shown in a general formula (I). The invention also provides a radionuclide complex containing radionuclide and the prostate specific membrane antigen small-molecule inhibitor. On the basis of a prostate specific membrane antigen small-molecule inhibitor, various medical radionuclides, such as a complex formed by 68Ga or 177Lu, are marked, and the complex can be respectively used for PSMA specific SPECT / CT (Single Photon Emission Computed Tomography / Computed Tomography), PET / CT (Positron Emission Tomography / Computed Tomography) imaging or prostate cancer treatment. The complex has the characteristics of high labeling rate, good stability, good tumor tissue targeting property and the like, provides a new idea for diagnosis and treatment integration of prostate cancer, and has a wide application prospect.

The present invention relates to combinations for use and methods of treating cancers that express prostate specific membrane antigen (PSMA). In particular, the invention provides novel therapies based on the combination of a PSMA therapeutic agent, such as radiolabeled Compound I, and immuno-oncology (I-O) therapeutic agents, wherein said I-O therapeutic agents are selected from the group consisting of LAG-3 inhibitors, TIM-3 inhibitors, GITR agonists, TGF-β inhibitors, IL15 / IL-15RA complex, PD-1 inhibitors, PD-L1 inhibitors, and CTLA-4 inhibitors.

The present disclosure relates to prostate specific membrane antigen (PSMA) ligands. In particular, the disclosure relates to PSMA ligands having a glutamate-urea-lysine (GUL) moiety, a radioisotope and a chelating agent that can comprise a radiometal.

The present application relates to humanized and / or deimmunized antibodies, antibody fragments or antibody derivatives that bind to Prostate Specific Membrane Antigen (PSMA), and to methods for using said antibodies, antibody fragments or antibody derivatives in the treatment of prostate cancer and other neoplastic as well as neurological diseases.

Binding proteins that are specific for prostate specific membrane antigen (PSMA), multimers thereof, and conjugates thereof are described. Also described are PSMA binding proteins that include a diagnostically or therapeutically active component and / or a pharmacokinetics-modulating moiety, as well as methods for using the described PSMA binding proteins in medicine, for example, in diagnosis and therapy of cancer associated with PSMA expression.

The invention relates to a method for researching an action mechanism of organic framework nanoparticles on prostate cancer cells. The nanoparticles are PSMA-PEG-MOF (at) Enza + CpG, a pH responsive metal organic framework (MOF) carrier is synthesized through a solvothermal method, PEG and prostate specific membrane antigen (PSMA) antibody surface modification is sequentially performed, and then enzalutamide (Enza) and CpG oligodeoxynucleotide are co-loaded. According to the method disclosed by the invention, the killing effect of the nanoparticles on dendritic cell (DC) maturation, T cell activation and tumor cells is evaluated through an in-vitro experiment; the invention provides a set of complete research scheme for illustrating a specific molecular and cellular mechanism of the targeting nanoparticles for synergistically inhibiting tumor growth and activating anti-tumor immunity.

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).

The present disclosure relates to the synthesis of prostate specific membrane antigen (PSMA) ligands that are useful in the treatment of diseases like cancer. In particular, the disclosure relates to a method for synthesizing PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal.

Compositions and methods for the treatment of cancer, in particular prostate cancer, are described. According to certain embodiments, a method of treating cancer in a patient comprises administering to the patient a combination of a therapeutically effective amount of a bispecific antibody that bind to kallikrein related peptidase 2 (hK2) and cluster determinant 3 (CD3) and an antibody drug conjugate (ADC) targeting prostate specific membrane antigen (PSMA).

The present invention discloses a prostate specific membrane antigen (PSMA) binding compound, a radioactive isotope complex thereof, and the use thereof in nuclear medicine as a tracer and an imaging agent for different disease states of prostate cancer.

Provided herein are a compound of Formula (I), a pharmaceutical composition comprising said compound, and method of use of the compound or pharmaceutical composition in the diagnosis or treatment of a disease or disorder, e.g., a disease or disorder characterized by overexpression of prostate-specific membrane antigen (PSMA).

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and / or mammalian tissue overexpressing prostate specific membrane antigen ("PSMA") where the compounds are represented by the following Formulas (I), or a pharmaceutically acceptable salt thereof (IA), or a pharmaceutically acceptable salt thereof (II), or a pharmaceutically acceptable salt thereof, wherein M1 is independently at each occurence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.