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91 results about "Estrogenic drug" patented technology

Fulvestrant, a steroidal antiestrogen and a drug used in the treatment of breast cancer. Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body.

Benzopyran-containing compounds and method for their use

Certain benzopyran antiestrogens are disclosed for treating estrogen sensitive diseases such as breast cancer. Prodrug forms provide ease of manufacturing, good shelf life, and bioavailability, and preferred stereoisomers are shown to be more effective than racemic mixtures.
Owner:ENDORES & DEV

Prevention and treatment of androgen-deprivation induced osteoporosis

This invention provides: 1) a method of treating androgen-deprivation induced osteoporosis and / or bone fractures and / or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 2) a method of preventing androgen-deprivation induced osteoporosis and / or bone fractures and / or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 3) a method of suppressing or inhibiting androgen-deprivation induced osteoporosis and / or bone fractures and / or loss of BMD in a male subject suffering from prostate cancer; and 4) a method of reducing the risk of developing androgen-deprivation induced osteoporosis and / or bone fractures and / or loss of BMD in a male subject suffering from prostate cancer, by administering to the subject a pharmaceutical composition comprising an anti-estrogen agent and / or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein.
Owner:GTX INCORPORATED +1

Peptide antiestrogen compositions and methods for treating breast cancer

InactiveUS6306832B1Low backgroundReduction of nonspecific backgroundPeptide/protein ingredientsGenetic material ingredientsCo activatorCancer research
Disclosed are methods and compositions comprising native, site-specifically mutagenized, and synthetic peptides comprising portions of the human estrogen receptor, or estrogen receptor co-activator, and nucleic acid compositions encoding these polypeptide compositions. Also disclosed are methods for synthesizing phosphotyrosyl and malonyltyrosyl peptide derivatives and their use as antiestrogen compositions in the treatment of breast cancers, the preparation of pharmaceutical compositions, diagnostic kits, and the development of related assays for use in antitumor therapies.
Owner:UNIVERSTIY OF CALIFORNIA

Methods and kits for diagnosing tumorigenicity and determining resistance to the antineoplastic effects of antiestrogen therapy

Methods and kits for diagnosing tumorigenicity and for determining whether a cancer patient is resistant to the pharmacological effects of antiestrogen therapy. Increased levels of the PCDGF (GP88) growth factor are indicative of tumorigenicity and resistance to the pharmacological effects of antiestrogen therapy. The methods and kits of the invention are useful for assessing the tumorigencity of a biological sample from a patient and determining whether the patient is a candidate for antiestrogen, including tamoxifen, therapy.
Owner:A & G PHARMA

Trans-clomiphene for metabolic syndrome

The present invention relates to the administration of compositions comprising an antiestrogen, preferably trans-clomiphene, for treating metabolic syndrome in a subject. The invention is also directed to methods for reducing fasting glucose levels in a subject by administering a composition comprising an antiestrogen, preferably trans-clomiphene.
Owner:REPROS THERAPEUTICS

Predicting breast cancer treatment outcome

Methods and compositions are provided for the identification of expression signatures in ER+ breast cancer cases, where the signatures correlate with responsiveness, or lack thereof, to treatment with tamoxifen or another antiestrogen agent against breast cancer The signature profiles are identified based upon sampling of reference breast tissue samples from independent cases of breast cancer and provide a reliable set of molecular criteria for predicting the efficacy of treating a subject with breast cancer with tamoxifen or another antiestrogen agent against breast cancer. Additional methods and compositions are provided for predicting responsiveness to tamoxifen or another antiestrogen agent against breast cancer in cases of breast cancer by use of three biomarkers. Two biomarkers display increased expression correlated with tamoxifen response while the third biomarker displays decreased expression correlated with tamoxifen response.
Owner:THE GENERAL HOSPITAL CORP +1

Method of treating androgen receptor (AR) -positive breast cancers with selective androgen receptor modulator (SARMS)

ActiveUS20140350102A1Treating and preventing and suppressing and inhibiting metastasisProlonged progression-free survivalBiocideOrganic chemistryToremifeneLymphatic Spread
This invention relates to the treatment of breast cancer in a subject, for example a 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 SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and / or fulvestrant treatments; metastasis in a subject suffering from breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.
Owner:UNIV OF TENNESSEE RES FOUND

Genetic markers and diagnostic methods for resistance of breast cancer to hormonal therapies

This application provides a method to identify genetic markers associated with increased sensitivity or resistance to hormonal therapies using an outlier analysis. More specifically, this application discloses that amplifications on chromosomes 8 and 17 are associated with increased proliferation and poor outcome in ER-positive breast cancer, and amplicons 17q21.33-q25.1, 8p11.2 and 8q24.3 may be responsible for higher proliferation and poor outcome in the setting of antiestrogen, in particular Tamoxifen, treatment clinically observed in a subset of ER-positive, HER2-negative breast cancers. The invention also provides use of the identified genetic markers in the development of targeted treatments for antiestrogen-resistant ER-positive breast cancers as well as in improving current methods of drug response prediction.
Owner:RUTGERS THE STATE UNIV

Diagnosis and treatment of breast cancer

InactiveUS20060154267A1Improve survival outcomeGene expressionMechanical/radiation/invasive therapiesData processing applicationsCurative effectOncology
Methods and compositions are provided for the identification of expression signatures in ER+ breast cancer cases, where the signatures correlate with responsiveness, or lack thereof, to treatment with tamoxifen or another antiestrogen agent against breast cancer The signature profiles are identified based upon sampling of reference breast tissue samples from independent cases of breast cancer and provide a reliable set of molecular criteria for predicting the efficacy of treating a subject with breast cancer with tamoxifen or another antiestrogen agent against breast cancer. Additional methods and compositions are provided for predicting responsiveness to tamoxifen or another antiestrogen agent against breast cancer in cases of breast cancer by use of multiple biomarkers. Two biomarkers display increased expression correlated with tamoxifen response while two other biomarkers display decreased expression correlated with tamoxifen response.
Owner:AVIARADX +1

Treatment and prevention of benign breast disease with 4-hydroxy tamoxifen

ActiveUS7507769B2BiocideAbsorbent padsAnti estrogenicBenign breast condition
The present invention provides methods for treating and preventing benign breast disease by administering 4-hydroxy tamoxifen to a patient. When percutaneously administered to a patient's breasts, 4-hydroxy tamoxifen concentrates locally, and exerts an anti-estrogenic effect. In patients with benign breast disease, this effect induces disease regression. In patients at risk for developing breast cancer, the anti-estrogenic effect prevents formation of benign breast conditions that can lead to cancer.
Owner:BESINS HEALTHCARE LUXEMBOURG (LU)

Compounds having antiestrogenic and tissue selective estrogenic properties, and compounds with anti-androgenic properties for treatment of prostate cancer and androgen receptor dependent diseases

Compounds for the treatment of estrogen-receptor related maladies are provided. Compounds with anti-androgenic properties also are provided. In particular, the invention provides compounds that are tetrahydroquinoline phenylamide derivatives and are useful for the treatment of breast and prostate cancer, and osteoporosis.
Owner:VIRGINIA COMMONWEALTH UNIV

Method of treating bipolar disorder or depression using an antiestrogen

InactiveUS20120201908A1Alleviate or prevent one or more symptoms of bipolarBiocideNervous disorderBipolar mood disorderEstrogen
The disclosure provides methods of treating bipolar disorder by administering an antiestrogen to reduce the severity and frequency of mood episodes. The disclosure further provides methods of treating depression with an antiestrogen in a descending dose protocol.
Owner:LUNERA RES

Steroidal antiestrogens and antiandrogens and uses thereof

InactiveUS7041839B2Inhibit transcriptional responseEffective treatmentOrganic active ingredientsSteroidsDiseaseSide effect
The present invention comprises the design, synthesis and development of a new class of chemotherapeutic agents for prophylactic and therapeutic treatments in a mammal, particularly a human, believed to be at risk of suffering from a hormone-responsive disorde. In an embodiment of the invention, such treatments include therapeutic compositions comprising novel steroidal antiestrogen and antiandrogen compounds. In a preferred embodiment, such a novel compound of the present invention has an address and a message component, which are made into a single composite entity for more aggressive intervention and effective treatment of hormone-responsive disorders, thereby prolonging the disease-free interval for the patient and reducing a number of side effects.
Owner:NORTHEASTERN UNIV

Methods and kits for diagnosing tumorigenicity and determining resistance to the antineoplastic effects of antiestrogen therapy

InactiveUS6881548B2Organic active ingredientsVirusesEstrogenAntiestrogen therapy
Methods and kits for diagnosing tumorigenicity and for determining whether a cancer patient is resistant to the pharmacological effects of antiestrogen therapy. Increased levels of the PCDGF (GP88) growth factor are indicative of tumorigenicity and resistance to the pharmacological effects of antiestrogen therapy. The methods and kits of the invention are useful for assessing the tumorigencity of a biological sample from a patient and determining whether the patient is a candidate for antiestrogen, including tamoxifen, therapy.
Owner:A & G PHARMA

Polynucleotides for use in treating and diagnosing cancers

The present invention provides methods for increasing sensitivity of cancer cells to an antiestrogen agent, such as a selective estrogen receptor modulator (SERM). The methods include administering to the subject a polynucleotide in an amount effective to increase the antiestrogen agent sensitivity of the cancer cells. The cancer cells may be estrogen receptor positive, such as ER-α66 positive or ER-α36 positive, prior to the administering. Also provided are methods for decreasing the amount of estrogen receptor present in a cancer cell, methods for determining whether antiestrogen agent sensitivity of cancer cells in a subject can be increased, methods for diagnosing whether a subject has, or is at risk for developing, cancer, and methods for identifying an agent that increases the amount of let-7 miRNA in a cell.
Owner:CREIGHTON UNIVERSITY

Complexes of fulvestrant and its derivatives, process for the preparation thereof and pharmaceutical compositions containing them

The present invention relates to pharmaceutically acceptable complex formulae comprising complexes of Fulvestrant, or a salt, or derivatives thereof and complexation agents and pharmaceutically acceptable excipients, process for the preparation thereof and pharmaceutical compositions containing them. The complex formulae of the present invention have improved physicochemical properties which makes the compound orally available and makes oral administration of the compound possible in the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy.
Owner:DRUGGABILITY TECH IP HOLDCO

Method of treating estrogen responsive breast cancer

InactiveUS20050002900A1Inhibit estradiol productionLower estrogen levelsOrganic active ingredientsPeptide/protein ingredientsTreatment choicesSide effect
The present invention is directed to a method of treating estrogen responsive breast cancer in an individual comprising administering to an individual a therapeutically effective estradiol inhibiting amount of interferon gamma (IFN-γ) and / for a tumor necrosis factor (TNF) antagonist and / or an interleukin-1 (IL-1) antagonists. The invention is based upon the surprising discovery that IFN-γ and / or a tumor necrosis factor (TNF) antagonist and / or an interleukin-1 (IL-1) antagonists inhibit estradiol production in human adipocytes. This discovery is not only important because it allows for the treatment and / or prevention of estrogen dependent breast cancer using IFN-γ, TNF antagonists or IL-1 antagonist each alone or in combination, but also because IFN-γ and / or TNF antagonists and / or IL-1 antagonists can be used in conjunction with standard anti-estrogen therapy, e.g., tamoxifen and / or aromatase inhibitor, to result in lower estrogen levels than seen with standard anti-estrogen therapy alone. Moreover, the ability to lower estrogen levels by means of the present invention, when combined with standard anti-estrogen therapy, provides an important therapeutic option in that it allows the dose of the anti-estrogen to be reduced, reducing the likelihood of side effects and complications commonly seen with anti-estrogen therapy.
Owner:LAB SERONO SA

Fulvestrant compositions

The invention relates to novel formulations of fulvestrant for intramuscular administration. Methods of preparing such fulvestrant formulations are also provided. The present invention further relates to the use of fulvestrant formulation in the treatment of a disease or condition that is or is believed to be responsive to anti-estrogen therapy, such as cancer.
Owner:AHMED SALAH UDDIN +6

Hormonal implants treatment of the breast cancer

An improved method and products for the hormonal treatment of breast cancer by breast implants of anti-estrogens and steroid hormones in formulations as fused with a lipoid carrier or encapsulated in microcapsules or in Silastic capsules is provided. Such breast implants renders a constant slow-release of their contents to the breast tissue for extended periods by biodegradation and diffusion. It facilitates higher breast tissue concentrations of anti-estrogen and hormonal compositions. Because of their high concentration in the breast and lower systemic distribution, tumor control is much improved and the their systemic toxicity is minimized. An added beneficial effect of these breast implants on breast cancer is mediated by the inhibition of hypothalamic-pituitary LHRH, FSH and LH secretion by these composition's systemic contents. It is also an effective prophylaxis against breast cancer. Furthermore, it reduces the cost of hormonal treatment of breast cancer. Anti-estrogen hormonal implants to the breast as concomitant hormonal treatment with conventional radiation therapy also facilitates improved tumor control and cure rates of breast cancer.
Owner:SAHADEVAN VELAYUDHAN

P38 MAPK pathway predicts endocrine-resistant growth of human breast cancer and provides a novel diagnostic and treatment target

Acquired and de novo endocrine resistance are major clinical problems in the management of breast cancer patients. Though the antiestrogen tamoxifen prolongs disease-free and overall survival in the adjuvant setting, and induces remissions in over half of the patients with estrogen receptor positive metastatic disease, all patients eventually acquire tamoxifen resistance. Furthermore, many of the resistant tumors actually appear to be stimulated by tamoxifen just as they are by estrogens. The present invention provides methods of predicting endocrine resistance comprising detecting the biological activity and / or expression of p38 MAPK and / or AIB1. The invention further provides methods of reducing, reversing, or preventing endocrine resistance comprising contacting a breast or prostate tumor with a p38 MAPK pathway inhibitor.
Owner:BAYLOR COLLEGE OF MEDICINE

Method for rapidly evaluating composition effect of estrogen and antiestrogen

The invention relates to a method for rapidly evaluating composition effect of estrogen and antiestrogen. The method comprises the following steps of: obtaining zebrafish embryos; mixing the estrogen with different concentration of antiestrogens to form different ratios of exposure liquid; putting the zebrafish embryos into the exposure liquid to expose for 96 hours lastingly, and maintaining the water temperature at 26+ / -1 DEG C, wherein the photoperiod is 16 hours in daytime and 8 hours at night; exchanging 80% of exposure liquid after 24 hours, and recording the hatching rate, the aberration rate and the hatching time of the zebrafish embryos; collecting juvenile fishes to store for use after exposure is finished; and evaluating the composition effect on morphological level of embryonic development and / or gene transcription level. The method for evaluating the composition effect of estrogen and antiestrogen by the zebrafish embryos is simple, rapid and objective, just needs 96 hours, and is a novel method for rapidly evaluating the composition effect of the estrogen and the antiestrogen.
Owner:SHANGHAI JIAO TONG UNIV

Composition comprising progesterone-receptor antagonists and pure antiestrogens for prophylaxis and treatment of hormone-dependent diseases

InactiveUS20050014736A1Effective treatmentEffectively inhibit the growth of such tumorsOrganic active ingredientsAntineoplastic agentsProgestin AntagonistTherapeutic Hormone
The present invention relates to methods and uses for preventing or treating hormone-dependent diseases, in particular breast cancer, in a mammal, by a combination of an progesterone-receptor antagonist, in particular the progesterone-receptor antagonist 11β-(4-acetylphenyl)-17β-hydroxy-17α-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, and a pure antiestrogen, in particular a compound of general formula I as defined in the specification, for instance 11β-Fluoro-17α-methyl-7α-{5-[methyl(8,8,9,9,9-pentafluorononyl)amino]pentyl}-estra-1,3,5(10)-triene-3,17β-diol. The invention further relates to pharmaceutical compositions comprising said combination.
Owner:BAYER SCHERING PHARMA AG

Letrozole I-type crystal and preparation method thereof

The invention relates to a letrozole I-type crystal and a preparation method thereof, in particular to an anhydrous letrozole crystal. The structure and characteristics of the anhydrous letrozole crystal are represented by X-radial powder diffraction, differential scanning calorimetry, infrared spectrum and the like. Characteristic diffraction peaks, which are positioned at the degrees 2theta of 13.08+ / -0.2, 14.06+ / -0.2, 17.04+ / -0.2, 21.44+ / -0.2 and 29.24+ / -0.2, are positioned in the X-radial powder diffraction pattern of the crystal powder. The anhydrous letrozole crystal is simple in preparation process, the yield and purity of the crystal are high, and the anhydrous letrozole crystal has good stability and is suitable for production of medicinal preparations. The invention also provides a method for preparing the anhydrous letrozole crystal by using an anhydrous and pure organic solvent as a crystallization solvent and application of the crystal in the medicinal preparations which are used for treating advanced breast cancer of a patient after menopause by antiestrogen.
Owner:SHENZHEN NEPTUNUS PHARM CO LTD

Antiestrogenic glyceollins suppress human breast and ovarian carcinoma proliferation and tumorigenesis

InactiveUS20080200537A1Preventing minimizing development growthBiocideAnimal repellantsDiseaseStress induced
The flavonoid family of phytochemicals, particularly those derived from soy, has received attention regarding their hormonal activity and their effects on human health and disease. The types and amounts of these compounds in soy and other plants are controlled by both constitutive expression and stress-induced biosynthesis. The health benefits of soy may therefore be dependent upon the amounts of the various hormonally active phytochemicals present. We have identified increased biosynthesis of the isoflavonoid phytoalexin compounds, Glyceollins I, II and III, in soy plants grown under stressed conditions (elicited soy), which exhibit marked anti-estrogenic effects on ER function. Here we demonstrate that specific glyceollins, isolated from elicited soy, displayed anti-estrogenic activity, suppressing basal and estrogen stimulated colony formation of ER-positive estrogen dependent breast cancer cells and inhibiting ER-dependent gene expression of progesterone receptor (PgR) and stromal derived factor-1 (SDF1 / CXCL12). Examining the effects of glyceollin on in vivo tumor formation / growth we demonstrate the ability of glyceollins to significantly suppress basal and estrogen-stimulated tumor growth of ER-positive MCF-7 breast and BG-1 ovarian carcinoma cells in ovariectomized female nude mice. We further demonstrate that the effects of glyceollins on suppression of tumor growth correlate with inhibition of estrogen stimulated PgR expression. In contrast to the uterotropic activity of tamoxifen the glyceollins displayed no uterine agonist activity. The Glyceollin (I-III) compounds may represent an important component of the health effects of soy as well as represent novel anti-estrogens useful in the prevention or treatment of breast and ovarian carcinoma.
Owner:UNITED STATES OF AMERICA +1

Treatment of male androgen deficiency symptoms or diseases with sex steroid precursor combined with serm

ActiveUS20150250802A1Proper increases in serum testosteroneBiocideOrganic active ingredientsInsulin resistanceGonadal Steroid Hormones
Novel methods for prevention, reduction or elimination of the incidence of male androgen deficiency symptoms or diseases including male hypogonadism-associated symptoms and diseases associated with low serum testosterone and / or low DHEA or low total androgens in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and a selective estrogen receptor modulator (SERM) (particularly acolbifene), an antiestrogen or a prodrug of the two. The symptoms or diseases are loss of libido, erectile dysfunction, tiredness, loss of energy, depression, bone loss, muscle loss, muscle weakness, fat accumulation, memory loss, cognition loss, Alzheimer's disease, dementia, loss of body hair, fertility problems, insomnia, gynecomastia, anemia, hot flushes, sweats, decreased sense of well-being, obesity, osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, cardiovascular disease and type 2 diabetes. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
Owner:ENDORES & DEV
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