23 results about "Castration resistant" patented technology

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

The invention belongs to the technical field of protein polypeptides, and particularly relates to a polypeptide targeting BRCA2 protein, application of the polypeptide and a medicine for treating prostatic cancer. The amino acid sequence of the polypeptide is shown as SEQ ID NO.1, the polypeptide has high binding capacity with BRCA2 protein, cell proliferation and tumor growth can be effectively inhibited when the polypeptide is delivered to prostatic cancer, and meanwhile the polypeptide has the capacity of degrading BRCA2 in a targeted mode. The combined application of the polypeptide and the PARP inhibitor can enhance the sensitivity of prostate cancer cells to the PARP inhibitor. Therefore, the polypeptide can be applied to preparation of a medicine for treating metastatic castration-resistant prostate cancer or preparation of a reagent for degrading the BRCA2 protein. The BRCA2 targeting PROTAC medicine can provide a new treatment strategy for prostatic cancer treatment, and the PARP targeting inhibitor is combined to provide a PARP inhibitor synthesis lethal treatment effect for metastatic castration resistant prostatic cancer patients.

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.

Provided is a novel method for treating castration resistant prostate cancer (CRPC), particularly CRPC that has acquired resistance to antiandrogen agents.　This antitumor agent is characterized by the co-administration of an antiandrogen agent and 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide or a salt thereof.

The present invention relates to a composition for the treatment of castration resistant prostate cancer, the composition comprising (i) a first active ingredient comprising a CDK9 degrading agent; and (ii) a second active ingredient, wherein the second active ingredient comprises olaparib. The effects of inhibiting tumor cell proliferation and promoting cell apoptosis of the composition are obviously higher than those of a single drug under the same dosage.

The present invention concerns pharmaceutical formulations of ARN-509, which can be administered to a mammal, in particular a human, suffering from an androgen receptor (AR)-related disease or condition, in particular cancer, more in particular prostate cancer, including but not limited to castration-resistant prostate cancer, metastatic castration resistant prostate cancer, chemotherapy-naive metastatic castration resistant prostate cancer, biochemically relapsed hormone sensitive prostate cancer, or high-risk, non-metastatic castration-resistant prostate cancer. In one aspect, these formulations comprise a solid dispersion of ARN-509 and HPMCAS. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by melt-extruding a mixture comprising ARN-509 and HPMCAS and optionally subsequently milling said melt-extruded mixture. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by spray drying a mixture comprising ARN-509 and HPMCAS in a suitable solvent.

The present disclosure provides methods for treating, reducing the severity, or inhibiting the growth of cancer (e.g., 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 CD3, either alone or in combination with an antibody, or antigen-binding fragment thereof, that specifically binds to programmed death 1 (PD-1) receptor.

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and / or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic to or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

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

The present invention concerns pharmaceutical formulations of ARN-509, which can be administered to a mammal, in particular a human, suffering from an androgen receptor (AR)-related disease or condition, in particular cancer, more in particular prostate cancer, including but not limited to castration-resistant prostate cancer, metastatic castration resistant prostate cancer, chemotherapy-naive metastatic castration resistant prostate cancer, biochemically relapsed hormone sensitive prostate cancer, or high-risk, non-metastatic castration-resistant prostate cancer. In one aspect, these formulations comprise a solid dispersion of ARN-509 and HPMCAS. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by melt-extruding a mixture comprising ARN-509 and HPMCAS and optionally subsequently milling said melt-extruded mixture. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by spray drying a mixture comprising ARN-509 and HPMCAS in a suitable solvent.

The present invention concerns pharmaceutical formulations of ARN-509, which can be administered to a mammal, in particular a human, suffering from an androgen receptor (AR)-related disease or condition, in particular cancer, more in particular prostate cancer, including but not limited to castration-resistant prostate cancer, metastatic castration resistant prostate cancer, chemotherapy-naive metastatic castration resistant prostate cancer, biochemically relapsed hormone sensitive prostate cancer, or high-risk, non-metastatic castration-resistant prostate cancer. In one aspect, these formulations comprise a solid dispersion of ARN-509 and HPMCAS. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by melt-extruding a mixture comprising ARN-509 and HPMCAS and optionally subsequently milling said melt-extruded mixture. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by spray drying a mixture comprising ARN-509 and HPMCAS in a suitable solvent.

Downregulated miR-99b-5p and upregulated mTOR cooperatively promotes the African American (AA) PCa aggressiveness and drug resistance. Nuclear mTOR, AR, and SMARCD1 are highly expressed in AA PCa (MDA PCa 2b) compared to EA PCa (LNCaP) cell line. miR-99b-5p inhibited protein levels of mTOR, AR / AR-V7 and SMARCD1 in cytoplasm and nuclei of EA and AA PCa. miR-99b-5p effectively inhibits cell proliferation / survival and induced cell apoptosis in EA and AA PCa cells. Moreover, combination of miR-99b-5p and enzalutamide (Enz) synergistically enhances the cytotoxicity against aggressive AA PCa and castration resistant prostate cancer (CRPC). miR-99b-5p or miR-99b-5p / Enz significantly reduces the recruitment of mTOR to the genes involved in the metabolic reprogramming in CRPC. miR-99b-5p can function as an epigenomic driver to modulate the mTOR / AR / SMARCD1 signaling axis in AA PCa and resistant CRPC. miR-99b-5p can be utilized as a biomarker for identifying the presence of prostate cancer.

The present invention belongs to the technical field of medicines, and relates to novel use of a kinase inhibitor. Disclosed is use of a compound of general formula (I) or a pharmaceutically acceptable salt, stereoisomer or crystal form thereof in the manufacture of a medicament for treating and / or preventing prostate cancer, wherein variables in the general formula are as defined in the specification. Researches show that the compound of general formula (I) or the pharmaceutically acceptable salt, stereoisomer or crystal form thereof has a therapeutic effect on prostate cancer, and further has a significant therapeutic effect on castration resistant prostate cancer and castration sensitive prostate cancer as well as metastatic castration resistant prostate cancer.

The present invention relates to the field of therapeutic antibodies for use in the treatment of individuals with castration-resistant prostate cancer. More specifically, the present invention relates to the treatment of castration-resistant prostate cancer using a bispecific antibody comprising an antigen binding site that can bind to an extracellular portion of ERBB2 and an antigen binding site that can bind to an extracellular portion of ERBB3. In addition, the present invention relates to the treatment of castration resistant prostate cancer using an antibody comprising an antigen binding site that can bind to an ERBB3 extracellular portion. The invention also relates to the treatment of castration resistant prostate cancer using a combination of one of the antibodies and an androgen receptor axis-targeting agent.

Embodiments of the invention are directed to the treatment of subjects with prostate cancer, in particular those with castration resistant prostate cancer, with glucocorticoid receptor antagonists. The prostate cancer may be one that has become resistant to androgen deprivation therapy, for example, by increase in glucocorticoid receptor expression and / or activity.

Compositions and treatment methods for cancer, such as enzalutamide resistant cancers, using one or more alternatives to daclatasvir (DCV). DCV has been shown to inhibit the Tribbles homolog 2 (TRIB2) pseudokinase encoded in humans by the TRIB2 gene, but more potent compounds are described herein that bind and inhibit the TRIB2 pseudokinase with greater affinity. TRIB2 is a target for several types of very aggressive cancers, such as castration resistant prostate cancer (CRPC), small cell lung cancer (SCLC), pancreatic neuroendocrine cancer (PNEC), triple negative breast cancer (TNBC), sarcomatoid kidney cancer, and melanoma.

To provide novel therapeutic agents for treating and / or diagnosing non localized prostate cancer, metastatic prostate cancer and / or castration resistant prostate cancer.SOLUTION: A composition for use in the treatment and / or diagnosis of prostate cancer comprises an antibody polypeptide that specifically binds to human kallikrein-2 (hK2), where the antibody polypeptide comprises: (a) a heavy chain variable region comprising compatibility determining region (CDR) CDRH1, CDRH2 and CDRH3 comprising the amino acid sequences shown by SEQ ID NO: 1, SEQ ID NO: 2 and SEQ ID NO: 3 respectively; and (b) a light chain variable region comprising compatibility determining region (CDR) CDRL1, CDRL2 and CDRL3 comprising the amino acid sequences shown by SEQ ID NO: 4, SEQ ID NO: 5 and SEQ ID NO: 6 respectively.SELECTED DRAWING: Figure 15

Pharmaceutical compositions including an effective amount of an antiandrogen or androgen antagonist in combination with a Plk inhibitor and methods of use thereof for treating cancer are disclosed. Administration of the combination of the active agents can be effective to reduce cancer cell proliferation or viability in a subject with cancer to the same degree, or a greater degree than administering to the subject the same amount of either active agent alone. The active agents can be administered together or separately. Methods of selecting and treating subjects with cancers, particular prostate cancers including castration resistant prostate cancer, breast cancers, particularly androgen receptor positive breast cancers, and pancreatic cancers are also provided.

The present invention relates to a combination of taprazopalide, or a pharmaceutically acceptable salt thereof, and enzalocamide, or a pharmaceutically acceptable salt thereof, for use in the treatment of metastatic castration resistant prostate cancer; and a method of extending its lifetime.

Disclosed herein are methods and uses of the polypharmacological modulator SR1903 and related compounds for inhibiting triggering receptor expressed on myeloid cells-1 (TREM-1) and treating diseases and conditions that are related to or mediated by TREM-1, such as inflammatory diseases, autoimmune diseases, metabolic disorders, and castration resistant prostate cancer (CRPC).

Disclosed herein are methods and uses of the polypharmacological modulator SR1903 and related compounds for inhibiting triggering receptor expressed on myeloid cells-1 (TREM-1) and treating diseases and conditions that are related to or mediated by TREM-1, such as inflammatory diseases, autoimmune diseases, metabolic disorders, and castration resistant prostate cancer (CRPC).

The invention relates to the technical field of nano material preparation, in particular to spine-shaped zinc oxide nanoparticles and a preparation method and application thereof.The preparation method comprises the steps that green tea extract powder is subjected to gamma-ray irradiation treatment, green tea polyphenol obtained through extraction treatment is mixed with a zinc source and an alkali solution, the pH is adjusted, and precipitates are obtained after a reaction; and calcining the precipitate to obtain the spine-shaped zinc oxide nanoparticles. Green tea polyphenol is obtained from the green tea extract powder subjected to gamma-ray irradiation treatment and serves as a reducing agent and a stabilizing agent; the green tea polyphenol reacts with a zinc source, so that the spine-shaped ZnO nanoparticles are synthesized in a green manner. The zinc oxide nanoparticle prepared by the preparation method has a spine-shaped structure and good crystallinity, the median inhibitory concentration of the zinc oxide nanoparticle in a castration resistant type prostate cancer cell line is obviously lower than that of a hormone sensitive type prostate cancer cell line, and the zinc oxide nanoparticle shows a more obvious cytotoxic effect on invasive prostate cancer.

This invention is directed to selective androgen receptor degrader (SARD) compounds including heterocyclic rings and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedys disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.