156 results about "Hormone receptor" patented technology

The present disclosure provides a method of treating estrogen receptor-positive (ER+) breast cancer, comprising the combined administration of therapeutically effective amounts of a KAT6A / B inhibitor and a Menin inhibitor to a patient in need thereof.

Methods for treating a cancer patient with a neutrophil-to-lymphocyte ratio (NLR) greater than 3 are disclosed, comprising administering a nonsteroidal glucocorticoid receptor antagonist (GRA) to such a cancer patient, effective to reduce the patient's NLR. The methods include administering a nonsteroidal GRA and a cancer treatment to such a cancer patient, effective to reduce the patient's NLR and enhance the treatment of the cancer patient. The GRA may be orally administered. The nonsteroidal GRA may be a nonsteroidal compound comprising a heteroaryl ketone fused azadecalin structure (e.g., relacorilant) or an octahydro fused azadecalin structure (e.g., exicorilant). The cancer treatment may include chemotherapy, immunotherapy, radiation therapy, administration of an anti-angiogenic agent, administration of a growth factor inhibitor, and surgery. The methods may enhance the cancer treatment, improve the prognosis of the cancer patient, improve the survival of the cancer patient, and provide beneficial clinical effects and advantages to the patient.

The invention belongs to the technical field of biological medicine, and particularly relates to a reagent for improving ovarian development and a preparation method and application thereof. The reagent for improving ovarian development is prepared by mixing the following raw materials in parts by weight: 20-30 parts of N-acetylcysteine; 5 to 10 parts of tranexamic acid; 3 to 8 parts of creatine; and 3000 parts of water. According to the reagent, the mRNA expression of PKD1P6 and follicle stimulating hormone receptors (FSHR) in ovarian tissues is up-regulated, the activity and functions of cumulus granular cells are enhanced, and apoptosis of the cumulus granular cells is inhibited, so that the effects of effectively promoting follicle development and inhibiting the apoptosis of the cumulus granular cells are achieved.

The invention relates to the technical field of functional drinks, in particular to a polypeptide synergistically strengthened cubilose collagen composite drink with a breast enlarging function and a preparation method of the polypeptide synergistically strengthened cubilose collagen composite drink. The drink contains fish collagen tripeptide, elastin peptide, cubilose peptide, pueraria mirifica isoflavone, red clover isoflavone and saffron crocus extract. A lipidosome delivery system is adopted to entrap polypeptide to form a nano-scale compound, nano-emulsion entraps phytoestrogen, and berry polyphenol and lipidosome-polypeptide form a stable ternary compound. Through the multi-way synergistic effect that phytoestrogen activates a mammary gland estrogen receptor, polypeptide promotes connective tissue collagen synthesis and cubilose peptide activates a growth factor signal, mammary gland development is remarkably promoted, the breast enlarging effect is achieved, the bioavailability reaches 85% or above, and the retention rate of active ingredients stored at normal temperature for 24 months is larger than 90%.

Provided is a bifunctional compound, or a pharmaceutically acceptable salt, hydrate, solvate, metabolite or prodrug thereof, wherein the bifunctional compound is represented by Formula (I) : ABM-L-CLM (I); wherein: ABM is an androgen receptor binding moiety; -L-is a linking moiety; and CLM is a cereblon E3 ubiquitin ligase binding moiety represented by Formula (II) -1: wherein one end of the -L-is covalently joined to Q3, Q4, Q5 or Q6; and the other end of the -L-is covalently joined to the ABM. Also provided are a pharmaceutical composition comprising the bifunctional compound and a method for treating an androgen receptor related disease or disorder by administering the bifunctional compound.

The invention relates to an estrogen receptor alpha and fibroblast activating protein dual-targeting near-infrared fluorescent probe as well as a preparation method and medical application thereof. Specifically, the probe can be used as a fluorescence probe for developing cells co-expressing the estrogen receptor alpha and the fibroblast activating protein, and can also be used as a near-infrared fluorescence imaging probe for diagnosing benign / malignant lesions such as nodules / tumors co-expressing the estrogen receptor alpha and the fibroblast activating protein. The fluorescent probe can also be applied to research on related biological events in cells for co-expressing the estrogen receptor alpha and the fibroblast activating protein, and particularly can be applied to fluorescent navigation in tumor resection operations for co-expressing the estrogen receptor alpha and the fibroblast activating protein; particularly, the composition can be applied to the synergistic treatment of an anti-estrogen therapy and a photodynamic therapy on a diseased region which co-expresses the estrogen receptor alpha and the fibroblast activating protein.

A compound represented by formula (I) or a stereoisomer, tautomer or pharmaceutical salt thereof, and its use in the preparation of a medicament to prevent and / or treat estrogen receptor (ER) related diseases or disorders.

Methods and compositions for treatment of prostate cancers, such as androgen receptor (AR) deficient and androgen receptor (AR) low cancers, are disclosed. The methods include administration of an agent that inhibits activity of eIF4F or an agent that disrupts the eIF4F translation-initiation complex (composed of eIF4E, eIF4A, and eIF4G).

Described herein are radiotherapeutic agents that target tumor cells that express the follicle-stimulating hormone receptor (FSHR), and their use in the treatment and / or diagnosis of cancer.

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.

The present application relates to the technical field of biological medicine, in particular to a curcumin analogue, a synthetic method and application thereof. The present application takes curcumin as a lead compound, introduces cyclopropylmethyl, n-butyl and isobutyl in acetylacetone, introduces 4-acetylamino, 3,4-dimethoxy, 2-fluoro and 3-trifluoromethyl on a benzene ring, and designs and synthesizes a series of curcumin analogues. In vitro cytotoxicity experiments show that the killing effect of the newly synthesized curcumin analogue on prostate cancer cells is stronger than that of dimethyl curcumin, and the androgen receptor inhibition effect is also stronger than that of dimethyl curcumin.

The present invention discloses an adjuvant treatment of node-positive, carly stage, hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2—) breast cancer comprising administering an effective amount of an endocrine therapy in combination with an effective amount of abemaciclib or a pharmaceutically acceptable salt thereof.

The present invention is directed to a therapeutic agent for use in the treatment of a disease associated with gain-of-function of androgen receptor (AR) and / or with overexpression of an AR coactivator, such as Kennedy disease or cancer. The therapeutic agent of the invention comprises at least one inhibitor of an androgen receptor (AR) coactivator, selected from protein arginine methyltransferase 6 (PRMT6) inhibitor, lysine specific demethylase 1 (LSD1) inhibitor, or combinations thereof.

The present application relates to a kind of SGLT2 inhibitor in the preparation for treating hormone receptor low reaction type reproductive system disease in the application of drug, in particular, SGLT2 inhibitor and hormone can improve or enhance the sensitivity and / or for reversing the drug resistance of endocrine therapy drug, such as hormone, can enhance the therapeutic effect of such drug, especially in drug-resistant reproductive system disease and tumor treatment has good application prospect.

Systems, methods, and computer programs disclosed herein relate to the determination of a dosage of a mineralocorticoid receptor antagonist (MRA) for a patient suffering from a disease that can be treated with an MRA.

Provided herein are methods of determining tumoral sensitivity to hormonal (endocrine) therapy based upon an index of estrogen receptor (ER)- and progesterone receptor (PR)-related genes, referred to as the sensitivity to endocrine therapy index (SETER / PR index), and may have additional consideration for the proportion of ER gene (ESR1) RNA transcripts that contain a mutation relative to the value of the SETER / PR index. Further provided are methods of treating breast cancer patients determined to be sensitive to an endocrine therapy by the SETER / PR index.

The invention relates to a pharmaceutical composition comprising tamoxifen-loaded mesenchymal stem cell-derived exosomes enriched with miR-342 for use in the pharmaceutical and vaccine industry, in the treatment of cancer, in the treatment of breast cancer, in overcoming tamoxifen resistance in the treatment of estrogen receptor positive breast cancer using tamoxifen.

The application relates to a compound of Formula (I′) or (I):or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of thyroid hormone receptors, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease or disorder regulated by thyroid hormone.

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 application discloses a furan amide compound and application thereof, and belongs to the technical field of medicines.The structural general formula of the furan amide compound is shown as formula (I).The application provides a novel furan amide AR antagonist, the compound and the derivative thereof have obvious antagonistic activity on an androgen receptor, and exhibit good biological activity in in-vivo and in-vitro biological evaluation, the androgen receptor antagonistic activity is better than that of enzalutamide, the compound is effective in an AR F877L / T878A double-point mutant cell model resistant to enzalutamide, the activity is better than that of darolutamide, and the compound has good safety.Therefore, the compound can be applied to the treatment of diseases related to the androgen receptor as an androgen receptor antagonist, including but not limited to the treatment of prostate cancer, breast cancer, ovarian cancer and the like.

Described herein are radiotherapeutics that target tumor cells expressing the follicle-stimulating hormone receptor (FSHR) and their use in the treatment and / or diagnosis of cancer.

Disclosed herein are methods of treating a CDK4 / 6 inhibitor resistant estrogen receptor alpha-positive cancer in a subject having either a wild-type estrogen receptor alpha and / or a mutant estrogen receptor alpha, the method comprising administering to the subject a therapeutically effective amount of elacestrant, or a pharmaceutically acceptable salt or solvate thereof, wherein the mutant estrogen receptor alpha comprises one or more mutations selected from the group consisting of D538G, Y537X1, L536X2, P535H, V534E, S463P, V392I, E380Q and combinations thereof, wherein: X1 is S, N, or C; and X2 is R or Q. In some embodiments, the CDK4 / 6 inhibitor resistant estrogen receptor alpha-positive cancer is selected from the group consisting of breast cancer, uterine cancer, ovarian cancer, and pituitary cancer.

Relates to androgen receptor modulators and uses thereof. The present invention relates to compounds of formula (I)-(VI), in particular to compounds of formula (I)-(VI), pharmaceutical compositions comprising these compounds and the use of these compounds for the prophylaxis or treatment of diseases, in particular for modulating androgen receptor activity and treating diseases including prostate cancer.

The present invention relates to a novel compound for autophagy-mediated targeted degradation of an androgen receptor and medical use thereof. The novel compound according to the present invention is an autophagosome-tethering compound (ATTEC) targeting an androgen receptor, which has not been previously reported, and exhibits excellent binding affinity for the androgen receptor and the autophagy marker LC3, and thus can activate autophagy and ultimately target and degrade the androgen receptor, thereby effectively treating androgen receptor-associated diseases.

A double-stranded oligonucleotide construct is disclosed, configured such that a hydrophilic material and a hydrophobic material are conjugated through a single covalent bond or a linker-mediated covalent bond at both ends of a double-stranded oligonucleotide in order to efficiently deliver an androgen receptor-specific oligonucleotide in a cell; a nanoparticle capable of being produced by the self-assembly of double-stranded oligonucleotide constructs in an aqueous solution through hydrophobic interactions; and a composition for preventing hair loss or promoting hair growth containing the double-stranded oligonucleotide construct.The construction of double-stranded oligonucleotides that includes the androgen receptor-specific oligonucleotide and the composition to prevent hair loss or promote hair growth containing the same as an active ingredient can suppress the expression of an androgen receptor with high efficiency without side effects, and can thus exhibit excellent effects in preventing hair loss, particularly androgenetic alopecia, alopecia areata and telogen effluvium, and promoting hair growth.

The purpose of the present invention is to provide a composition having an action of inhibiting the androgen receptor (AR) pathway activity, and the present invention aims to effectively utilize discarded pomegranate seeds and add value thereto.　A pharmaceutical composition for inhibiting the androgen receptor (AR) pathway activity according to the present invention is characterized by containing a pomegranate seed extract. Furthermore, a preferred embodiment of the pharmaceutical composition for inhibiting the androgen receptor (AR) pathway activity according to the present invention is characterized in that the inhibition of the androgen receptor (AR) pathway activity is due to the inhibition of the transcription activity of the androgen receptor (AR). Furthermore, a preferred embodiment of the pharmaceutical composition for inhibiting the androgen receptor (AR) pathway activity according to the present invention is characterized in that the inhibition of the androgen receptor (AR) pathway activity is due to the inhibition of the androgen receptor (AR) protein expression.

The present disclosure relates to a method of determining a prognostic outlook for patients having metastatic breast cancer. The method includes receiving imaging data from an image of a patient that is receiving or that is to receive cycline dependent kinase 4 and 6 (CDK 4 / 6) inhibitor therapy for hormone receptor-positive (HR+) metastatic breast cancer. Radiomic heterogeneity features are extracted from imaging data associated with a metastasis within the imaging. A prognostic marker is determined from the radiomic heterogeneity features. The prognostic marker is indicative of a response of the patient to CDK 4 / 6 inhibitor therapy for HR+ metastatic breast cancer.

The invention belongs to the technical field of biological medicines, and particularly relates to a drug-loaded vesicle for treating thyroid cancer as well as a preparation method and application of the drug-loaded vesicle. The drug-loaded vesicle comprises a vesicle, wherein a cavity of the vesicle is loaded with radioactive iodine; the membrane surface of the vesicle is modified with: a) a first single-chain antibody fragment capable of specifically binding to thyroglobulin; according to the present invention, after the intravenous injection, the drug-loaded vesicle can be enriched in the thyroid cancer lesion area of the RAIR-DTC patient, such that the cancer cell proliferation is inhibited while the radioactive iodine is continuously released so as to provide the long-term treatment effect;