Abstract: Non-aqueous, ethanol-free taxane formulations are provided. Formulations of embodiments of the invention include a taxane, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid component, wherein the organic acid component is soluble in the non-aqueous solvent and the amount by weight of non-ionic surfactant is equal to or greater than the amount by weight of non-aqueous solvent. Also provided are methods of using the formulations, as well as kits that include the formulations. Non-aqueous, ethanol-free docetaxel formulations are provided. Formulations of embodiments of the invention include docetaxel, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid which is soluble in the non-aqueous solvent and is substantially free of any conjugate base. Also provided are methods of using the formulations, as well as kits that include the formulations.

Abstract: Methods for the treatment of systemic disorders treatable with mast cell stabilizers, including mast cell related disorders, are provided. Some embodiments relate to dosage forms. Dosage forms can include an aqueous pharmaceutical composition containing (i) from about 2% to about 6% by weight of cromolyn sodium, and (ii) an osmolarity adjusting agent consisting of (A) between about 0.1% to about 0.5% by weight of sodium chloride, inclusive of the endpoints, and (B) optionally salts of EDTA; and an inhalation device that forms an aerosol of said pharmaceutical composition, said aerosol exhibiting a respirable fraction of said pharmaceutical composition (<5 ?m) as measured by USP <1601> of at least about 60%, are provided.

Abstract: A liquid composition which includes a taxane-based active ingredient (a) selected from the group consisting of docetaxel and a derivative thereof; at least one glycol (b); and at least one surfactant component (c) selected from the group consisting of a polysorbate, a polyoxyethylene glycol ester, and a polyoxyethylene castor oil derivative, in which a volume ratio of the glycol (b) to the surfactant component (c) is in a range of form 45/55 to 55/45, and a total content of the glycol (b) and the surfactant component (c) with respect to a total volume of the liquid composition is 95% (v/v) or more.

Abstract: The invention provides new cabazitaxel isoserine ester intermediates and new synthetic methods, and a preparation method for the anti-tumour drugs cabazitaxel, docetaxel and paclitaxel from the new cabazitaxel isoserine intermediates.

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.

Abstract: Disclosed is a method of crystallizing docetaxel comprising combining docetaxel and at least one solubilizing solvent to obtain a solution, wherein the solubilizing solvent is methylene chloride and adding an anti-solvent to the solution to obtain a crystalline docetaxel, wherein the anti-solvent is water.

Abstract: Compositions and methods for the treatment of cancer are provided.

Abstract: The present disclosure generally relates to lyophilized pharmaceutical compositions comprising a sugar, a cyclodextrin, and polymeric nanoparticles comprising a copolymer and a therapeutic agent which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles.

Abstract: The present invention relates to compositions and methods to modulate ?-secretase and/or to improve cognitive ability. The invention further relates the improved/enhanced cognitive ability in diseased individuals, particularly Alzheimer's Disease patients, and treatment thereof through increased sAPP production. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are compounds preferred for use with the present composition. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP comprising the activation of protein kinase C (PKC) by administering an effective amount of PKC activator(s).

Abstract: The present invention provides methods and compositions for treating non-small-cell lung cancer (NSCLC) by administering a) a composition comprising nanoparticles that comprise paclitaxel and an albumin and b) a platinum-based agent (e.g., carboplatin). The present application also provides methods of treating prostate cancer by administering to the individual a) an effective amount of a composition comprising nanoparticles comprising docetaxel and an albumin; and b) an effective amount of a steroid.

Abstract: A liquid composition of an insoluble medicament and a preparation method thereof are disclosed. The composition includes insoluble medicament, oil for injection, phospholipid, and solvent; the percentage by weight of each component is as follows: insoluble medicament 0.01-10%, oil for injection 0%-20%, phospholipid 10-80%, solvent 20-89%. The preparation method for the composition includes the following steps: dissolving an insoluble medicament into solvent or oil for injection or a mixture thereof firstly, and then adding other components, and mixing uniformly; or dissolving an insoluble medicament into a mixture of other components, and mixing uniformly; or dissolving an insoluble medicament into part of solvent firstly, and then adding into a mixed solvent of other components and the remaining solvent, and mixing uniformly.

Abstract: An object of the invention is to provide a transdermal absorption preparation capable of sustaining the blood morphine concentration at an effective level over at least 48 hours, etc.

Abstract: The invention relates to topical formulations of flucytosine which demonstrate a clear advantage over currently available therapeutic regimens for the treatment and maintenance of fungal infections, particularly vulvovaginal candidiasis. The invention provides compositions which solve the long-standing need for antimicrobial agents which treat effectively resistant strains of Candida spp., especially C. albicans, C. glabrata, and C. tropicalis, and which pose limited risk of side effects, adverse reactions, or the development of resistant pathogens. The invention provides novel topical formulations of flucytosine designed to allow the active drug to act at the local application area, but which inhibit or moderate transdermal or transmucosal absorption of the drug, thus limiting systemic exposure.

Abstract: Non-aqueous, ethanol-free taxane formulations are provided. Formulations of embodiments of the invention include a taxane, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid component, wherein the organic acid component is soluble in the non-aqueous solvent and the amount by weight of non-ionic surfactant is equal to or greater than the amount by weight of non-aqueous solvent. Also provided are methods of using the formulations, as well as kits that include the formulations. Non-aqueous, ethanol-free docetaxel formulations are provided. Formulations of embodiments of the invention include docetaxel, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid which is soluble in the non-aqueous solvent and is substantially free of any conjugate base. Also provided are methods of using the formulations, as well as kits that include the formulations.

Abstract: Disclosed are methods of treating a chemotherapy-resistant cancer, of treating a cholangiocarcinoma, of treating a metastatic carcinoma, and of treating a transition cell urothelial carcinoma by administering a therapeutically effective amount of an endothelin B (ETB) receptor agonist and a chemotherapeutic agent to a subject afflicted with such a cancer.

Abstract: Disclosed is a method of crystallizing a taxane comprising combining the taxane and methylene chloride to obtain a solution and adding an anti-solvent to the solution to obtain a crystalline taxane, wherein the anti-solvent is selected from the group consisting of hexane and heptane.

Abstract: The invention relates to a coated medical device for rapid delivery of a therapeutic agent to a tissue in seconds to minutes. The medical device has a layer overlying the exterior surface of the medical device. The layer contains a therapeutic agent, at least one of an oil, a fatty acid, and a lipid, and an additive. In certain embodiments, the additive has a hydrophilic part and a drug affinity part, wherein the drug affinity part is at least one of a hydrophobic part, a part that has an affinity to the therapeutic agent by hydrogen bonding, a part that has an affinity to the therapeutic agent by charge, and a part that has an affinity to the therapeutic agent by van der Waals interactions. In embodiments, the additive is at least one of a surfactant and a chemical compound. In further embodiments, the chemical compound is water-soluble.

Abstract: Provided herein are methods and compositions, including pharmaceutical compositions, for treating thrombosis, vascular inflammation, and thrombocytopenia. The methods and compositions of the present invention are also useful for extending the useful storage shelf life of platelets.

Abstract: According to an aspect of the present invention, medical devices are provided which comprise: (a) a substrate and (b) bioerodable polymeric layer over the substrate that contains (i) one or more biodegradable polymers, (ii) one or more therapeutic agents, and (iii) one or more plasticizers.

Abstract: A pharmaceutical solution of taxanes, its preparation method, a composition comprising said solution and its pharmaceutical combination package are disclosed. Said pharmaceutical solution comprises taxanes, a pH regulator and a solvent, wherein the pH regulator is a water-soluble acid.

Abstract: The present invention relates to the use of pharmaceutical preparations comprising paclitaxel for administration to a human patient in need thereof.

Abstract: The present invention relates to a combination of (i) a statin, and (ii) a taxane, for simultaneous or sequential use in the treatment of a patient suffering from solid tumor, e.g. a gastric cancer. The present invention also provides a statin, for use in a method for enhancing sensitivity of a patient suffering from a solid tumor to a taxane.

Abstract: The invention relates to (among other things) non-ring hydroxy substituted taxanes and methods for synthesizing the same. The invention further relates to conjugating the non-ring hydroxyl substituted taxanes to a water-soluble, non-peptidic polymer.

Abstract: The present invention relates to a stable liquid cabazitaxel formulation in an enclosed container. The enclosed container comprises a liquid phase and an gaseous phase, wherein the liquid phase comprises cabazitaxel, polysorbate 80, ethanol, and one or more pH adjusters to maintain pH about 2.8-6.0, and the gaseous phase is saturated with CO2. The present invention is also directed to a process for preparing the enclosed liquid pharmaceutical composition container.

Abstract: The invention is directed to a probe-type imaging device useful to visualize interior surfaces, e.g., the lumen of blood vessels. Specifically, the probe-type device is particularly useful for direct tissue imaging in the presence or absence of molecular imaging agents.

Abstract: The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.

Abstract: The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

Abstract: The present invention features a method for the treatment of Hepatitis C in a human in need thereof comprising administering a compound of Formulas (II) or (IIB) described herein or a pharmaceutically acceptable salt thereof in combination with one or more alternative Hepatitis C therapeutic agents.

Abstract: Pharmaceutical compositions and methods for the treatment of neoplastic disease and comprising the combination of a taxane, such as docetaxel, with a CYP3A4 inhibitor, such as ritonavir. Methods of treatment of neoplastic disease incorporating the administration of a taxane and the administration of a CYP3A4 inhibitor, either simultaneously or separately, are also included. Further, kits for carrying out the methods are included. Solid pharmaceutical taxane compositions for oral administration comprising a substantially amorphous taxane, a carrier and a surfactant are also included.

Abstract: An article comprising a polyelectrolyte complex comprising an interpenetrating network of at least one predominantly positively charged polyelectrolyte polymer and at least one predominantly negatively charged polyelectrolyte polymer, the polyelectrolyte complex further comprising a plurality of closed-shell pores, the plurality of pores having at least one average transverse dimension between about 100 nanometer and about 1000 micrometers.

Abstract: The invention provides methods for predicting or determining the response of a mammalian tumor to a chemotherapeutic agent and for treating a mammalian tumor comprising detecting and quantifying the SPARC protein or RNA in a sample isolated from the mammal. The invention further provides kit for predicting the response of a mammalian tumor to a chemotherapeutic agent, comprising a means for the isolation of protein or RNA from the tumor, a SPARC protein or RNA detection and quantification means, control RNAs, and rules for predicting the response of the tumor based on the level of SPARC protein or RNA in tumor.

Abstract: The present invention relates to the BAD pathway's influence on development, progression, chemo-sensitivity, and overall survival for multiple human cancers and its potential as a therapeutic target to increase chemo-sensitivity. BAD pathway expression was associated with the development and/or progression of breast, colon, and endometrial cancers, relapse-free survival from breast cancer, and overall survival from ovarian, colon, and brain cancers. Expression was also associated with in vitro sensitivity to a range of cytotoxic agents. pBAD levels were higher in cancer versus immortalized normal cells and chemo-resistant versus—sensitive cancer cells and associated with increased cell proliferation.

Abstract: Compositions, methods of making, and methods of using nanoclusters in which the nanoclusters comprise a plurality of nanoparticles having a core of nanoparticles arranged such that the surfaces of the nanoparticles contact adjacent nanoparticles, the nanoparticles comprise an active ingredient, and the nanocluster has a mass median aerodynamic diameter of from about 0.25 ?m to about 20 ?m.

Abstract: Embodiments of the invention include drug delivery coatings and devices including the same. In an embodiment, the invention includes a drug delivery coating including a polymeric layer. The polymeric layer can include a hydrophilic outer surface. The coating can also include a matrix contacting the hydrophilic outer surface. The matrix can include a particulate hydrophobic therapeutic agent and a cationic agent. The polymeric layer can further include a hydrophilic polymer having pendent photoreactive groups and a photo-crosslinker including two aryl ketone functionalities. Other embodiments are also included herein.

Abstract: The present invention relates to the field of pharmacology and medicine, specifically to a new generation of anticancer drugs with the cytostatic action based on docetaxel. In the drug composition of the invention docetaxel is included in biodigestible stable nanoparticles. The nanoparticles comprise of docetaxel, PLGA, serum albumin and D-mannitol The developed drug is proposed to be manufactured as enterosoluble tablets, capsules granules, powder, or in any other peroral form.

Abstract: The present invention relates to: a pharmaceutical composition or a Nurr1 activating composition for the prevention or treatment of a neurodegenerative disease or a disease induced by impaired Nurr1 function, wherein the composition comprises an active ingredient in the form of genkwanin N or yuanhuacine, a Daphne genkwa extract comprising one or more of the above compounds, or a fraction thereof; or a functional food additive for preventing or alleviating a neurodegenerative disease or a disease induced by impaired Nurr1 function, wherein the additive comprises genkwanin N or yuanhuacine, a Daphne genkwa extract comprising one or more of the above compounds, or a fraction thereof; and a method for the prevention or treatment of a neurodegenerative disease or a disease induced by impaired Nurr1 function, wherein the method comprises the step of administering the pharmaceutical composition.

Abstract: Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies.

Abstract: Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G? or Formula M?: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.

Abstract: The present invention includes drug-loaded, polymer nanoparticles and liposomes further incorporating a non-paramagnetic, bioorganic CEST agent. The CEST agent allows for an alternative approach to accomplish MR-compatible in vivo tracking of drug-loaded polymer nanoparticles and liposomes, including simultaneous multi-color mapping of more than one particle type, or of the same particle type delivered via two different routes (e.g., systemic versus local). Additionally, the present invention can include a library of biodegradable diamagnetic (DIA)CEST agents. These DIACEST agents can be incorporated into nanoparticle-based delivery systems, such as stealth liposomes loaded with doxorubicin and stealth polymer nanoparticles loaded with paclitaxel. These systems can be tracked, according to an embodiment of the present invention using CEST-based MRI (compared to SPECT/CT) as a method to monitor the efficiency with which the nanoparticles reach the targeted tumors and how long they persist.

Abstract: A liquid composition which includes a taxane-based active ingredient (a) selected from the group consisting of docetaxel and a derivative thereof; at least one glycol (b); and at least one surfactant component (c) selected from the group consisting of a polysorbate, a polyoxyethylene glycol ester, and a polyoxyethylene castor oil derivative, in which a volume ratio of the glycol (b) to the surfactant component (c) is in a range of form 45/55 to 55/45, and a total content of the glycol (b) and the surfactant component (c) with respect to a total volume of the liquid composition is 95% (v/v) or more.

Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R4, R5, X1, X2, X3 and X4 are as defined herein, and wherein the compound comprises at least one F, Cl, Br, I or 123I moiety, are provided. Uses of such compounds for imaging diagnostics in cancer and therapeutics methods for treatment of subjects in need thereof, including prostate cancer as well as methods and intermediates for preparing such compounds are also provided.

Abstract: The present invention relates to methods for treating pancreatitis and/or organ failure comprising administering, to a subject in need of such treatment, an effective amount of a lipase inhibitor. It is based, at least in part, on the discoveries that lipotoxicity contributes to inflammation, multisystem organ failure, necrotic pancreatic acinar cell death and in acute pancreatitis, and that inhibition of lipolysis was able to reduce indices associated with these conditions. Accordingly, in various embodiments, the present invention provides for methods and compositions for limiting lipotoxicity and thereby reducing the likelihood of poor outcomes associated with acute pancreatitis and other severe systemic conditions, especially in obese individuals.

Abstract: Medical device are provided for delivering a therapeutic agent to a tissue. The medical device has a layer overlying the exterior surface of the medical device. The layer contains a therapeutic agent and an additive. In certain embodiments, the additive has a hydrophilic part and a drug affinity part, wherein the drug affinity part is at least one of a hydrophobic part, a part that has an affinity to the therapeutic agent by hydrogen bonding, and a part that has an affinity to the therapeutic agent by van der Waals interactions. In embodiments, the additive is water-soluble. In further embodiments, the additive is at least one of a surfactant and a chemical compound, and the chemical compound has a molecular weight of from 80 to 750 or has more than four hydroxyl groups.

Abstract: Methods for maintaining patency in a bronchus of a patient are presented. A catheter is positioned within the bronchus. A target region of one or more of a bronchial wall, submucosa, media, and adventitia is punctured at or adjacent a location of a debulked bronchial carcinoma with an injection needle disposed on a distal end of the catheter. Such puncturing is achieved by expanding a balloon disposed on the distal end of the catheter. The balloon is comprised of at least two materials of different elastic modulus, which allows for a flexible but relatively non-distensible, unfolding component of the balloon as well as an elastomeric, inflatable component of the balloon. Through the injection needle, an amount of cytotoxic, cytostatic, or anti-neoplastic agent is delivered to the target region. The delivered amount is effective to limit by a therapeutically beneficial amount recurrent bronchial occlusion due to recurrence of the bronchial carcinoma.

Abstract: The invention relates to a compound of formula: which may be in base form or in the form of a hydrate or a solvate, in combination with prednisone or prednisolone, for its use as a medicament in the treatment of prostate cancer, particularly metastatic prostate cancer, especially for patients who are not catered for by a taxane-based treatment.

Abstract: Brain-penetrating polymeric nanoparticles that can be loaded with drugs and are optimized for intracranial convection-enhanced delivery (CED) have been developed. In the preferred embodiment, these are loaded with FDA-approved compounds, identified through library screening to target brain cancer stem cells (BSCSs). The particles are formed by emulsifying a polymer-drug solution, then removing solvent and centrifuging at a first force to remove the larger particles, then collecting the smaller particles using a second higher force to sediment the smaller particles having a diameter of less than 100 nm, more preferably less than 90 nanometers average diameter, able to penetrate brain interstitial spaces.

Abstract: The present invention provides a method of treating cancer using benzoic acid derivatives, alone or in combination with standard treatments such as chemotherapy and radiotherapy. Also provided are methods of screening for benzoic derivatives based on their ability to inhibit the enzyme tyrosinase or to bind to and activate PXR/SXR xenobiotic receptors.

Abstract: The present invention provides a pharmaceutical composition for delivering an active agent taxane through transmucosal administration, more particularly through the buccal mucosa or sublingual mucosa. The present invention provides a method for treating cancer by buccal or sublingual administration of the pharmaceutical composition to a subject. The pharmaceutical composition comprises a taxane, a non-ionic surfactant, a viscosity enhancing agent, an adhesive agent, and an alcohol solvent at pH 4-6.

Abstract: The disclosure provides a recipe for in-situ gel, formed by dissolving at least one polymer and at least one gel prevention agent in a polar solvent to form a solution and placing the solution in a condition for in-situ forming gels. The disclosure also provides an implant and a drug delivery system formed by the recipe.

Abstract: Numerous diseases have been linked to the production of effector cells. The present invention relates to the realization that effector cells are cycling in these diseases. In addition, the present invention relates to the determination that regulator cells are cycling in degenerative diseases. Based on these realizations, the present invention provides methods for treating conditions such as autoimmune diseases, degenerative diseases, and graft-versus-host disease. The present invention also relates to methods of determining when therapy should be administered to a patient.