Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.

Abstract: The present invention describes the use of translation inhibitors for the treatment of cancer and other disorders. Described herein are translation-inhibiting compounds, and methods of using those compounds for the treatment of cancer and other disorders. In some aspects the compounds inhibit translation elongation at the ribosome. In some aspects the compounds are used alone or in combination with known therapies.

Abstract: The present invention provides triazole compounds of Formula I: as further described herein. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, and a method of treating a disorder mediated, at least in part, by KSP in a mammalian patient comprising administering to a mammalian patient in need of such treatment a therapeutically effective amount of a compound of Formula I.

Abstract: The subject of the present invention is a liposomal formulation containing an anti-tumour compound characterised in that it contains the active compound encapsulated in liposome vesicles forming a composition of lipid components in the ratio of 1 part by mass of the active compound per 5 parts by mass of the lipid components, preferably 1 part by mass of the active compound per 5 parts by mass of the lipid components as well as a vitamin or a derivative thereof, a method of producing it as well as composition containing the said formulation.

Abstract: Described herein are compositions and methods for the prognosis, prevention and treatment of melanoma or melanoma associated symptoms. The compositions are microRNA molecules associated with melanoma or with melanoma brain tropism, as well as various nucleic acid molecules relating thereto or derived therefrom.

Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.

Abstract: The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer.

Abstract: Nanoparticle having a poly(beta-amino ester) coating. The poly(beta-amino ester) coating includes one or more therapeutic agents that can be delivered by the particle and one or more anchoring groups that couple the polymer to the nanoparticle's core surface. In certain embodiments, the poly(beta-amino ester) includes one or more polyalkylene oxide groups. The poly(beta-amino ester) can further include a targeting agent to target the nanoparticle to a site of interest and a diagnostic agent that allows for imaging of the particle. Methods for making and using the nanoparticles are also provided.

Abstract: The present invention relates to a microvesicle that is derived from nucleated mammalian cells, which are smaller than the nucleated cells. The microvesicles of the present invention can be used in the delivery of a therapeutic or diagnostic substance to specific tissues or cells, and more particularly, relates to microvesicles derived from monocytes, macrophages, dendritic cells, stem cells or the like, which can be used to deliver specific therapeutic or diagnostic substances for treating and/or diagnosing tissue associated with cancer, diseased blood vessels, inflammation, or the like.

Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

Abstract: Methods for treating neoplasm, tumors and cancers, using one or more tumor treating drug carriers, haptens and anticancer drugs, alone or in combination with other antineoplastic agents or treatments, are provided. Also provided are compositions, and kits containing the composition for affecting the therapy.

Abstract: The present invention relates to compounds and pharmaceutical compositions for treating cellular proliferative disorders, e.g., in patients having one or more p53-deficient cells, screening assays for identifying such compounds, and methods for treating such disorders.

Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a chemosensory receptor ligand, such as a bitter receptor ligand. Also provided herein are chemosensory receptor ligand compositions, including bitter receptor ligand compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Abstract: The present invention provides thermo-sensitive, mucoadhesive biopolymer formulations that enhance the penetration of therapeutics across the skin or mucosal surfaces. In a preferred embodiment, the biopolymer formulation comprises co-polymer of poloxamer 188 and propylene glycol, laurocapram and, optionally, one or more therapeutic agents. Also provided are uses of the biopolymer formulations for topical therapy of cancer including cervical cancer.

Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.

Abstract: Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises wherein R? is —H or —CH3, wherein R is —NR1R2, wherein R1 and R2 are alkyl groups, wherein R1 and R2 are the same or different, wherein R1 and R2 together have from 5 to 16 carbons, wherein R1 and R2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.

Abstract: The invention relates to new therapeutic approaches for treating cancer, in particular hepatocellular carcinoma, with Nanoparticules loaded with a chemotherapeutic antitumoral agent. In particular, it relates to the treatment of cancer by administration of said Nanoparticules by intravenous infusion for at least 2 hours in order to prevent toxicological side effects and increase the benefit/risk ratio of the treatment.

Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of chronic and acute conditions. Such conditions may be caused by disease, be symptoms or sequelae of disease. Chronic and acute conditions may be due to viral infections such as HIV and AIDS, neoplastic diseases stroke, kidney disease, urinary incontinence, autoimmune disorders, Parkinson's disease, prostate hypertrophy, aging, or the treatment of such diseases. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools against acute and chronic conditions in mammalian subjects.

Abstract: Disclosed are nanoparticles, such as carbon nanotubes or other graphitic sheet materials having extended aromatic surfaces, which are used to deliver active agents such as drugs, labels or dyes (termed for convenience a “drug”) to the interior of cells. The nanoparticles are functionalized by a hydrophilic polymer or adsorption of an amphiphilic molecule to render them stable in suspension. The drug is therefore capable of release in the cell exterior. The drug is more rapidly released at lower pH, as found e.g., in tumor cells. The drug may also be linked to a branched chain hydrophilic polymer, so that each polymer molecule carries more than one drug bound by a cleavable linker.

Abstract: Time-staggered inhibition of EGFR, in combination with DNA damaging agents, is a useful therapeutic strategy for treating cancers, particularly drug resistant cancers such as a subset of triple-negative tumors, particularly those with high basal levels of phosphorylated EGFR. The staggered therapy was also demonstrated to be applicable to other types of tumors, especially lung cancers, which contain either high levels of phosphorylated wild-type EGFR or mutations within EGFR itself. EGFR inhibition dramatically sensitizes cancer cells to DNA damage if the drugs are given sequentially, but not simultaneously. The first drug must be administered in a dosage and for a period of time sufficient for the dynamic network rewiring of an oncogenic signature maintained by active EGFR signaling to unmask an apoptotic process that involves activation of caspase-8.

Abstract: Methods for forming, modifying, and drug loading of a copolymer are provided, along with the resulting products. The method can include polymerizing 2-(pyridin-2-yldisulfanyl)ethyl acrylate with poly(ethylene glycol)methacrylate via free radical polymerization to form the copolymer. The molar ratio of 2-(pyridin-2-yldisulfanyl)ethyl acrylate to poly(ethylene glycol)methacrylate is about 100:1 to about 1:100. After polymerizing, the copolymer can be reacted with a thiol monomer that contains a carbon-bonded sulfhydryl to modify end groups on a first portion of the 2-(pyridin-2-yldisulfanyl)ethyl acrylate repeating units. Thereafter, the copolymer can be crosslinked, and a drug can then be loaded into the crosslinked copolymer.

Abstract: In the present invention there is provided a pharmaceutical composition in a solid dosage form suitable or oral administration, the composition comprising bendamustine or a pharmaceutically acceptable ester, salt or solvate thereof as an active ingredient, and at least one pharmaceutically acceptable excipient, which is a pharmaceutically acceptable saccharide selected from the group consisting of one or more of a monosaccharide, a disaccharide, an oligosaccharide, a cyclic oligosaccharide, a polysaccharide and a saccharide alcohol, wherein the ratio by weight of the active ingredient to the saccharide excipient(s) is in the range of 1:1-5.

Abstract: The present invention relates to pharmaceutical formulations that increase the solubility and bioavailability of indibulin, such as a spray-dried solid dispersion of indibulin with at least one matrix polymer. The invention further provides dosage formulations comprising the dispersion and processes for making the dispersion. The present invention also discloses a method of treating immune system based disorders, hyper-proliferative disorders, angiogenesis, malignancies, and neoplasms with the indibulin formulations disclosed herein.

Abstract: A method for treating core binding factor (CBF) leukemia in a subject, comprising administering to a subject having CBF leukemia a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt or ester thereof, that inhibits CBF? and RUNX1 binding in the subject, thereby treating the CBF leukemia.

Abstract: The present invention provides compositions including anti-tumor agents and inhibitors of Goodpasture antigen binding protein, p21, and ABCC7, and their use in treating cancer.

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: Provided are methods, nucleic acids, and arrays for assessing the susceptibility of a subject to the development of cardiotoxicity in response to receiving one or more anthracycline compounds, the method including determining the presence or absence of one or more polymorphisms, wherein the presence or absence of one or more such polymorphisms is indicative of susceptibility to the development of cardiotoxicity.

Abstract: The present invention relates to a polymer obtained from the polymerization of: (i) at least one monomer of formula (I) (CH2?CR1)CO—K (1) wherein: K represents O—Z or NH—Z, Z representing (CR2R3)m-CH3, (CH2—CH2—O)m-H, (CH2—CH2—O)m-CH3, (CH2)m-NR4R5 with m representing an integer from 1 to 30; R1, R2, R3, R4 and R5 independently represent H or a C1-C6 alkyl; (ii) at least between 0.1 and 50% mol, advantageously between 1 and 30% mol, more advantageously between 1 and 20 mol % of a cyclic monomer having a exomethylene group of formula (II) wherein: R6, R7, R8 and R9 represent independently H or a C5-C7 aryl group or R6 and R9 are absent and R7 and R8 form together with the carbon atom on which they are bonded a C5-C7 aryl group; i and j represent independently an integer chosen between 0 and 2; X represents either O or X is not present and in this latter case, CR6R7 and CR8R9 are linked via a single bond C—C and (iii) at least one bio-resorbable block copolymer cross-linker.

Abstract: The application describes methods for screening subjects with breast cancer to determine if the breast cancer will be responsive to a breast cancer therapy including a taxane or a taxane derivative. The application also describes methods for treating subjects with breast cancer by screening them for the likelihood of the effectiveness of treating the cancer with a therapy including a taxane or a taxane derivative and administering the therapy in subjects when it is found that a taxane or a taxane derivative is likely to be effective.

Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such compound admixed with at least one pharmaceutically acceptable excipient.

Abstract: The use of specific microRNAs (miRNAs) present in CSF as biomarkers for particular brain malignancies and disease activity.

Abstract: This invention relates to high-throughput, semi-automated methods for identifying compounds that are effective in targeting leukemia stem cells, as well as compounds identified by those methods and uses thereof for treating leukemia.

Abstract: Antibodies to human ?V-tubulin, fragments thereof, and compositions comprising such are provided. Diagnostic, prognostic and identification methods employing such antibodies or fragments thereof are also provided.

Abstract: A plurality of artificial red blood cell particles includes each particle of the plurality being substantially monodisperse and each particle having a largest common linear dimension of about 5 ?m to about 10 ?m. The particles can also have a modulus configured such that a particle of the plurality of particles can pass through a tube having an inner diameter of less than about 3 ?m.

Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.

Abstract: A delivery device for an active agent comprises nanoparticles based on a biopolymer such as starch. The delivery device may also be in the form of an aptamer-biopolymer-active agent conjugate wherein the aptamer targets the device for the treatment of specific disorders. The nanoparticles may be made by applying a high shear force in the presence of a crosslinker. The particles may be predominantly in the range of 50-150 nm and form a colloidal dispersion of crosslinked hydrogel particles in water. The biopolymer may be functionalized. The aptamer may be conjugated directly to the cross-linked biopolymers. The active agent may be a drug useful for the treatment of cancer. The delivery device survives for a period of time in the body sufficient to allow for the sustained release of a drug and for the transportation and uptake of the conjugate into targeted cells. However, the biopolymer is biocompatible and resorbable.

Abstract: Anthracycline derivatives are suitable for use in cancer therapy and diagnosis. These anthracycline derivatives can be radiolabelled and used as an imaging agent in cancer diagnosis. The radiolabelled anthracycline derivatives can also be used together with a drug delivery system, in particular including a two-step targeting strategy, for treating solid and disseminated tumors. These drug delivery system can advantageously be used for treatment and diagnosis of breast cancer.

Abstract: Polymeric nanoparticles with a hydrophobic core that encapsulates curcumin and a hydrophilic shell with one or more chemotherapeutic agents (e.g., doxorubicin) associated with the shell surface are formed from N-isopropylacryl amide (NEPAAM), acrylic acid (AA), and at least one vinyl monomer selected from the group consisting of vinyl acetate, 4-vinyl benzoic acid, methylmethacrylate, vinylmethacrylate, N-vinylpyrrolidone, N-vinyl piperidone, N-vinyl caprolacum, N-vinyl carbazole, and styrene, where the NIPAAM, the AA, and the vinyl monomer are present at molar ratios of 50-70:10-30:10-30 for NIPAAM:AA:vinyl monomer. These nanoparticles effectively overcome multidrug resistance and ameliorate cardiomyopathy in vivo.

Abstract: The present invention relates to a method for effectively delivering an anticancer drug into cancer cells by binding the anticancer drug to pH-sensitive metal nanoparticles so as to be separated from cancer cells. The pH-sensitive metal nanoparticles according to the present invention may be heated by photothermal therapy, thereby effectively killing cancer cells in conjunction with the isolated anticancer drug.

Abstract: A polymeric drug, in which a cancerostatic connected via spacers containing hydrolytically cleavable hydrazone bonds is bound to a water-soluble polymeric carrier prepared on the basis of a N-(2-hydroxypropyl)methacrylamide copolymer, wherein the structure of the polymeric drug consists of the main chain of N-(2-hydroxypropyl)methacrylamide carrying the cancerostatic and another chain of N-(2-hydroxypropyl)methacrylamide—a graft, which may also carry a cancerostatic, said grafts being bound to the main chain by a bond that is stable in the body and/or by a bond cleavable in the body, especially by an oligopeptide spacer selected from the series of GlyLeuGly (SEQ ID. NO. 1), GlyPheGly (SEQ ID. NO. 2), GlyPheLeuGly (SEQ ID. NO. 3) and GlyLeuPheGly (SEQ ID. NO. 4), and a method of its preparation.

Abstract: A drug carrier is provided with a structure of a lipid shell enclosing aqueous micelles. The lipid shell includes lipid and emulsifier, in which the emulsifier encloses the lipid. The components of the aqueous micelles are phospholipids and amphiphilic chitosan, and the aqueous micelles enclose an aqueous solution containing a drug. Furthermore, the method of preparing the drug carrier is also provided. Therefore, with the pharmaceutical advantages of lipid-based nanoparticle included low drug leakage and the ability of to overcome the multiple drug resistance, this new formulation were further incorporated with the chitosan and featured with high payload efficiency. The features could enhance intracellular concentration of anti-cancer drug and oral bioavailability.

Abstract: The present invention relates in general to the field of targeted drug delivery of anti-cancer drugs. More precisely, the present invention concerns polymer drug conjugates, namely, conjugates of poly(organo)phosphazenes and anti-cancer drugs, wherein the conjugates are suitable to selectively release anti-cancer drugs in tumor tissue. In addition, the present invention relates to a method for manufacturing such poly(organo)phosphazene molecule conjugates, to poly(organo)phosphazene molecule conjugates for use in medicine, in particular, to poly(organo)phosphazene molecule conjugates for use in the treatment of cancer, and to pharmaceutical compositions comprising such poly(organo)phosphazene molecule conjugates.

Abstract: Disclosed is a lyophilized liposome composition encapsulating a water-soluble drug and a preparation process thereof. The lyophilized liposome composition comprises a water-soluble drug, a phospholipid, a polyethylene glycol-derivatized phospholipid, cholesterol and a lyoprotectant, wherein the lyoprotectant comprises a saccharide and a cyclodextrin or cyclodextrin derivative. The encapsulation rate of the lyophilized liposome composition encapsulating the water-soluble drug is ?90%.

Abstract: A particle includes an aqueous core; a first amphiphilic layer surrounding the aqueous core; and a polymeric matrix surrounding the first amphiphilic layer.

Abstract: Clostridium novyi is an obligate anaerobe that can infect hypoxic regions within experimental tumors. We found that mice bearing large, established tumors were often cured when treated with C. novyi plus a single dose of liposomal doxorubicin. The secreted factor responsible for this phenomenon was identified and, surprisingly, proved to be a member of the lipase family. The gene encoding this protein, called liposomase, has the potential to be incorporated into diverse therapeutic methods to deliver specifically a variety of chemotherapeutic agents to tumors.

Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.

Abstract: The present invention provides micelles having an anthracycline encapsulated therein, the micelles comprising a multiblock copolymer. The invention further provides methods of preparing and using said micelles, and compositions thereof.

Abstract: The present invention relates to a composition for enhancing immunity through inducing the expression of interferon-? comprising a compound represented by Formulas 1 to 8, or Sophora flavescens extract comprising the same and fractions thereof as an active ingredient, a feed additive, feed composition, pharmaceutical composition, food composition, and over-the-counter (OTC) drug composition comprising the composition, and a method for enhancing immunity through administrating the composition. A composition for inducing the expression of interferon-?, comprising a compound represented by Formulas 1 to of the present invention, Sophora flavescens extract comprising the same, or fractions thereof as active ingredient can prevent, alleviate, or treat the diseases that can be prevented or treated by increasing the expression of interferon.

Abstract: A composition comprising a pharmaceutically effective amount of zeaxanthin or its derivative for use in treating a malignant tumor and a method of using a pharmaceutically effective amount of zeaxanthin or its derivative either alone or together with one or more pharmaceutical agents for treating a malignant tumor. The tumor may be, but is not limited to breast cancer, cervix cancer, colon cancer, cutaneous melanoma, cutaneous squamous carcinoma, hepatocellular carcinoma, lung cancer, osteosarcoma, prostate cancer, and uveal melanoma. The pharmaceutically effective amount of zeaxanthin is generally above about 0.5 mg/kg/d to about 20 mg/kg/d.

Abstract: The present invention provides compositions and methods for the delivery of nucleic acids to a cell. The present invention additionally provides compositions and methods for the treatment of a disease or disorder, particularly cancer.