66 results about "Fulvestrant" patented technology

Provided are a combination therapy comprising inavolisib, palbociclib and fulvestrant and methods of treating PIC3CA-mutant, hormone receptor positive (HR+) and HER2 negative (HER2-) locally advanced or metastatic breast cancer comprising administering a therapeutically effective amount of inavolisib, palbociclib and fulvestrant. The combination therapy produces a statistically significant and clinically meaningful improvement to the patient as compared to administering palbociclib and fulvestrant alone to a comparable patient.

The invention provides a preparation method of fulvestrant. According to the technical scheme, (7alpha, 17beta)-7-(9-bromononyl) estra-1, 3, 5 (10)-triene-3, 17-diol-17-acetate (intermediate I) is used as a starting material, fulvestrant is prepared through three-step reaction, the reaction condition is mild, the total molar yield is 52.8%, the HPLC purity of the obtained product fulvestrant can reach 99.8% or above, all the raw materials are domestic, operation is easy and convenient, column chromatography is not needed, and the method is suitable for large-scale production.

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 present disclosure relates to methods of treating breast cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a radiopharmaceutical compound having a GRPR antagonist moiety, such as [177Lu] Lu-NeoB, in combination with a CDK4 / 6 inhibitor, such as ribociclib, and a therapeutically effective amount of an endocrine therapy, such as fulvestrant.

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.

Long term storage stable fulvestrant-containing compositions are disclosed. The compositions can include fulvestrant; a solvent selected from dimethyl sulfoxide (DMSO), glycofurol, N-methyl pyrrolidone, and mixtures thereof; an oil mixture selected from a mixture of caprylic and capric triglycerides, a mixture of caprylic, capric and linoleic triglycerides, a mixture of caprylic, capric and succinic triglycerides, and a mixture of propylene glycol dicaprylate and propylene glycol dicaprate; and a sustained release member selected from benzyl benzoate, dihydrolipoic acid, benzyl alcohol and lipoic acid. The fulvestrant-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 223 nm, after at least about 24 months of storage at a temperature of from about 5° C. to about 25° C.

The utility model belongs to the field of medical instruments, and particularly relates to a fulvestrant intramuscular injection positioning ruler which comprises a long fixed ruler, two short shifting rulers and two arc-shaped pieces, and the two short shifting rulers are located on the two sides of the long fixed ruler respectively and rotationally connected with the long fixed ruler; the two arc-shaped pieces are symmetrically distributed on the two sides of the long fixed ruler, one side of each arc-shaped piece is fixedly connected with the long fixed ruler, the other side of each arc-shaped piece is fixedly connected with the short shifting ruler, an arc-shaped notch is formed in the inner side of each arc-shaped piece, and a plurality of positioning holes are formed in each arc-shaped piece. The fulvestrant injection device is directly aligned with the highest point of iliac spine and the peak of hip fissure of a human body through the positioning rule in one step, compared with operation modes such as a cross method and a line connection method, the time for manual searching and positioning is saved, meanwhile, injection of fulvestrant is completed in the positioning hole, and the injection efficiency is improved. And injection errors and complications caused by non-professional operation methods, inaccurate manual positioning, repeated part injection and the like are solved, so that the injection pain of a patient is reduced, and the treatment compliance and the life quality are improved.

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 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. # imgabs0 #

The invention relates to a fulvestrant intermediate and a preparation method thereof. Specifically, the invention relates to a compound shown as a formula V and a preparation method thereof, and R1 is hydrogen or a hydroxyl protecting group. The invention also relates to a preparation method for the synthesis of fulvestrant from the compound as shown in the formula V. The method has the advantages of short reaction steps, mild and safe reaction conditions, high selectivity, simplicity and convenience in operation and purification, high synthesis efficiency and the like, 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.

The invention belongs to the technical field of analytical chemistry, and particularly relates to a method for separating and determining a fulvestrant starting material SM1 and seven impurities thereof. The method comprises the following steps: carrying out gradient elution by taking octadecylsilane chemically bonded silica as a chromatographic column filler, taking purified water as a mobile phase A and taking an organic solvent as a mobile phase B, and then detecting in a detector with the detection wavelength of 240nm, wherein the flow velocity of the mobile phase is 0.9-1.1 ml / min, and the temperature of a column box of the chromatographic column is 28-32 DEG C. According to the method disclosed by the invention, the fulvestrant starting material SM1 and seven process impurities thereof can be simultaneously and completely separated and qualitatively or quantitatively detected, and the method is simple, convenient, feasible, good in reproducibility, strong in specificity and high in sensitivity. According to the method, the problem of separation and determination of the fulvestrant starting material SM1 and seven process impurities is solved, the quality of the fulvestrant starting material SM1 is ensured to be controllable, and the safety and effectiveness of the product are finally determined.

The present specification relates to a therapeutic combination of kapatinib, a CDK4 / 6 inhibitor (such as palbociclib, ribociclib, or abelsib) and fulvestrant for use in the treatment of breast cancer, and methods of treating a breast cancer patient with a combination of kapatinib, a CDK4 / 6 inhibitor (such as palbociclib, ribociclib, or abelsib) and fulvestrant.

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.

The invention belongs to the field of biological medicine, and provides application of a HER2-targeting antigen binding construct and a small molecule drug in combined treatment of breast cancer. Also provided is a pharmaceutical combination comprising an antigen binding construct targeting HER2, a compound of formula (I) or a pharmaceutically acceptable salt thereof, and fulvestrant, comprising an antigen binding construct targeting HER2. Also provided is a pharmaceutical combination comprising an antigen binding construct targeting HER2, comprising an antigen binding construct targeting HER2 and a chemotherapeutic drug. The invention further provides a kit for treating tumors. The kit comprises the medicine composition. In addition, the invention also provides application of the medicine composition in preparation of medicines for treating tumors and a method for treating tumors by using the medicine composition.

The present disclosure provides methods of treating breast cancer including administering aqueous suspensions com-prising solubilized fulvestrant, non-solubilized fulvestrant particles having one or more of an LD Dv(1 0) between about 1.5 and about 2.1 microns, an LD Dv(50) between about 5.5 and about 9.0 microns, and an LD Dv(90) between about 15 and about 35 microns, with the aqueous suspensions further including a surfactant, a polyvinylpyrrolidone, and a sugar alcohol, and a water-soluble excipient. The water-soluble excipient can be an aryl-Ci-6alk-OH, a Ci-6alkyl-OH, a buffering salt, a polysorbate, a polyalkylene glycol, a Ci-i2alkylene glycol, a phosphatidylcholine, or a combination thereof.

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.

The present invention relates to a pharmaceutical composition containing fulvestrant and a manufacturing method thereof. More specifically, the present invention relates to a pharmaceutical composition and a manufacturing method thereof that contains a specific nonionic surfactant, lecithin, castor oil and a specific alcohol in combination with fulvestrant, a poorly soluble drug, thereby improving the solubility of the drug and increasing the concentration of the drug in the formulation, thereby reducing the number of times the drug is administered while exhibiting the same pharmacological therapeutic effect as conventional fulvestrant formulations, thereby reducing the inconvenience of conventional formulations and increasing convenience for patients and medicine providers.

To provide a combination therapy for use in treating hormone receptor positive and HER2 negative locally advanced unresectable or metastatic breast cancer.SOLUTION: Provided is a method comprising administering a combination therapy including ipatasertib, fulvestrant, and a CDK4 / 6 inhibitor over a 28-day cycle.SELECTED DRAWING: Figure 1A

The present invention relates to a new process of preparation of an intermediate compound for the synthesis of Fulvestrant, and its use for the preparation of Fulvestrant.

The present invention belongs to the technical field of anti-tumor drug preparations and relates to a long-acting fulvestrant liposome for injection and a method for preparing the same. The long-acting fulvestrant liposome for injection comprises a fulvestrant inclusion complex, a liposome membrane material, a lyoprotectant, and an aqueous medium. The long-acting fulvestrant liposome for injection exhibits good stability, high encapsulation efficiency, long-lasting sustained release, and high bioavailability.

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.

The present application relates to the use of a VRAC modulator of formula I or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment of cancer in combination with an anti-hormone agent selected from the group consisting of: a. An anti-estrogen selected from fulvestrant, tamoxifen, toremifene and clomifene; and b. An anti-progestational hormone selected from the group consisting of mifepristone, ulipristal acetate, ensipristone, liropristone, and onapristone. # imgabs0 #

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.

The invention provides a fulvestrant composition comprising a pharmaceutically acceptable vehicle and not more than 2% total impurities and which, optionally, is free of a non-aqueous ester solvent. The composition may be used to treat hormone receptor positive metastatic breast cancer in a subject.

A set of small molecules ERα biomodulators that kill therapy-resistant ERα positive breast, ovarian, and endometrial cancer cells. These small molecules have increased therapeutic potential because of an increased ability to kill therapy-resistant breast cancer cells compared to BHPI and other conventional therapies (endocrine therapies, tamoxifen and fulvestrant / ICI). The new compounds do not only inhibit proliferation of the cancer cells but actually kills them, which prevents reactivation of tumors years later.