Abstract: Provided is a teverelix-TFA composition having a molar ratio of teverelix to trifluoroacetate composition of at least 1:2.2. Such a molar ratio will prevent undesirable gel-formation and provide a homogenous suspension, whereby a unique bioavailablity of teverelix is obtained.

Abstract: This invention relates to a bioerodible drug delivery device that can be implanted in a patient at or near an area in need of treatment. The bioerodible drug delivery device can be used to deliver a wide variety of different pharmaceutically active agents, and can do so at a controlled rate and over an extended period of time. The bioerodible drug delivery device includes a bioerodible polymeric outer housing with one or more delivery ports for delivering the pharmaceutically active agent(s) contained therein. The polymer used as the bioerodible polymeric outer housing is not substantially degraded during the dosing of the pharmaceutically active agent(s) in the bioerodible drug delivery device. The invention also provides methods of making the bioerodible drug delivery device and using it for the treatment of diseases and disorders.

Abstract: A veterinary pharmaceutical composition, including at least one active veterinary pharmaceutical substance which is selected among gonadorelin and gonadorelin analogs as well as salts of gonadorelin and of the gonadorelin analogs, is provided. The composition includes a liposome-free matrix which delays the release of the active veterinary pharmaceutical substance from the composition, which matrix includes a basic material which is selected from the group consisting of natural and synthetic triglycerides, vegetable oils, diacylpropanediols, diacylbutanediols and mixtures of these substances, the veterinary pharmaceutical composition including no biodegradable polymer.

Abstract: LHRH analogues and LHRH antagonists for use in the treatment or prophylaxis of hormone-dependent cancers, in particular prostate cancer, prostate carcinoma and/or advanced prostate carcinoma, by administering an initial dose of an LHRH analogue over a first period sufficient to effect hormonal castration, then administering a maintenance dose of an LHRH antagonist over a second period, the dose being insufficient to achieve and/or maintain hormonal castration.

Abstract: A method of treating or preventing an ovary-related syndrome associated with infertility in a subject in need thereof is provided. The method comprising administering to the subject a pharmaceutical composition comprising an active ingredient consisting of pigment epithelium-derived factor (PEDF) and a pharmaceutically acceptable carrier, thereby treating or preventing the ovary-related syndrome associated with infertility in the subject.

Abstract: A method for recognizing and evaluating the presence and function of GnRH receptors on tumor cells including those originating in the brain and/or nervous system and/or the meninges and/or reactive neuroglia cells and/or primitive neuroectodermal tumor cells and/or on Kaposi sarcoma is provided. Furthermore, a method for reducing degenerate GnRH-positive tumor cells and/or for decreasing cellular replication of the above GnRH-positive tumor cells comprising administering to a cell or to a subject a replication decreasing amount of a GnRH agonist and/or GnRH antagonist and/or an erythropoietin agonist, and/or a thrombopoietin agonist, and/or a endothelin antagonist and/or a gonadotropin inhibiting hormone agonist is also provided. Furthermore, a diagnostic kit for detecting GnRH receptors on tumor cells according to the present methods is disclosed.

Abstract: The present invention relates to pharmaceutical compositions for the controlled and sustained release of active substance comprising a biodegradable polymer or copolymer. Furthermore, the invention relates to pharmaceutical compositions for the controlled and sustained release of at least one active substance such as peptides or hormones and analogs thereof and the manufacturing process of such pharmaceutical compositions.

Abstract: The present invention relates to pharmaceutical compositions for the controlled and sustained release of active substance comprising a biodegradable polymer or copolymer. Furthermore, the invention relates to pharmaceutical compositions for the controlled and sustained release of at least one active substance such as peptides or hormones and analogues thereof and the manufacturing process of such pharmaceutical compositions.

Abstract: LHRH analogs and LHRH antagonists for use in the treatment or prophylaxis of hormone-dependent cancers, in particular prostate cancer, prostate carcinoma and/or advanced prostate carcinoma, by administering an initial dose of an LHRH analog over a first period sufficient to effect hormonal castration, then administering a maintenance dose of an LHRH antagonist over a second period, the dose being insufficient to achieve and/or maintain hormonal castration.

Abstract: Sustained release triptorelin microspheres include triptorelin or a salt of triptorelin, a copolymer of lactide and glycolide, and glucose or mannitol. The sustained release triptorelin microspheres have a relatively high initial release after administration, which allows the drug to produce its pharmaceutical effects immediately and to maintain long-term steady pharmaceutical effects.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

Abstract: The invention provides methods and dosing regimens for eating metastatic stage prostate cancer in a subject using degarelix, as well as related methods of using degarelix in a subject identified as having metastatic stage prostate cancer, and methods of using degarelix to prevent or delay the progression of locally advanced prostate cancer.

Abstract: The present invention is directed to the controlled delivery of gonadotropin-releasing hormone (GnRH) agonists, preferably from a polymeric material that is implanted in the body. More specifically, the present invention relates to compositions comprised of a GnRH agonist, preferably histrelin, in a polymeric material that results in a desired and controlled delivery of a therapeutically effective amount of GnRH agonist over an extended period of time in order to treat central precocious puberty (CPP).

Abstract: Polymeric devices for controlled release of an active agent of interest are provided. The active agent is provided within a biodegradable polymer system to supply a polymeric device for controlled release of the active agent. The polymer system is a copolymer or a polymer blend comprising a hydrophobic component and a hydrophilic component, and the polymer system does not form a hydrogel when contacted with, or immersed in an aqueous system, for example when the device is implanted in a subject. When the device is administered to a subject, for example, when it is implanted, the device releases the active agent in a controlled fashion without a lag period, or with a minimal lag period. Methods for producing the polymeric devices are also provided, as are methods of using the polymeric devices to provide for controlled release of an active agent in a subject.

Abstract: A new microsphere formulation (composition) for controlled- or sustained-release delivery of therapeutic ingredient(s), mainly peptides and proteins not over 10K in molecular weight, comprises at least a therapeutic ingredient, a helping agent (such as PH sensitive agent whose solubility is a function of pH) and a biodegradable polymer. The therapeutic ingredient(s) and the helping agent are in the form of fine particles, less than 1O um in diameter, encapsulated in the polymer which forms the microsphere matrix. A method for preparing the composition comprises a step of in-situ precipitating the therapeutic ingredient(s) and the helping agent to the fine particles and successive steps for forming the microspheres. Such a microsphere formulation offers a well-controlled release profile for prolonged period and encapsulation efficiency over 95%.

Abstract: The invention relates to fusion constructs, methods of using fusion constructs and methods of treating undesirable or aberrant cell proliferation or hyperproliferative disorders, such as tumors, cancers, neoplasia and malignancies.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

Abstract: Antagonistic peptides of GnRH having improved water solubility are disclosed. These peptides are capable of suppressing serum testosterone levels in vivo to chemical castration levels of ?0.5 ng/ml. Stable, filter sterilizable, non-gelling solutions containing the GnRH antagonists at least at levels typically used in sustained release formulations also are disclosed, as is a method of increasing the solubility of GnRH antagonist in a polymer containing dispersed phase, which method comprises addition of an acid to the dispersed phase.

Abstract: The present invention relates to pharmaceutical compositions for the controlled and sustained release of active substance comprising a biodegradable polymer or copolymer. Furthermore, the invention relates to pharmaceutical compositions for the controlled and sustained release of at least one active substance such as peptides or hormones and analogues thereof and the manufacturing process of such pharmaceutical compositions.

Abstract: The present disclosure is directed to compositions and kits comprising degarelix or a pharmaceutically acceptable salt thereof for the treatment of benign prostate hyperplasia (BPH), methods for treating BPH, and methods for preparing compositions of degarelix or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to the controlled delivery of gonadotropin-releasing hormone (GnRH) agonists, preferably from a polymeric material that is implanted in the body. More specifically, the present invention relates to compositions comprised of a GnRH agonist, preferably histrelin, in a polymeric material that results in a desired and controlled delivery of a therapeutically effective amount of GnRH agonist over an extended period of time in order to treat central precocious puberty (CPP).

Abstract: A method of therapeutic management of infertility by programming of controlled ovarian stimulation and assisted reproductive procedures is disclosed containing the steps of a) suppression of premature ovulation with an LHRH-antagonist in controlled ovarian stimulation and assisted reproductive techniques with multiple follicle and oocyte development; b) programming the start of controlled ovarian stimulation by the administration to a patient of progestogen only-preparations or, alternatively, combined oral contraceptive preparations; c) exogenous stimulation of the ovarian follicle growth; d) ovulation induction with HCG, native LHRH, LHRH-agonists or recombinant LH; and e) application of assisted reproduction techniques, especially of IVF, ICSI, GIFT, ZIFT or by intrauterine insemination by sperm injection, wherein onset of the patient's menstrual cycle and of controlled ovarian stimulation are programmed in order to perform oocyte pickup and fertilization procedures during Mondays to Fridays.

Abstract: A method of treating or preventing neurodegenerative disease in a subject, the method includes administering to the subject a therapeutically effective amount of at least one physiologically acceptable agent that modulates levels, production, and/or function of brain-derived hormones of the hypothalamic-pituitary-gonadal (HPG) axis or their receptors.

Abstract: Methods and compositions for synchronizing the time of insemination in swine are described. More particularly, methods are described for synchronizing the time of insemination by administration of a composition comprising a hormone, wherein the swine is inseminated only one time after administration of the hormone, and wherein there is no heat detection.

Abstract: A method of treatment and/or prevention of cancer comprises administering agents which cause increased intracellular granularity in cancer cells, at least in an amount sufficient to inhibit proliferation of such cells and preferably in an amount sufficient to lead to cancer cell death. The method is particularly directed to refractory cancer, particularly hormone refractory prostate cancer. The agents identified cause increased intracellular granularity in the cancer cells, and also convert adherent cancer cells to non-adherent cancer cells, leading to cancer cell death. Using the present invention, cancer cells undergo increased intracellular granularity at relatively low agent concentrations, while also inhibiting cell proliferation. Increased concentrations lead to conversion of adherent cancer cells to non-adherent cancer cells, then to cell death.

Abstract: The present invention relates to a method for preparing a sustained-release microsphere which can control the long-term release of a drug. More particularly, as the preparation of a microsphere in which a drug is loaded in a carrier comprising a biodegradable polymer, the present invention relates to a method for preparing a sustained-release microsphere wherein a solvent intra-exchange evaporation method by means of co-solvent is used for suppressing the initial burst release of physiologically active substance, to release the physiologically active substance in the body continuously and uniformly.

Abstract: A sustained release apparatus including at least one sustained release mini-implant or pellet; the or each mini-implant or pellet including: a sustained release support material; and a pharmaceutical composition including a Luteinising Hormone Releasing Hormone (HLRH) agonist and/or antagonist component the size and/or number and/or payload of mini-implant(s) or pellet(s) providing, release of LHRH agonist and/or antagonist at, or above, a desired threshold level for treatment of a selected indication, the apparatus providing approximately zero order release of the LHRH agonist and/or antagonist.

Abstract: A method for treatment of benign prostate hyperplasia, prostate cancer, estrogen-dependent breast cancer, endometrial cancer, ovarian cancer, endometriosis and precocious puberty, or for use for contraceptive purposes or in an in vitro fertilization programme, or for treatment of sex offenders is provided. The method comprises the administration by subcutaneous or intramuscular injection of a therapeutically effective amount of an injectable pharmaceutical composition comprising a solution of a GnRH antagonist peptide according to general formula 1 or a pharmaceutically acceptable salt thereof in a concentration of 0.3-120 mg/ml. Also a pharmaceutical composition and a pharmaceutical kit of parts are provided.

Abstract: The invention relates to a fluid, milky microcrystalline aqueous suspension of a peptide or peptidomimetic and a counter-ion of a strong proton donor in water, wherein the peptide or peptidomimetic and counter-ion are present in amounts and at a molar ratio sufficient to form the suspension upon mixing and without formation of a gel. The invention also relates to lyophilized compositions that include a dried suspension, methods of making the lyophilized composition, methods of preparing the suspension, and sustained release formulations prepared by the methods.