Abstract: Methods are provided for selecting a new therapeutic indication for at least one first pharmaceutical comprising the steps of: generating a drug-side effect (SE) association for said at least one first pharmaceutical; generating a disease-side effect (SE) association for at least one disease or disorder and at least one second pharmaceutical intended for treatment of said at least one disease or disorder; determining an association strength between the drug-side effect (SE) association and the disease-side effect (SE) association; selecting said at least one disease or disorder as a new therapeutic indication for said at least one first pharmaceutical if said at least one first pharmaceutical induces at least one side effect which is the same as at least one side effect induced by at least one second pharmaceutical intended for treatment of said at least one disease or disorder.

Abstract: Disclosed herein are crystalline compounds of formula (I) wherein A+ represents a hydroxylated aliphatic ammonium species; and X and Y independently represent leaving groups.

Abstract: Extracellular vesicle-associated protein biomarkers for use in diagnosing and staging carcinomas, e.g., lung and ovarian cancers.

Abstract: The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.

Abstract: A drug delivery system (DDS) for administration of a water soluble, cationic, and amphiphilic pharmaceutically active substance (API) which DDS comprises poorly water soluble nanoparticles formed by the API together with a Na-salt of N-all-trans-retinoyl cysteic acid methyl ester and/or a Na-salt of N-13-cis-retinoyl cysteic acid methyl ester. A pharmaceutical composition comprising such a DDS. Methods for preparation of such a DDS and such a pharmaceutical composition. Use of such a DDS and pharmaceutical composition for treatment of cancer.

Abstract: The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: Methods of identifying a subject having an increased risk of developing anthracycline-related cardiotoxicity are provided. Such methods may include isolating a DNA sample from a biological specimen from the subject; genotyping the DNA sample to determine a copy number of a variant allele that increases the risk of developing chemotherapy-induced cardiotoxicity; and identifying the subject as having an increased risk of developing anthracycline-related cardiotoxicity when the copy number is at least one. In some embodiments, the methods may include optimally administering a therapeutically effective dose of a chemotherapy agent or an alternative non-cardiotoxic chemotherapeutic agent to the subject.

Abstract: A liquid embolic material may include a mixture of a first solution comprising between about 1.2% and about 2.5% weight per volume (w/v) carboxymethyl chitosan (CCN) in a first solvent and a second solution comprising between about 1.2% and about 2.5% w/v oxidized carboxymethyl cellulose (OCMC) in a second solvent. The liquid embolic material may be used to embolize a targeted embolization location by mixing the first solution and the second solution to form a liquid embolic material (or hydrogel precursor material), introducing the hydrogel precursor material to a targeted embolization location within a body of a patient, and allowing the CCN and the OCMC to react to form the hydrogel material and embolize the targeted embolization location.

Abstract: Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.

Abstract: There is provided a new use of microspheres comprising a water-insoluble, water-swellable polymer which is anionically charged at pH7, and electrostatically associated with the polymer, in releasable form, a cationically charged chemotherapeutic agent, in the manufacture of a composition for use in the treatment of a brain tumour, wherein in the treatment the composition is introduced into the brain and the chemotherapeutic agent is released from the microspheres, wherein the microspheres, when equilibrated in water at 37° C., comprise at least 40 wt % water based on weight of polymer plus water. Compositions comprising the microspheres and methods for the treatment of brain tumours are also provided.

Abstract: The present invention provides amphiphilic telodendrimers that aggregate to form nanocarriers characterized by a hydrophobic core and a hydrophilic exterior. The nanocarrier core may include amphiphilic functionality such as cholic acid or cholic acid derivatives, and the exterior may include branched or linear poly(ethylene glycol) segments. Nanocarrier cargo such as hydrophobic drugs and other materials may be sequester in the core via non-covalent means or may be covalently bound to the telodendrimer building blocks. Telodendrimer structure may be tailored to alter loading properties, interactions with materials such as biological membranes, and other characteristics.

Abstract: The invention relates to a quinazoline derivative represented by the general formula (I), a pharmaceutical acceptable salt and a stereoisomer thereof as tyrosine kinase inhibitor, wherein R1, R2, R3, R3?, R4, R5, R6, X, L, T, Z and q are as defined in the specification. The invention also relates to a process for preparing the same, a pharmaceutical composition and a pharmaceutical formulation containing the derivative, use of the derivative for treating excessive proliferative diseases and chronic obstructive pulmonary disease and use of the derivative in the manufacture of a medicament for treating excessive proliferative diseases and chronic obstructive pulmonary disease.

Abstract: Compositions comprising hydroxytyrosol-containing formulations and treatment regiments comprising hydroxytyrosol and/or oleuropein and chemotherapeutic agents are disclosed. Compositions and/or regiments may optionally include the administration of vitamins, minerals, and anti-oxidants. Methods for using these compositions and treatment regimens for treating subjects for diseases, such as a malignancy, and for inducing or enhancing angiogenesis, treating or preventing oxidative stress, for treating or preventing high glucose-induced dysfunction, treating or preventing chemotherapy-induced dysfunction, and for improving cell viability are provided. Various methods for use of the hydroxytyrosol compositions for inhibition of lysine specific demethylase 1 (LSD1) in various cancers are also provided.

Abstract: A composition comprising intact killed bacterial cells that contain a therapeutic nucleic acid, a drug or a functional nucleic acid is useful for targeted delivery to mammalian cells. The targeted delivery optionally employs bispecific ligands, comprising a first arm that carries specificity for a killed bacterial cell surface structure and a second arm that carries specificity for a mammalian cell surface receptor, to target killed bacterial cells to specific mammalian cells and to cause endocytosis of the killed bacterial cells by the mammalian cells. Alternatively, the delivery method exploits the natural ability of phagocytic mammalian cells to engulf killed bacterial cells without the use of bispecific ligands.

Abstract: Compounds useful for the treatment of giardiasis are described.

Abstract: The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational change in the protein AuroraB and whose binding constant for the two-step process is given as Ki*. Finally, this invention also relates to compounds having the features of the pharmacophore.

Abstract: Disclosed herein are methods of treating, diagnosing, and prognosing GLUT-dependent cancers and OXPHOS-dependent cancers. In some embodiments, the methods comprise administering to a patient in need thereof a GLUT inhibitor and/or an OXPHOS inhibitor. The inhibitors may be administered before, concurrently, or after one another. Suitable GLUT-dependent cancers may include a GLUT4-dependent cancer, a GLUT8-dependent cancer, and a GLUT11-dependent cancer. Suitable GLUT inhibitors may include a GLUT4 inhibitor, a GLUT8 inhibitor, and a GLUT11 inhibitor. Suitable OXPHOS-dependent cancers may include mitochondrial OXPHOS-dependent cancers, including cancers that have developed resistance to treatment with a GLUT-inhibitor.

Abstract: The present invention relates to an amphiphilic polymer whose property and structure can change under hypoxic conditions, and to nanoparticles formed by self-assembly of the amphiphilic polymer. The hypoxia-responsive nanoparticles according to the present invention release a drug selectively under hypoxic conditions. Thus, the nanoparticles can be used for the selective diagnosis and treatment for diseases that are accompanied by hypoxia. Particularly, the nanoparticles can release a drug only to a targeted tumor in cancer therapy, and thus have minimized side effects and maximized therapeutic effects.

Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.

Abstract: The present invention provides three-component compositions comprising microparticles, a tumor antigen, a first immune adjuvant, and a second immune adjuvant. Also provided are chemo-immunotherapeutic compositions comprising microparticles, a chemotherapeutic agent, and an immune adjuvant.

Abstract: The present invention relates to a curcuminoid for enhancing the clinical efficacy of Docetaxel for the treatment of cancers and metastases.

Abstract: A dispersible powder composition comprises aminoglycoside for delivery to the lungs. The composition is effective to provide a therapeutically effective therapy via administration of less than 6 respirable unit doses by inhalation, wherein each unit dose comprises a volume of 0.30 to 0.95 mL.

Abstract: This application provides compositions and methods useful in the treatment of certain cancers. In part, this application is based on the recognition that certain molecules that target abasic lesions or AP sites in DNA improve, augment, or potentiate the chemotherapeutic efficacy of certain anticancer agents.

Abstract: The present invention describes novel amphoteric materials based on crosslinked hyaluronic acid, according to the general formula (I), and a method of preparation of said materials. Further, the invention relates to the material containing entrapped active agents (e.g. drugs, growth factors etc.) and a method of preparation thereof. Moreover, the present invention relates to the use of said materials for controlled release systems, in tissue engineering, wound dressing or tissue regeneration.

Abstract: The present invention relates to triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.

Abstract: The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.

Abstract: The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same. Compositions herein are useful for drug-delivery applications.

Abstract: The present invention relates to formulations comprising an anthracycline compound and an aromatic or heterocyclic compound.

Abstract: The present disclosure is directed to compositions for the promotion of muscle protein synthesis and control of tumor-induced weight loss in patients that are, for example, suffering from cancer cachexia. The present disclosure is also directed to methods of administering such compositions.

Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.

Abstract: The invention encompasses micelle assemblies, compositions having micelle assemblies, and methods for preparing micelle assemblies and compositions thereof. The invention also encompasses a prolamine protein conjugated to a polymer, such as a polyethylene glycol (PEG) chain, which conjugates can be used to prepare micelle assemblies. The invention further encompasses methods of encapsulating molecules using the conjugates of the invention. The micelle assemblies can be used for a variety of applications, such as treating cancer, targeting tumors, reducing the toxicity of a drug in vivo, increasing the efficacy of an encapsulated agent in vivo, protecting an encapsulated agent against degradation, and enhancing the water solubility of a drug or other agent.

Abstract: Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed.

Abstract: The present disclosure is generally directed to an embolic material which, in some embodiments, may be in the form of a microsphere or a plurality of microspheres. The embolic material generally comprises carboxymethyl chitosan (CCN) crosslinked with carboxymethyl cellulose (CMC). In some embodiments, the embolic material may further comprise a therapeutic agent, such as doxorubicin.

Abstract: Provided herein are methods of inhibiting proliferation of one or more tumor cells comprising contacting the one or more tumor cells with a composition comprising one or more epigenetic drugs that inhibit one or more epigenetic mechanisms of the tumor cells, wherein the one or more epigenetic drugs are encapsulated in a nanogel. The invention is also directed to methods of treating a tumor, metastasis of a tumor or a combination thereof in an individual in need thereof. The invention is also directed to a method of sequentially delivering one or more epigenetic drugs that alter one or more epigenetic mechanisms of a tumor cell and one or more chemotherapeutic drugs to an individual that has a tumor. Compositions which comprise one or more epigenetic drugs that alter one or more epigenetic mechanisms of a tumor cell, wherein the one or more epigenetic drugs are encapsulated in a nanogel.

Abstract: An aqueous hair cleansing agent contains a sulfate-type anionic surfactant having a specific structure, an ether carboxylate-type anionic surfactant having a specific structure, and an organic carboxylic acid or salt thereof, thereby has a pH of 1 to 5 at 25° C. when diluted 20-fold with water.

Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.

Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.

Abstract: The present invention relates to therapeutic compositions for treating cancer or preventing the growth of cancer cells, e.g., tumor growth, in a subject. The present invention also relates to methods for treating cancer, e.g., inhibiting tumor growth, in a subject who has become resistant to treatment, by administering to a subject an effective amount of a proteasome inhibitor and an effective amount of a therapeutic agent, e.g., a chemotherapeutic agent. The present invention further relates to methods for purging bone marrow, i.e., removing cancer cells from bone marrow, by exposing the bone marrow cells to a proteasome inhibitor and a therapeutic agent, e.g., a chemotherapeutic agent.

Abstract: The present invention relates to a bifunctional hydroxy-bisphosphonic acid derivative of formula (I) below: or a pharmaceutically-acceptable salt thereof, a method for producing the same, pharmaceutical compositions containing the same, and the use thereof as a medicament, as well as a compound of formula (II) below: or a pharmaceutically-acceptable salt thereof, and the use thereof for producing a vectorized molecule of therapeutic or diagnostic purpose.

Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to an binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.

Abstract: The present invention is directed to protocells for specific targeting of hepatocellular and other cancer cells which comprise a nanoporous silica core with a supported lipid bilayer; at least one agent which facilitates cancer cell death (such as a traditional small molecule, a macromolecular cargo (e.g.

Abstract: In this disclosure, a method is described wherein the method comprises mixing a therapeutic gas or a therapeutic liquid or a combination thereof and a liquid carrier in a high shear device to produce a dispersion; and administering the produced dispersion intravenously to a patient; wherein the produced dispersion contains nanobubbles of the therapeutic gas or droplets of the therapeutic liquid with a mean diameter of less than about 1.5 ?m. In this disclosure, a system is also described wherein the system comprises a therapeutic gas source or a therapeutic liquid source or a combination thereof; a liquid carrier source; a high shear device (HSD) having an inlet, an outlet, at least one rotor, and at least one stator separated by a shear gap; and a pump configured to control the flow rate and residence time of a fluid passing through the high shear device.

Abstract: The invention provides compositions and methods for visualizing particular tissues and delivering one or more therapeutics to that tissue using single-walled carbon nanotubes (SWNTs), which are taken up and delivered to target tissues by specific monocytes in the body. The delivery of SWNT to target tissues allows the visualization of the affected tissue for diagnostics and therapy in diseases where the specific monocyte is implicated in the disease pathogenesis. These nanotubes can be conjugated to a peptide, such as RGD, which helps direct the SWNT-containing monocytes to the vascular endothelium.

Abstract: A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.

Abstract: Receptor protein kinases (RPTKs) transmit extracellular signals across the plasma membrane to cytosolic proteins, stimulating formation of complexes that regulate key cellular functions. Over half of the known tyrosine kinases are implicated in human cancers and are therefore highly promising drug targets. A large-scale loss-of-function analysis of tyrosine kinases using RNA interference in the clinically relevant Erb-B2 positive, BT474 breast cancer cell line showed that Bruton's tyrosine kinase (BTK), a cytosolic, non-receptor tyrosine kinase that has been extensively studied for its role in B cell development, is required, in altered form, for BT474 breast cancer survival. This alternative form contains an amino-terminal extension that is also present in tumorigenic breast cells at significantly higher levels than in normal breast cells.

Abstract: What is described is a method for identifying a cancer patient that is amenable to anti-angiogenesis therapy in combination with chemotherapy for longer overall survival and/or progression-free survival by measuring the status of tumor cell HER2 expression, p53 expression, and apoptosis or endothelial cell CD31 expression in a tumor sample obtained from the patient prior to treatment. Bevacizumab, an antibody to vascular endothelial growth factor, is a preferred anti-angiogenesis therapy for treating several cancer types including breast cancer. Cancer patients with p53-negative or HER2 negative tumors, especially dual p53 HER2-negative tumors or tumors with low levels of apoptosis or high endothelial cell CD31 expression in the tumor samples are more amenable to anti-angiogenesis therapy with bevacizumab. These tumor characteristics provide a diagnostic method for identifying cancer patients amendable to anti-angiogenesis therapy plus chemotherapy for better treatment outcome.

Abstract: The invention features methods and compositions feature lapatinib and/or rapamycin for treating or preventing a cardiac condition induced by anthracycline treatment.

Abstract: Methods for treating cancer comprising administering a metabolic targeting chemo-immunotherapy regimen are provided herein. In one embodiment, the metabolic targeting chemo-immunotherapy regimen may include steps of administering a therapeutically effective dose of one or more immunologic agents (e.g., a therapeutic antibody) to stimulate an immune response in a subject having cancer; reducing the patient's blood glucose level; and administering a therapeutically effective dose of one or more chemotherapeutic agents. The methods described herein may be used to treat any type of cancer, especially malignant and metastatic late stage cancers.