151 results about "Membrane antigen" patented technology

The invention discloses a class of radiopharmaceutical labeled precursors targeting prostate specific membrane antigens, the structure of the radiopharmaceutical labeled precursors is shown as the following: # imgabs0 #, a precursor reagent RESCA-PSMA-1802 targeting prostate specific membrane antigens is synthesized for the first time, the reagent can be labeled by using an 18F-Al method to prepare a positron imaging agent 18FAl-RESCA-PSMA-1802, and the reagent can be used for preparing the prostate specific membrane antigens. The polymer has good stability and biological activity in vivo and in vitro, has good targeting property on prostate cancer cells, can reflect tumor recurrence or metastasis conditions, and is very suitable for PET imaging.

Disclosed herein are isolated polypeptide and polypeptide complex compositions that comprise a first antigen recognizing molecule that binds to CD28 and a second antigen recognizing molecule that binds to prostate-specific membrane antigen (PSMA).

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 pharmaceutical compositions comprising [61Cu]Cu-NODAGA-PSMA I&T or a pharmaceutically acceptable salt thereof. The present disclosure also relates to methods of imaging subjects suspected of having or diagnosed with a prostate-specific membrane antigen (PSMA)-expressing tumor by administering the pharmaceutical compositions described herein and generating one or more radiographic images of the subject.

The present disclosure relates to the synthesis of prostate-specific membrane antigen (PSMA) ligands useful in the treatment of diseases such as cancer. In particular, the present disclosure relates to methods for synthesizing PSMA ligands having a glutamic acid-urea-lysine (GUL) moiety and a chelator that may include a radiometal.

The invention relates to a molecular probe for targeting a prostate specific membrane antigen and application, and belongs to the technical field of nuclear medicine. The invention provides a molecular probe for targeting a prostate specific membrane antigen, and the molecular probe successfully obtains a PSMA targeting molecular probe by introducing iodobenzene butyric acid and a PEG4 group on the basis of a PSMA-617 molecular structure on the basis of a double-ligand covalent coupling technology. The molecular probe has the advantages that the residence time of the molecular probe in a tumor area is obviously prolonged, the treatment effect is improved, the requirement for radioactive dose is reduced, and radiation damage to surrounding normal tissues is reduced; the specificity is excellent, a tumor area with high PSMA expression can be accurately targeted, and tumors with different PSMA expression levels can be effectively distinguished; the speed of reaching a target tumor is high, and an ideal imaging effect can be realized only in 20 minutes. In conclusion, the molecular probe has great advantages in diagnosis and treatment of PSMA high-expression tumors, and has high specificity and high efficiency.

Prostate-specific membrane antigen targeted high-affinity agents for endoradiotherapy of prostate cancer are disclosed.

The present invention discloses an antibody targeting prostate-specific membrane antigen, an antigen-binding fragment thereof, a preparation method and uses thereof. In the antibody or its antigen-binding fragment, the amino acid sequences of HCDR1, HCDR2 and HCDR3 are respectively as shown in SEQ ID NO:4, SEQ ID NO:5 and SEQ ID NO:6; and / or, the amino acid sequences of LCDR1, LCDR2 and LCDR3 are respectively as shown in SEQ ID NO:7, SEQ ID NO:8 and SEQ ID NO:9. The antibody can specifically bind to the extracellular domain protein of human and monkey PSMA, can effectively bind to C4-2 and 22RV1 cells, and the ADC containing the same can effectively kill tumor cell lines.

The invention relates to a new therapeutic radiopharmaceutical as an inhibitor of prostate-specific membrane antigen (iPSMA), wherein 1,4,7,10-tetraazacyclododecane-N, N′, N″, N″″ -tetraacetic acid (DOTA) bonded to the heterocyclic molecule hydrazinonicotinamide (HYNIC), generates a rigid chemical structure that minimises the number of conformers and intramolecular hydrogen bonds, thereby producing a favourable spatial orientation of the active site (Lys(Nal)—NH—CO—NH-Glu) in the molecule, for biological recognition by the PSMA protein. The new DOTA-HYNIC-iPSMA radiopharmaceutical accumulates, with high affinity in vivo, in tumours that overexpress the PSMA protein, acting as a radiotherapeutic or radiodiagnostic agent. The purpose of the invention is to provide a new specific radiopharmaceutical (molecular target radiopharmaceutical) for the detection and treatment of tumours with PSMA overexpression. Radiolabelling of the new molecule is demonstrated with lutetium-177, actinium-225, terbium-161, gallium-67 or gallium-68 isotopes.

Disclosed are methods for imaging inflammation associated with inflammatory bowel disease (IBD), including administering to a subject a prostate-specific membrane antigen (PSMA)-targeted imaging agent and taking an image.

The present disclosure provides methods for treating, reducing the severity, 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 prostate- specific membrane antigen (PSMA) and CD28 as monotherapy or in combination with an anti-PDl antibody.

The present invention relates to tissue targeting compounds. In particular, the present invention relates to tissue targeting compounds comprising a monoclonal antibody or antigen binding fragment thereof having binding affinity for prostate specific membrane antigen (PSMA). Furthermore, the present invention relates to a combination, preferably a pharmaceutical combination comprising a tissue targeting compound of formula (I) and another agent. The combinations are useful in therapy, preferably in the treatment of hyperproliferative diseases such as cancer. # imgabs0 #

Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

This invention provides a dansulphamide-modified PSMA-targeting compound with the structure shown in Formula A or Formula I; wherein R1 is an amino acid analog structure; R2 is a prostate-specific membrane antigen-targeting compound structure; R3 is a radionuclide chelating group; L is -(X)n-(CH2)m-(Y)q-, where X and Y are independently selected from lysine, glutamic acid, or derivatives containing lysine or glutamic acid, n is an integer from 0 to 10, m is an integer from 0 to 20, and q is an integer from 0 to 6, wherein each CH2 can be individually replaced by -OCH2-, -NH(CO)-, or -(CO)-NH-. This invention also provides a radionuclide label based on the structure of the compound. The compound and the radionuclide label exhibit high tumor uptake and retention times, making them suitable for radionuclide therapy and imaging of tumors with high PSMA expression.

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 relates to small molecules having high affinity and specificity to prostrate-specific membrane antigen (PSMA) and methods of using them for therapeutic and diagnostic purposes.

Disclosed herein are isolated polypeptide and polypeptide complex compositions that comprise a prostate-specific membrane antigen (PSMA) binding domain that is linked to a peptide that impairs binding of the PSMA binding domain to PSMA.

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.

The present invention discloses a complex comprising (a) a compound, which is CA007 *, CA008 *, or CA009 *, or a pharmaceutically acceptable salt thereof, and (b) a radionuclide, which is selected from the group consisting of 203Pb and 212Pb. Also disclosed is the use of said complexes in the manufacture of a medicament for the treatment of cancers expressing prostate specific membrane antigen (PSMA). (CA007 *) (CA008 *) (CA009 *)

The present disclosure provides methods for treating, reducing the severity, or inhibiting the growth of clear cell renal cell carcinoma (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 that specifically binds prostate-specific membrane antigen (PSMA) and CD28.

An anti-PSMA peptide includes an STMG (SEQ ID N0;2) motif or a structurally similar PSMA-binding variant thereof. The anti-PSMA peptide may be used as a targeting domain in, for example, a multi specific compound, chimeric antigen receptor (CAR) compound, a targeted immunotherapeutic compound, a targeted therapeutic compound, a targeted imaging compound, or as a capture moiety immobilized to a substrate in an assay device. Compounds that include the anti-PSMA peptide can be used in methods of treating a disease (e.g., cancer) in subject, methods of detecting cells that express PSMA, and / or methods of isolating cells that express PSMA.

Imaging and radiotherapeutic agents targeting fibroblast-activation protein-α (FAP-α) and / or prostate-specific membrane antigen (PSMA) and their use in imaging and treating FAP-α and / or PSMA-related diseases and disorders are disclosed.

A treatment for patients having cancer expressing Prostate Cancer Specific Membrane Antigen (PSMA) is disclosed. Said treatment involves the use of an 225Ac-radioconjugate, in particular 225Ac-PSMA-I&T. A dosage regimen that entails more frequent administration of the 225Ac-radioconjugate at lower dose level may be employed. This involves the use of a dosage of 50-75 kBq / kg of body weight on a dosing schedule of every 4-6 weeks. A flat dosing may also be employed where the dose does not depend on the body weight of the subject. Such dosing improve the benefit / risk profile with fewer adverse events and less discontinuations, dosing interruptions and reductions in dose. Of particular importance is a reduction in salivary gland toxicity and xerostomia.

A prostate-specific membrane antigen (PSMA)-targeting ligand compound and a chelate thereof and use thereof are provided. The PSMA-targeting ligand compound has a structure as shown in formula I, where R1, R2 and R4 are each independently selected from the group consisting of H and optionally substituted linear or branched C1-C5 alkyl; R3 is selected from the group consisting of optionally substituted aryl and optionally substituted heteroaryl; X is a sulfur atom or an oxygen atom; Y is selected from the group consisting of a chemical bond and —NH—(CH2)m-, where m is an integer selected from 0-18; and Z is a radioactive metal ion chelating group.

A method for imaging inflammation associated with inflammatory bowel disease (IBD) has been disclosed, which involves administering an imaging agent targeting prostate-specific membrane antigen (PSMA) to a subject and acquiring images.

Provided herein are, inter alia, methods of treating prostate cancer in a subject by administering to the subject a combination comprising i) a chimeric polypeptide targeting PSMA and CD3, and ii) an androgen receptor antagonist.

The invention belongs to the technical field of antibody preparation, and particularly relates to an anti-human prostate specific membrane antigen (PSMA) antibody and application thereof. The amino acid sequences of CDR1-3 on a light chain variable region of the antibody are respectively shown as SEQ ID NO.3-5, and the amino acid sequences of CDR1-3 on a heavy chain variable region of the antibody are respectively shown as SEQ ID NO.8-10. The antibody with the complementarity determining region sequence provided by the invention can specifically recognize PSMA expressed by cells and tissues, has good affinity in combination with the PSMA, has high recognition sensitivity, can effectively resist the interference of complex non-target protein components in the cells / tissues, has no specific combination with non-target antigens, is suitable for immunological detection of the PSMA, and has good application prospects. The kit is especially suitable for western blot detection and immunohistochemical methods, and can reduce the occurrence rate of false positive and false negative results and improve the accuracy of immunodiagnosis.

The present application relates to the technical field of medicine, in particular to a functional nanomaterial based on choline phosphate-cell membrane interaction and application thereof.The present application modifies manganese mineralized black phosphorus nanomaterial by bio-inspired polymer pGluCP adsorption, which retains the excellent biocompatibility and photothermal performance of BP, and at the same time, pGluCP enhances the 'chassis' effect of the material, captures tumor-related antigens, and can simultaneously capture water-soluble antigens and water-insoluble membrane antigens and form pathogen-like micro-nanoparticles, which is helpful for antigen delivery and APC presentation, and provides a feasible tool for capturing non-water-soluble membrane antigens, which is a major challenge.MnBP and pGluCP synergistically act, and can realize the personalized conversion of autologous tumors to vaccine production and delivery.

Disclosed herein are modified HIV envelope immunogens, engineered nanoparticle vaccines comprising modified HIV envelope immunogens and methods of use thereof for HIV vaccines.

The invention relates to the technical field of radiopharmaceutical chemistry and clinical nuclear medicine, in particular to an amino adipic acid-urea derivative containing L-proline and application of the amino adipic acid-urea derivative. The radioactive preparation obtained by labeling the amino-containing adipic acid-urea derivative with radionuclide has high uptake in tumors, meanwhile, the uptake in kidneys is effectively reduced, and the radioactive preparation is specifically combined with prostate specific membrane antigens and can be used as a novel tumor radioactive drug with popularization and application values for prostate cancer diagnosis.