153 results about "Aromatase inhibitor" patented technology

The endometriosis treatment protocol provides for administering to a female patient in need of treatment for endometriosis a pharmaceutical composition in a form suitable for vaginal or rectal delivery having a pharmaceutically effective amount of an aromatase inhibitor, which may be either a steroid or non-steroidal. The pharmaceutical composition may be formed as a vaginal suppository, a rectal suppository, a vaginal gel, a rectal gel, a vaginal cream or a rectal cream. The pharmaceutical composition may optionally have pharmaceutically effective amounts of progesterone and calcitriol, and may be administered in combination with an oral COX-2 inhibitor. Alternatively, the pharmaceutical composition comprises an aromatase inhibitor administered vaginally or rectally and is administered in combination with oral calcitriol and the oral COX-2 inhibitor. The aromatase inhibitor is either steroidal or non-steroidal.

The present invention discloses a novel method of prevention of birth defects, miscarriages and infertility in women. The two therapies, disclosed herein, the hormone normalization therapy and the aromatase inhibitor-hormone normalization therapy, focus on restoring young hormonal levels in women in order to prevent female infertility and miscarriages, guide follicular and oocyte maturation, and promote correct chromosomal segregation in oocytes and early embryos.

The present invention relates to a method of treating or preventing musculoskeletal pain in a mammal receiving administration of an estrogen. suppressant selected from the group consisting of aromatase inhibitors, GnRH analogues, cyclo-oxy-genase 2 (COX-2) inhibitors, 17β-hydroxysteroid dehydrogenase type 1 inhibitors, progestogens, anti-estrogens and combinations thereof, said method comprising the administration of an effective amount of an estrogenic component, wherein the estrogenic component is selected from the group consisting of: substances represented by the following formula (1) in which formula R₁, R₂, R₃, R₄ independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors.

This invention relates to combination therapies for the treatment of breast cancer comprising administering to a subject in need thereof a compound of Formula I or a pharmaceutically acceptable salt thereof and an anti-estrogenic agent (e.g., an aromatase inhibitor, a SERM that is not the SERM of Formula I, a GNRH agonist, a GNRH antagonist, or an estrogen receptor downregulator) and to compositions (e.g., pharmaceutical compositions) comprising a compound of Formula I or a pharmaceutically acceptable salt thereof and an anti-estrogenic agent. This invention also relates to a method of treating the side effects (e.g., vasomotor disturbances, osteoporosis and musculoskeletal complaints) associated with anti-estrogen therapy in a subject treated with one or more anti-estrogenic agents (e.g., an aromatase inhibitor, a SERM that is not the SERM of Formula I, a GNRH agonist, a GNRH antagonist or an estrogen receptor downregulator). The method comprises administering to the subject an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof.

PCT No. PCT/GB95/02166 Sec. 371 Date Mar. 14, 1997 Sec. 102(e) Date Mar. 14, 1997 PCT Filed Sep. 13, 1995 PCT Pub. No. WO96/08231 PCT Pub. Date Mar. 21, 1998A method for treating hair loss is disclosed by topically adminstering an aromatase inhibitor to a mammal, including humans, on the area to be treated.

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.

A method for selecting a breast cancer patient for therapy with an agent that reduces production of angiotensin II, for example an ACE inhibitor or renin inhibitor, comprises (a) determining whether the cancer comprises a tumor that is estrogen receptor positive (ER+) and (b) selecting the patient for such therapy only if the cancer is determined to comprise an ER+ tumor. A method for treating breast cancer in a patient further comprises (c) administering to the patient, if so selected, an agent that reduces production of angiotensin II, for example an ACE inhibitor or renin inhibitor. A method for treating a breast tumor in a patient having SERM-resistant ER+ breast cancer comprises administering to the patient an agent that reduces production of angiotensin II, for example an ACE inhibitor or renin inhibitor. A therapeutic combination useful in treatment of a breast tumor comprises an agent that reduces production of angiotensin II, for example an ACE inhibitor or renin inhibitor, and a second agent that comprises (a) an aromatase inhibitor or (b) an estrogen receptor modulator or antagonist.

This invention relates a method of treating hyperproliferative diseases. More particularly, the present invention relates to a method of treating hyperproliferative diseases, such as cancer, comprising the step of administering to a mammal in need of such treatment, either simultaneously or sequentially, (i) a therapeutically effective amount of a taxane derivative, a platinium coordination complex selected from the group consisting of carboplatin, tetraplatin, and topotecan, a nucleoside analog selected from the group consisting of gemcitabine hydrochloride and 5-FU, an anthracycline, a topoisomerase selected from the group consisting of etoposide, teniposide, amsacrine, topotecan, and Camptosar®, an aromatase inhibitor; and (ii) a therapeutically effective amount of an isothiazole derivative. The combinations of the present invention may optionally include an anti-hypertensive agent. This invention also relates to pharmaceutical compositions useful in the treatment of hyperproliferative diseases in mammals, containing such combinations. The present invention also relates to kits having a first compartment with a compound of formula 1 and a second compartment containing a taxane derivative, a platinum coordination complex, a nucleoside analog, an anthracycline, a topoisomerase inhibitor, or an aromatase inhibitor and a third compartment containing an anti-hypertensive agent.

The invention relates to a male trait induction method for pelodiscus sinensis in embryonic periods. The male trait inducer is characterized in that through dissolving an aromatase inhibitor and an adjuvant into alcohol with the purity of 92-98%, the inducer with an aromatase inhibitor concentration of 50-150 mu g/mu l and an adjuvant concentration of 50-150 mu g/mu l is obtained; and the adjuvant is selected from testosterone, methyltestosterone or testosterone propionate. According to the induction method provided by the invention, the male induction rate can be more than 95% just through spraying the inducer two times at the sex determination key time point in embryonic development, and meanwhile, the normal development and low drug residues of pelodiscus sinensis gonads are ensured; and the induction method provided by the invention is easy to operate, low in cost, and remarkable in economic benefit, thereby being a sex control technology which is worthy of popularization in the existing pelodiscus sinensis breeding.

Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I:

wherein R¹ may be alkyl, cycloalkyl, haloalkyl, aryl, substituted aryl, haloaryl, alkoxy, alkylaryl, and arylalkyl; R² is H, alkyl, aryl, alkylaryl, arylalkyl, and cycloalkyl; R³, with the base nitrogen, forms an amide or sulfonamide; R⁴ is selected from nitro, amine, amide, and benzamide; or a pharmaceutically acceptable salts thereof Also provided are small molecule selective aromatase inhibitors having a molecular weight of less 500 g/mol. In some embodiments, the small molecule selective aromatase inhibitors described herein have a molecular weight of less than 450 g/mol. Also provided are methods for suppressing aromatase activity expression in cancer cells comprising the step of administering a pharmaceutically effective amount of a small molecule aromatase inhibitor to a subject in need of such treatment. In one embodiment, the cancer cells are breast cancer cells.

The present invention is directed generally to pharmaceutical compositions, methods, and kits for improving side effects associated with aromatase inhibitor treatment in a subject diagnosed with breast cancer. More specifically, the present invention provides compositions, methods, and kits comprising an aromatase inhibitor and an androgenic agent.

The present invention provides a composition suitable for forming an intramuscular implant. It comprises a biodegradable thermoplastic polymer of polylactic acid (PLA), DMSO and an aromatase inhibitor compound. The invention also provides a kit suitable for the in situ formation of the composition and its use as a medicine for treating cancer, especially breast cancer.

The present invention relates to a composition for increasing testosterone physiological levels comprising: a) a sufficient amount of at least one aromatase inhibitor chosen from a flavone substituted with at least one methoxy group at position 3′,4′,5 or 7, any combinations thereof, and any di, tri or tetra combinations thereof; and a flavanone substituted with at least one methoxy group at position 3′,4′,5 or 7, any combinations thereof, and any di, tri or tetra combinations thereof; and b) a sufficient amount of at least one 5α-reductase inhibitor that inhibit testosterone conversion to DHT, such as beta-sitosterols; in association with a pharmaceutically acceptable carrier.

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.

Disclosed is a safe substance which can inhibit the activity of aromatase (an enzyme capable of converting androgen into estrogen) to thereby effectively treat and/or prevent a sex hormone-dependent disease such as breast cancer occurring in a female person after menopause, as well as a climacteric disorder in a male person and metabolic syndrome caused by the accumulation of a visceral fat. Specifically disclosed is a therapeutic and/or prophylactic agent for a sex hormone-dependent disease, which is characterized by comprising at least one herbal extract selected from the group consisting of “Kokeiten” (golden root), prunella spike, sweet hydrangea leaf, milk thistle, a jasmine tea, “Bokusoku” (a bark of Quercus acutissima or a closely related plant thereof), “Tencha” (sweet tea), “Karensou” (Eclipta prostrata), “Youbaihi” (a bark of Myrica rubra Sie b. et Zucc.), French maritime pine, betel palm, asparagus, “Rouro” (a root of Rhaponticum unifloru m DC. or Echinops latifolius Tausch), “Ryoukyou” (a rhizome of Alpinia officinarum Hance), rooibos tea, rhubarb, pu-erh tea, green tea, “Ougon” (a root of Scutellaria baicalensis Georgi), St. John's wort (Hypericum perforatum L.), licorice, “Senrikou” (Senecio scandens Buch.-Ham.), wintergreen, “Kashi” (a matured fruit of Terminalia chebula Retz.), “Yagotou” (a bark of Mallotus japonicus), polygnum root, barrenwort (Epimedium Herb), guarana, “Ouhi” (a bark of Prunus jamasakura Sieb. ex. Koidz. or a closely related plant thereof), Argy's wormwood, sticky rehmannia, Japanese cornel, Asiasarum root, cinnamon, peony root, pine needle and amla fruit.

The invention provides a sustained release medicine for artificially inducing sex reversal of grouper and its preparation method, wherein the medicine comprises aromatase inhibitor 1.5-15%, synthetic rubber base material for medical purpose 75-90%, hardening agent 8.5-10%, the process for preparing the medicament comprises mixing homogeneously, dry forming, and refrigerated preservation.

The invention relates to administration of an anti-CTLA4 antibody, particularly human antibodies to human CTLA4, such as those having amino acid sequences of antibodies 3.1.1, 4.1.1, 4.8.1, 4.10.2, 4.13.1, 4.14.3, 6.1.1, 11.2.1, 11.6.1, 11.7.1, 12.3.1.1, 12.9.1.1, and 10DI (MDX-010), in combination with an aromatase inhibitor, for treatment of breast cancer. More particularly, the invention relates to administration of an anti-CTLA4 antibody and exemestane for treatment of breast cancer.

The invention relates to aromatase inhibitory activity high-throughput screening realized by means of a homogeneous time-resolved fluorescence technique. By detecting the fluorescence intensity ratio (665nm/610nm) of an excitation light irradiated reaction system and performing formula conversion, the inhibitory activity of a to-be-detected sample on aromatase can be determined. By means of high-throughput screening new model, the harm of a radioligand binding principle-based experimental method to laboratory personnel and environment can be avoided. And the high-throughput screening model provided in the invention has the advantages of high efficiency, rapidity, accuracy, and inexpensiveness.

The invention relates to a method for the treatment of an oestrogen-dependent proliferative disorder of the uterus such as endometriosis and uterine fibroids in a patient, by administering an aromatase inhibitor to the patient intravaginally. This achieves high local levels of aromatase inhibitor Locally, and therefore avoids some of the adverse reactions that are observed when aromatase inhibitors are delivered orally. Further, intravaginal delivery allows inhibition of the local lesional production without significantly affecting the circulating levels which have been produced by the ovaries. This results in minimal side-effects and will allow for longer term treatment than current therapies.

The invention relates to applications of combined CDK4/6 inhibitor and aromatase inhibitor in preparing medicines for treating breast cancer. Specifically, the CDK4/6 inhibitor is a compound A or medicinal salt of the compound A, and the aromatase inhibitor is selected from one or more of formestane, exemestane, fadrozole, letrozole, vorozole and anastrozole.

Methods using the application of the Ca isotope method for diagnosing and monitoring the progression of cancers that cause bone loss. The methods also can be used for evaluating cancer treatments, such as aromatase inhibitors and other chemotherapeutic agents, for effects on bone density so that treatment can be modified.

Aromatase inhibitors (AIs) are disclosed which are useful in the treatment and prevention of post-menopausal breast cancer. New AIs derived from natural products are disclosed that are evaluated for clinical utility for treating post-menopausal breast cancer and may also act as chemopreventive agents for preventing breast cancer. Several pure compounds demonstrated AI activity using a noncellular, enzyme-based microsomal and a cell-based aromatase assay. Correlations are made between structural classes with levels of aromatase inhibition. The disclosure may be utilized to direct synthetic modification of natural product scaffolds to enhance aromatase inhibition or to standardize botanical dietary supplements for increased aromatase inhibition activity.