19 results about "Fulvestrant" patented technology

The present invention relates to a process for preparing B-[(7α,17β)-17-hydroxy-7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-trien-3-yl]-boronic acid, also known as Fulvestrant-3-boronic acid or ZB716, whose structure is reported below.

The invention relates to the technical field of biological medicine, in particular to application of a creatine related gene detection reagent in preparation of breast cancer prognosis products. The creatine related gene is an IGFBP1 gene and / or a TBC1D4 gene. According to the method, the expression levels of IGFBP1 and TBC1D4 genes in breast cancer patient samples are detected, a risk score is calculated by using a random survival forest (RSF) model, and the one-year, two-year and three-year survival rates of breast cancer patients are accurately predicted according to the risk score result. Meanwhile, the invention proves that IGFBP1 and TBC1D4 genes can be used as potential targets for breast cancer treatment, the IGFBP1 and fulvestrant as well as the TBC1D4 and vinblastine have stable binding capacity, and a new basis is provided for selection of individualized treatment medicines for breast cancer.

The invention relates to a compound as well as a preparation method and application thereof. The preparation method comprises the following steps: taking a compound 1 as an initial raw material, and sequentially carrying out condensation with thiourea, alkaline hydrolysis and oxidative coupling with pentafluoropentanethiol to obtain the compound 1, the raw materials are easy to obtain, the reaction conditions are mild, the post-treatment process is effectively simplified through an optimized pulping purification technology, the purity of the final product is up to 98.5% or above, and the method is suitable for industrial production. And a key material basis is provided for quality research of fulvestrant bulk drugs.

The invention discloses an application of PIK3CA and ESR1 gene co-mutation in predicting the sensitivity of a breast cancer patient to combined treatment of piloxil and fulvestrant. Through verification, it is found that PIK3CA and ESR1 gene co-mutation has high accuracy, sensitivity and specificity, can be used for accurate prediction of the sensitivity of breast cancer to pilosilil and fulvestrant combined treatment, can assist clinicians in judging the sensitivity of breast cancer patients to a pilosilil and fulvestrant combined treatment scheme, and can be used for predicting the sensitivity of the breast cancer patients to the pilosilil and fulvestrant combined treatment scheme. And good balance and maximum benefit among curative effect, adverse reaction and medication cost are achieved.

To provide a compound or a salt thereof which is rapidly metabolized to produce fulvestrant in the body.SOLUTION: The compound is a compound of formula (IV), an enantiomer, a diastereomer, a racemate, a pharmaceutically acceptable salt or a solvate thereof: Wherein R7 comprises certain phosphorus-containing esters and R8 represents certain substituents.SELECTED DRAWING: None

The present application relates to an intermediate of fulvestrant and a preparation method thereof. Specifically, the present application relates to a compound as shown in formula V and a preparation method thereof, wherein R 1 is hydrogen or a hydroxyl protecting group. The present application also relates to a preparation method for synthesizing fulvestrant via the compound as shown in formula V, which has the advantages of short reaction steps, mild and safe reaction conditions, high selectivity, simple operation and purification, high synthesis efficiency, and is suitable for large-scale production.

The invention relates to an injectable composition comprising compound I, pharmaceutically acceptable salts or solvates thereof; and at least one pharmaceutically acceptable excipient, wherein the injectable composition provides sustained release of compound I and thereby maintains blood plasma fulvestrant concentration. Also, the present invention used for method of treatment of breast cancer comprising compound of formula I, pharmaceutically acceptable salts or solvates thereof; and at least one pharmaceutically acceptable excipient.

Small molecule ERα biomodulators that kill therapy-resistant ERα positive breast, ovarian, and endometrial cancer cells are disclosed. In one embodiment, the small molecule biomodulator has increased therapeutic utility because of an increased ability to kill therapy-resistant cancer cells compared to BHPI and other conventional therapies (endocrine therapies, tamoxifen, and fulvestrant / ICI). The small molecule biomodulators not only inhibit proliferation of the cancer cells but kills them, which prevents reactivation of tumors years later. Compounds of the invention, such as ErSO-TFPy, are effective for treating ERα positive cancers such as breast cancer, ovarian cancer, uterine cancer, cervical carcinoma, endometrial cancer, and the like.

This invention discloses a nanomedicine and its application in the four-modal synergistic treatment of ER+ breast cancer, encompassing gas therapy, photothermal therapy, photodynamic therapy, and combined therapy, relating to the fields of biotechnology and new medicine. This nanomedicine uses an amphiphilic polymer as a carrier and organic compounds and photosensitizers as drug loading agents. Through the synergistic effects of four modes—photothermal, photodynamic, gas therapy, and combined therapy—it effectively inhibits the growth and metastasis of breast cancer cells. The amphiphilic polymer, based on PHHM-ADT, is modified with hydrogen sulfide gas as a donor, and its amphiphilicity allows for spontaneous assembly into nanoscale hollow, regular spheres. Utilizing the high permeability and retention effect (EPR effect) at the tumor site, it achieves efficient drug accumulation in tumor tissue. The prodrug PSF couples fulvestrant and pabuxiparin via disulfide bonds, and the photosensitizer IR808 integrates photothermal and photodynamic therapy. The synergistic effect of multiple mechanisms of action enhances the therapeutic effect.

This invention belongs to the fields of pharmaceutical chemistry and photocatalysis, and discloses a method for the photocatalytic synthesis of fulvestrant intermediates using pentafluorochloroethane and its applications. The method uses allyl ester compounds as substrates and pentafluorochloroethane (Freon-115) as a perfluoroalkylating agent. Under visible light irradiation, a specific photocatalytic redox system is constructed, and a boron-containing activator is introduced to synergistically activate the inert C-Cl bond, achieving the pentafluoroethylation-hydrogenation reaction of allyl esters to efficiently synthesize pentafluoropentyl benzoate. The method of this invention features mild reaction conditions, avoiding the use of highly toxic tin reagents in traditional processes, and simultaneously achieving high-value utilization of industrial waste gas Freon-115, demonstrating significant atom economy and promising industrial application prospects.

This invention discloses the use of AKT inhibitors in the manufacture of drugs for the prevention or treatment of breast cancer. In particular, it provides the combination of an AKT inhibitor and fulvestrant in the manufacture of drugs for the prevention or treatment of breast cancer. The combination of an AKT inhibitor and fulvestrant can effectively inhibit the proliferation and colonization of breast cancer cells. The combination is clearly more effective than monotherapy, exhibits additive or synergistic effects, has lower toxicity and side effects to normal cells, is safer, and provides a more effective method for treating breast cancer, thus having significant clinical value.

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 invention discloses application of an AKT inhibitor in preparation of a medicine for preventing or treating breast cancer. In particular, the invention provides application of an AKT inhibitor combined with fulvestrant in preparation of medicines for preventing or treating breast cancer. The AKT inhibitor and fulvestrant are combined to effectively inhibit the growth of breast tumor cells and cell clone formation, the combined effect is obviously superior to that of single medication, the additive or synergistic effect is achieved, meanwhile, the toxic and side effects on normal cells are low, the safety is high, a more effective method is provided for treating breast cancer, and the important clinical value is achieved.

The invention relates to a combined pharmaceutical composition of a CDK4 / 6 inhibitor and application of the combined pharmaceutical composition, in particular to a combined pharmaceutical composition containing a compound shown in a formula (I) or pharmaceutically acceptable salt of the compound and fulvestrant. The invention further relates to application of the combined pharmaceutical composition to treatment of breast cancer. The combined pharmaceutical composition disclosed by the invention has a better curative effect in the aspect of reducing the growth of tumors or even eliminating tumors.

Provided are combination therapies comprising a PI3K inhibitor (e.g., inavolisib), a CDK4 / 6 inhibitor (e.g., palbociclib), and fulvestrant; and methods of treating hormone receptor positive and HER2 negative (HR+ / HER2−) locally advanced or metastatic breast cancer in a patient (preferably a patient with a PIC3CA mutant patient) comprising administering a therapeutically effective amount of inavolisib, or a pharmaceutically acceptable salt thereof, a CDK4 / 6 inhibitor (e.g., palbociclib), and fulvestrant or letrozole.

The application belongs to the technical field of high polymer materials, and discloses a supramolecular hydrogel carrier, a supramolecular hydrogel loaded with fulvestrant and a preparation method and application thereof. Raw materials of the supramolecular hydrogel carrier are composed of carboxyl-modified PF127, amino-modified β-cyclodextrin, (ferrocenemethyl) trimethylammonium bromide, MXene and a residual amount of deionized water. The carboxyl-modified PF127 is a substance for forming a network structure of the supramolecular hydrogel carrier. The supramolecular hydrogel can be used as a carrier of fulvestrant for treating tumors, has the properties of being injectable, temperature-sensitive and having a porous structure, and is helpful for killing tumor cells.

The present disclosure relates to a pharmaceutical combination comprising (1) a first agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof and (2) a second agent which is an anti-hormonal agent or a pharmaceutically acceptable salt thereof. The present disclosure also relates to a pharmaceutical combination comprising (1) a first agent which is a CDK inhibitor or a pharmaceutically acceptable salt thereof, (2) a second agent which is an anti-hormonal agent or a pharmaceutically acceptable salt thereof, and (3) a third agent which is an agent that regulates the PI3K / Akt / mTOR pathway or a pharmaceutically acceptable salt thereof.

A combination therapy comprising enoxacin, palbociclib, and fulvestrant is provided, along with a method for treating locally advanced or metastatic breast cancer with PIC3CA mutations, hormone receptor-positive (HR+), and HER2-negative (HER2-), the method comprising administering therapeutically effective amounts of enoxacin, palbociclib, and fulvestrant. The combination therapy produced statistically significant and clinically meaningful improvements in comparable patients compared to administration of palbociclib and fulvestrant alone.

The invention relates to a compound as well as a preparation method and application thereof. The preparation method comprises the following steps: by taking a compound 1 and thiourea as starting raw materials, sequentially carrying out three-step reaction of nucleophilic substitution, alkaline hydrolysis and secondary nucleophilic substitution. The invention provides a synthetic route of the compound for the first time, and solves the technical problem of lack of a standard substance of the compound for a long time. The prepared standard substance can be used for establishing a monitoring analysis method for the key impurity in a fulvestrant production process, and has important significance for improving the quality of fulvestrant bulk drugs. The method has the advantages of mild conditions and safe operation, avoids the use of high-risk reagents, and is suitable for the preparation of standard substances.