29 results about "Positive Estrogen Receptor" patented technology

Provided is an indole compound. In particular, disclosed are a compound represented by formula (II) or an isomer or pharmaceutically acceptable salt thereof and a use of the same as an estrogen receptor antagonist in preparing a drug for treating estrogen receptor-positive breast cancer.

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.

The invention relates to a breast cancer dynamic risk assessment method based on an adaptive model, and aims to improve the accuracy of early screening and risk prediction of breast cancer. The method comprises the following steps that firstly, clinical data of the unresected side mammary gland of an estrogen receptor positive breast cancer patient are obtained, and the data comprise the estrogen receptor state, the hormone treatment duration and mammary gland density classification; selecting an imaging detection mode according to the mammary gland density grading and the estrogen receptor state, and obtaining a calcification focus image of the target mammary gland; performing multi-parameter quantitative analysis on the image, and extracting parameters such as hydroxyapatite crystal proportion, calcification edge sharpness index and the like; and carrying out risk value calculation by using the trained adaptive risk assessment model, comparing the risk value with a preset risk grading threshold, and finally generating an assessment report based on a risk grade. According to the method, accurate dynamic risk assessment can be provided for the breast cancer patient, and personalized health management and intervention decision are supported.

The present invention provides a method of slowing the progression of ER + breast cancer in a patient comprising administering to the patient an effective amount of lasofoxifene or a pharmaceutically acceptable salt thereof and an effective amount of a CDK4 / 6 inhibitor (CDK4 / 6i) wherein breast cancer: (i) is estrogen receptor positive (ER +); (ii) having at least one function-acquired missense mutation within the ligand binding domain (LBD) of the estrogen receptor 1 (ESR1) gene; and (iii) have progressed and / or have oncogenic mutations in genes other than ESR1 during previous treatment with a CDK4 / 6 inhibitor.

The invention relates to methods and pharmaceutical composition for the treatment of estrogen-dependent cancers, particularly estrogen receptor-related cancers such as estrogen receptor-positive (ER+) cancers, like ER+ breast cancer (ER+BC). The invention relates to the combined use of an inhibitor of the methyltransferase-like protein 3 (METTL3) and an inhibitor of the nuclear DNA topoisomerase I (TOP1) for the treatment of estrogen-dependent cancers, particularly estrogen receptor-related cancers such as ER+ cancers. The inhibition of METTL3 increases the sensitivity of ER + breast cancer cells to Topoisomerase-1 inhibitor.

The application discloses application of AGPG in treatment of endocrine-resistant estrogen receptor positive breast cancer, and finds that AGPG can promote in-vitro endocrine-resistant cell cycle progression and cell proliferation through stable knockout research. Finally, a small interfering RNA drug is tested in an in-vivo experiment, and it is further proved that down-regulation of AGPG mediated by the small interfering RNA can significantly inhibit growth of tamoxifen-resistant MCF7 xenografts.

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.

The present invention discloses a method of treating a CDK4 / 6 inhibitor resistant estrogen receptor alpha positive cancer in a subject having 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 elastrant, or a pharmaceutically acceptable salt or solvate thereof, wherein the mutated 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.

The present disclosure relates to compositions and methods for the diagnosis and treatment or prevention of cancers, particularly cancers that exhibit elevated expression of FOXA1 and / or FOXA1 gene targets, such as certain breast, liver and / or prostate cancers, including luminal and / or ER-positive forms of breast cancer. Three previously identified adenosine receptor antagonists, CGS-15943, MRS-1220 and SCH-58261, as well as furan ring moiety-possessing derivatives of CGS-15943 are specifically provided for killing cancer cells in a manner that appears to involve activation of the aryl hydrocarbon receptor (AHR) by such compounds. The instant disclosure therefore provides for selecting and / or administering CGS-15943, MRS-1220, SCH-58261 and / or a furan-possessing derivative of CGS-15943, MRS-1220 and / or SCH-58261 as a therapeutic agent to target a cancer cell and / or subject having or at risk of developing a cancer. Methods and compositions for therapies that include such compounds are also provided.

Aspects of the disclosure relate to a composition and methods for treating breast cancer using a cannabinoid-based nanoplatform. The composition comprises phytocannabinoids, including THC, CBD, CBG, and CBC, incorporated into nanoparticles for enhanced bioavailability and controlled release. The method involves administering the composition to patients with breast cancer, particularly stages I and II, to inhibit VEGF pathways and induce apoptosis. The treatment targets estrogen receptor-positive (ER+), progesterone receptor-positive (PR+), HER2-positive, and triple-negative breast cancers. Aspects of the disclosure further provide the production of the composition using nano emulsification techniques to create nanoparticles smaller than 200 nm. This composition offers a novel, targeted approach to reducing tumor growth and metastasis in breast cancer patients.

Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM.

The present disclosure describes an oligobenzamide-based peptidomimetic agent with potent antiproliferative activity against triple negative breast cancer (TNBC), including TNBC cells representing all the known molecular subtypes. Lysosomal acid lipase A (LIPA) was identified as important for this agent's activity with the ER localization, not the lysosomal lipase function, of LIPA being critical. This agent can also block the growth in vitro and in vivo of multiple cancer types that have high basal level of ER stress and LIPA expression, including estrogen receptor-positive breast, pancreatic, glioblastoma and ovarian cancers. Thus, the inventors propose a new targeted strategy for TNBC and other rapidly proliferating cancers.

This invention discloses the application of WWP1 as a targeted biomarker for estrogen receptor-positive breast cancer. By detecting WWP1 gene amplification or protein overexpression, this invention can be used to assess ER. + Important biomarkers for prognosis and predicting response to CDK4 / 6 inhibitor therapy in breast cancer patients. This invention further provides a combination of WWP1 inhibitors and CDK4 / 6 inhibitors that exhibits potent synergistic antitumor effects both in vitro and in vivo, effectively overcoming drug resistance and improving the tumor immune microenvironment. Particularly in ER⁺ breast cancer patients, the combination therapy significantly improves treatment efficacy, providing a novel treatment strategy. This invention provides a novel ER⁺... + An integrated approach to breast cancer prognosis assessment and treatment has significant clinical application value.

Provided include methods, compositions and kits for treating hormone receptor positive (HR+) breast cancer, e.g., estrogen receptor positive (ER+) and progesterone receptor positive (PR+) breast cancer, in a subject. The method can comprise administrating a PI3K inhibitor and a cell cycle inhibitor, such as a PLK1 inhibitor, to the subject in a manner sufficient to inhibit or reduce progression of the cancer.

Disclosed herein are methods of inhibiting tumor growth or producing tumor regression in a subject having a drug-resistant estrogen receptor alpha positive cancer or a mutant estrogen receptor alpha positive cancer. The methods entail administering to the subject a therapeutically effective amount of RAD1901 having the structure:or a salt or solvate thereof.

The invention belongs to the technical field of tumor drugs, and particularly relates to application of a compound or salt thereof in preparation of drugs for treating estrogen receptor positive (HR < + >) breast cancer. The compound can effectively inhibit proliferation of estrogen receptor positive breast cancer cells and tumor growth of HR < + > breast cancer tumor-bearing mice, and can treat estrogen receptor positive breast cancer in cooperation with tamoxifen and / or fulvestrant. Meanwhile, the drug resistance of tamoxifen and / or fulvestrant to estrogen receptor positive breast cancer can be reduced.

Described herein are compositions, pharmaceutical compositions, kits, and methods of use relating to anti-Dio3os antisense RNA. In embodiments, antisense Dio3os compositions, kits, and methods are described to improve symptoms of osteoporosis, for example, osteoporosis induced by a disorder characterized by a thyroid hormone imbalance (i.e., hyperthyroidism or hypothyroidism). In embodiments, antisense Dio3os compositions, kits, and methods are described to improve sensitivity of cancer cells to anti-cancer therapeutics, for example, sensitivity of ER+ breast cancer or other breast cancer cells, thyroid cancer cells, prostate cancer cells, hepatocellular cancer cells, pancreatic cancer cells, and ovarian cancer cells that are sensitized or otherwise non-responsive to cancer therapeutics (for example, aromatase inhibitors or HDAC inhibitors). Combination therapies are also contemplated utilizing antisense RNA according to the present disclosure and other drugs, for example, thyroid and anti-cancer medications.

Disclosed herein are methods of treating a drug resistant estrogen receptor alpha-positive cancer in a subject having 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 drug resistant estrogen receptor alpha-positive cancer is selected from the group consisting of breast cancer, uterine cancer, ovarian cancer, and pituitary cancer.

The present invention provides peptides containing the BIG3 polypeptide-binding site in a PHB2 polypeptide, which inhibit the binding between a PHB2 polypeptide and a BIG3 polypeptide, and pharmaceutical compositions containing the peptide. The peptides of the present invention have the ability to bind not to PHB2, whose expression is found in organs throughout the human body, but to BIG3, which is a protein highly expressed specifically in particularly estrogen receptor-positive cancer, and have excellent growth suppressive effects on BIG3-positive cancer cells. Accordingly, the peptides of the present invention are useful as therapeutic agents for breast cancer which can avoid expression of side effects.

The present invention relates to quinazoline carboxamide azetidine compounds, and to pharmaceutical combinations and compositions comprising such compounds, preferably with at least one different therapeutic agent, preferably an anti-cancer agent, and to the use thereof for the treatment of diseases, preferably cancer, even more preferably estrogen receptor positive (ER +) cancer, in particular for the treatment of estrogen receptor positive (ER +) cancer. In particular in subjects resistant to endocrine therapy.

This invention relates to the treatment of breast cancer in a subject, and the subject can be either a male or female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed selective estrogen receptor modulator (SERM) (tamoxifen, toremifene, raloxifene), gonadotropin-releasing hormone (GnRH) agonist (goserelin), aromatase inhibitor (AI) (letrozole, anastrozole, exemestane), cyclin-dependent kinase 4 / 6 (CDK 4 / 6) inhibitor (palbociclib (Ibrance), ribociclib (Kisqali), lerociclib, abemaciclib (Vorzenio), trilaciclib, lerociclib), mTOR inhibitor (everolimus), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), alpelisib (Piqray) (an inhibitor of phosphatidylinositol-3-kinase subunit alpha (PI3Kα)), lapatinib, neratinib (Nerlynx), olaparib (Lynparza) (an inhibitor of the enzyme poly ADP ribose polymerase (PARP)), bevacizumab (Avastin), and / or fulvestrant treatments; metastasis in a subject suffering from breast cancer; HER2-positive; treating a subject suffering from ER mutant expressing breast cancer and / or treating breast cancer in a subject, by first determining the 18F-16β-fluoro-5α-dihydrotestosterone (18F-DHT) tumor uptake and identifying said subject as having AR-positive breast cancer based on 18F-DHT tumor uptake, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound and a cyclin-dependent kinase 4 / 6 (CDK 4 / 6) inhibitor.

The present application provides a kind of estrogen receptor positive breast cancer fluorescent probe by parent nucleus dye nile blue derivative, estrogen receptor (ER) recognition group tamoxifen and alkane chain three parts constitute, the probe has the structure of general formula 1.The probe shows folded conformation in water environment, there is photoinduced electron transfer effect between nile blue derivative and tamoxifen, no obvious fluorescence signal;When the probe recognizes ER protein, the recognition group is combined with the binding site, the conformation of the probe changes into unfolded conformation, and strong fluorescence signal is shown.The excitation wavelength of the probe is about 630 nm, the emission wavelength is about 640-700nm, has stronger tissue penetration ability, lower tissue self-absorption and light scattering, can be targeted to breast cancer cell overexpressed ER protein, and specifically highlights estrogen receptor positive breast cancer.

The present invention relates to a quinazoline carboxamide azetidine compound, and to pharmaceutical combinations and compositions comprising such a compound preferably together with at least one distinct therapeutic agent, preferably anti-cancer agent, as well as to uses thereof for treating a disease, preferably a cancer, even more preferably estrogen receptor-positive (ER+) cancer, in particular in a subject resistant to endocrinal therapy.

The present invention relates to a quinazoline carboxamide azetidine compound, and to pharmaceutical combinations and compositions comprising such a compound preferably together with at least one distinct therapeutic agent, preferably anti-cancer agent, as well as to uses thereof for treating a disease, preferably a cancer, even more preferably estrogen receptor-positive (ER+) cancer, in particular in a subject resistant to endocrinal therapy.

The invention provides a traditional Chinese medicine composition and application thereof. The traditional Chinese medicine composition is prepared from angelica sinensis, cynanchum atratum, poria cocos, radix bupleuri, radix paeoniae alba, honey-fried licorice root, moutan bark, fructus gardeniae, mint and rhizoma zingiberis and can be used for treating cancers, and the cancers refer to breast cancers including triple negative breast cancers and estrogen receptor positive breast cancers. The mechanism for treating cancers refers to inhibition of invasion activity and metastasis capability of tumor cells, inhibition of escape of host cell immunosuppression of the tumor cells and reduction of growth and development of the tumor cells. The traditional Chinese medicine composition can be combined with chemotherapeutic drugs for use.

The invention discloses a boron-functionalized berberine derivative, a preparation method thereof and application of the boron-functionalized berberine derivative in preparation of anti-breast cancer drugs, and belongs to the technical field of medicinal chemistry and medicine. The structure of the boron-functionalized berberine derivative is shown as a general formula (I), and the boron-functionalized berberine derivative is obtained by connecting an aromatic or heterocyclic segment containing a boric acid (or boric acid ester) group to the ninth site of a berberine parent nucleus through an ether bond, an ester bond or an amido bond. In-vitro activity tests show that the boron-functionalized berberine derivative has good proliferation inhibition activity on triple negative breast cancer (MDA-MB-468) and estrogen receptor positive breast cancer (MCF-7) cells, the selectivity index (SI) is higher than that of parent berberine and a control drug 5-fluorouracil, and a wider treatment window is shown. The boron functionalized berberine derivative has the advantages of novel structure, good activity and high selectivity, and can be used for preparing high-efficiency and low-toxicity anti-breast cancer drugs.