Abstract: This disclosure relates generally to the field of prostate cancer and, in particular, methods of identifying and treating patients having castrate resistant prostate cancer.

Abstract: The present invention is a method and compound for treating cancer and tumors. The invention treats cancer by encapsulating certain cancer fighting drugs in a liposome. Peptides attached to the compound then guide the compound towards its target. During its journey, DSPE-PEG is used to stabilize the compound, to allow more time in the blood stream before losing effectiveness.

Abstract: The present invention is directed to a crosslinked or non-crosslinked polymer particle, wherein the crosslinked polymer particle comprises a copolymer of poly(alkylene glycol-graft-acrylate) that is crosslinked by at least one hydrolysable monomer or crosslinking agent. The present invention is also directed to a polymer particle comprising a crosslinked polymer particle that is a product of starting materials comprising (a) a hydrophilic monomer, (b) a hydrophobic monomer, and (c) a hydrolysable crosslinking agent (the crosslinking agent may be absent in the case of non-crosslinked particles). The present invention is still further directed to a polymer particle comprising a crosslinked copolymer, where the crosslinked copolymer includes structures represented by Formulas (I), (II), and (III), as defined in the specification. Other embodiments of the present invention also include methods of manufacturing polymer particles.

Abstract: The present invention relates to a stable crystalline monohydrate of epirubicin hydrochloride having water content in the range between 2.7% and 3.5% (w/w) and being devoid of residual solvents as well as to a corresponding method for its production. The method comprises: (a) adding at least a first solvent and at least a second solvent to epirubicin hydrochloride, wherein the first solvent is a linear or branched C4 to C5 alcohol, and the second solvent is a linear or branched C2 to C3 alcohol; (b) adjusting in the solution obtained the water content to an amount in the range between 7% and 12% (w/w); and (c) heating the mixture to a temperature of 70° C. to 90° C. in order to allow crystallization.

Abstract: Polymorphic forms of onapristone and methods of making and using such polymorphic forms are provided. Crystalline polymorphic forms can be characterized by their X-ray powder diffraction patterns and other properties.

Abstract: Compounds having the Formula I and pharmaceutically acceptable salts thereof are provided in which the variables are described herein. Methods of making the compounds of Formula I are also disclosed.

Abstract: A pharmaceutical combination comprising a topoisomerase I inhibitor, and an Hsp90 inhibitor according to the following formulae (I) (Ia) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein.

Abstract: Provided is a compound represented by the general formula (1) (where: G represents a hexose-6-phosphate residue; and L represents a divalent linker group).

Abstract: The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula (I) wherein: (i) R1 is chosen from the group constituted of —CH(CH3)2, —CH(CH3)CH2CH3, or cyclohexyle, (ii) X represents —CH2CH2—, or —CH?CH—, (iii) R2 is chosen from the group constituted of or —OH group, (iv) R3 is OH or NOH, (v) represents a single bond when R3 is OH, or a double bond when R3 is NOH, as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.

Abstract: A pharmaceutical composition is provided. The pharmaceutical composition includes a nanoparticle, a shell and a drug, wherein the nanoparticle has an outer surface and the drug is mixed with the shell and is formed on the outer surface.

Abstract: Lyophilized liposomal formulations with two or more encapsulated drugs are disclosed. These formulations display superior drug retention profiles and also maintain size distribution following lyophilization and reconstitution.

Abstract: Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the present application.

Abstract: The present invention relates to substituted imidazopyridine compounds of general formula (I) in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract: The present invention relates to a complex comprising a compound of formula (I), or a plant extract comprising the compound or a fraction thereof; and stevioside, or a plant extract comprising the stevioside or a fraction thereof, and relates to a pharmaceutical composition for preventing or treating an influenza virus infection comprising the complex as an active ingredient. Also, the present invention relates to a food composition for preventing or improving an influenza virus infection, a virucidal quasi-drug composition, a virucidal feed additive, and a feed, which comprises the complex as an active ingredient.

Abstract: The present invention is directed to a novel use of pyridone derivatives such as pirfenidone for the prevention and treatment of damages to tissues or organs induced by various cytotoxic agents, such as chemotherapeutic agents, biologics, immunosuppressants and radiation. Such prophylactic and/or therapeutic effects of the pyridone derivatives make it possible to increase therapeutic dosages of the cytotoxic agent, thereby enhancing the therapeutic efficacy of the cytotoxic agent and radiation therapy.

Abstract: A method of treating a tar-responsive dermatological disorder includes topically applying an anhydrous tar composition to skin of a mammal, preferably a human, that is involved with the disorder, the composition including a wax and a therapeutically effective amount of tar for topical treatment of the tar-responsive dermatological disorder, the composition being in liquid form when at a temperature selected from room temperature and a temperature of skin of a mammal upon application of the composition to the skin of the mammal.

Abstract: The presently disclosed subject matter generally relates to methods and compositions for inhibiting the expression and/or activation of hypoxia-inducible factor 1 (HIF-1) genes in a cancer cell, tissue or tumor. More particularly, the methods disclosed herein relate to inhibition of HIF-1 activation in a tumor, increasing sensitivity of a tumor cell to radiation and/or chemotherapy, delaying tumor growth, inhibiting tumor blood vessel growth, inhibiting inflammatory responses in a cell through the use of compositions that prevent the nitrosylation of HIF-1, and methods for screening for new inhibitors of HIF-1 activation. Additionally, the compositions disclosed herein relate to compositions that can be employed in, and are identified by, the disclosed methods.

Abstract: Provided herein are nanobubbles designed for use in ultrasound-mediated ablation of cancer cells. The nanobubbles undergo ultrasound-mediated cavitation at an ablation threshold which is significantly decreased, relative to standard ultrasound-mediated treatment of cancer cells. In exemplary embodiments, the nanobubbles comprise an amphiphilic ABC triblock copolymer, wherein block A comprises a hydrophilic polymer, block B comprises a crosslinking polymer, and block C comprises a hydrophobic copolymer comprising (i) methyl methacrylate (MMA) and (ii) a fluorinated monomer, wherein the fluorinated monomer is present in the hydrophobic copolymer of block C at 25 mole percent or less. Related treatment and diagnostic methods, as well as materials relating to the nanobubbles are provided herein. Methods of making a random copolymer are furthermore provided herein.

Abstract: Methods for preventing and/or reducing side effects of an anti-cancer agent in a subject in need thereof are disclosed. The method comprises administering to the subject, who is under an anti-cancer agent treatment, a composition comprising a therapeutically effective amount of isolated deoxyelephantopin and/or an analogue thereof; and a pharmaceutically acceptable carrier.

Abstract: Provided herein is a pharmaceutical composition comprising at least one isoflavonoid. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions.

Abstract: The invention relates to the use of encapsulates of cancer cells, in agarose coated, agarose containing beads, for isolating chemotherapeutic resistant cells which have at least one stem cell property, such as expression of OCT4.

Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Described herein are compounds, compositions and methods for treatment of cancer. Also described are methods and uses for identifying subject with cancer that are suitable for treatment with the compounds, composition and methods are described herein. In one aspect of the present invention, there is provided a method of treating a subject having a cancer deficient in NMT2, comprising: administering to said subject an NMT inhibitor.

Abstract: Erastin analogs are useful in treating various cancers, particularly multiple myeloma. Erastin analogs are also useful in treating cancers that are resistant to other anticancer agents.

Abstract: A method of improving longevity and/or alleviating a symptom of aging or preventing age related diseases is provided. The method includes a step in which the subject's average and type of daily protein intake, IGF-I, and IGFBP1 levels, and risk factors for overall mortality, cancer and diabetes are determined. With respect to protein consumption, the relative amounts of protein calories from animal and plant sources are determined. A periodic normal calorie or low calorie but low protein fasting mimicking diet with frequencies of every 2 weeks to 2 months is provided to the subject if the subject's average daily protein intake level and type and/or IGF-I levels, and/or IGFBP1 levels is identified as being greater or lower than a predetermined cutoff intake/level and if the subject is younger than a predetermined age. The method is also shown to alleviate symptoms of chemotoxicity.

Abstract: The present application relates to a method of monitoring the membrane permeabilization of liposome and the incidental release of a compound of interest.

Abstract: A method is provided for production of crystalline idarubicin hydrochloride, the method including the steps of: (i) producing a mixture containing (a) idarubicin hydrochloride, (b) at least one alcohol selected from 1-butanol, 2-butanol, and 1-pentanol, and (c) water; and (ii) crystallizing idarubicin hydrochloride from this mixture. A crystalline idarubicin hydrochloride is also provided characterized by a powder x-ray diffraction pattern in which at least reflexes at diffraction angles occur in the following ranges (in 2?): 7.2-7.7; 11.7-12.2; 16.2-16.7; 16.7-17.2; 19.6-20.1; 19.8-20.3; 22.2-22.7, and 22.9-23.4.

Abstract: This invention is in the field of anthracycline family of drugs. More particularly, it concerns converting daunorubicin hydrochloride to an orotate salt and providing methods of improving the tolerability of daunorubicin in animals by reducing the adverse effects and toxicity in noncancerous tissues. Daunorubicin orotate provides a safer treatment for specific types of leukemias and neuroblastomas in adults and in pediatric patients.

Abstract: Disclosed are methods of increasing the chemosensitivity of normal and/or chemoresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof. Also disclosed are methods of increasing radiosensitivity of normal and/or radioresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof.

Abstract: A method of preparing an anthracyclin such as epirubicin from a starting material comprising 13-dihydrodaunorubicine (13-daunorubicinol). The method comprises producing N-Trifluoroacetyl-13-daunorubicinol from 13-daunorubicinol by acylation. The N-Trifluoroacetyl-13-daunorubicinol is reacted with an aprotic solvent and an acylating agent to produce an intermediate sulfoxy salt which is treated with a strong base to produce 4?-keto-N-Trifluoroacetyldaunorubicin. The 4?-keto-N-Trifluoroacetyldaunorubicin is reacted with a reducing agent, such as borohydride of an alkaline metal, to produce N-Trifluoroacetyl-4?-epi-daunorubicin. The N-Trifluoroacetyl-4?-epi-daunorubicin is hydrolyzed in a basic solution to produce an intermediate compound. The intermediate compound is reacted with a halogenizing agent to produce a 14-Hal-derivative. The 14-Hal derivative is hydrolized in the presence of a formate of an alkaline metal to produce the desired final compound.

Abstract: The present disclosure provides methods and compositions for enhanced delivery of siRNA or miRNA, into the interior of multilayered tissues, and into the cytoplasm or nucleus of cells of a tissue. Such methods and compositions yield tumor-selective and intracellular delivery of RNAi agents and allow for RNAi-mediated activity such as knock-down of the target genes and associated products. The current disclosure further provides methods and compositions for improving the intracellular bioavailability of nucleotide agents.

Abstract: A composition comprising intact minicells that contain a drug molecule is useful for targeted drug delivery. One targeted drug delivery method employs bispecific ligands, comprising a first arm that carries specificity for a bacterially derived minicell surface structure and a second arm that carries specificity for a mammalian cell surface receptor, to target drug-loaded minicells to specific mammalian cells and to cause endocytosis of the minicells by the mammalian cells. Another drug delivery method exploits the natural ability of phagocytic mammalian cells to engulf minicells without the use of bispecific ligands.

Abstract: A method of treating a cancer comprising administering to a subject in need thereof an effective amount of a glycylcycline, for example tigecycline in combination with a chemotherapeutic such as daunorubicin or cytarabine.

Abstract: A process for producing a small-sized, lipid-based cochleates. Cochleates are derived from liposomes which are suspended in an aqueous two-phase polymer solution, enabling the differential partitioning of polar molecule based-structures by phase separation. The liposome-containing two-phase polymer solution, treated with positively charged molecules such as Ca2+ or Zn2+, forms a cochleate precipitate of a particle size less than one micron. The process may be used to produce cochleates containing biologically relevant molecules.

Abstract: Disclosed are methods, compositions and uses of conjugates of prodrug forms of 2-pyrrolinodoxorubicin (P2PDox) with antibodies or antigen-binding fragments thereof (ADCs), with targetable construct peptides or with other targeting molecules that are capable of delivering the P2PDox to a targeted cell, tissue or pathogen. Once delivered to the target cell, the ADC or peptide conjugate is internalized, a highly toxic 2-pyrrolinodoxorubicin (2-PDox) is released intracellularly. The P2PDox-peptide or ADC conjugates are of use to treat a wide variety of diseases, such as cancer, autoimmune disease or infectious disease.

Abstract: In a process for forming a hydrogel, a precursor crosslinkable through disulfide bonds for forming the hydrogel is provided in a solution. The precursor comprises a branched molecular structure, which comprises a plurality of branches. At least three of the branches each comprises a disulfide bond. The pH in the solution is adjusted to initiate thiol-disulfide exchange in the precursor, thus crosslinking the precursor through disulfide bonds formed by thiol-disulfide exchange. After the precursor is sufficiently crosslinked to form a hydrogel, the pH in the solution is adjusted to inhibit further thiol-disulfide exchange in the hydrogel. Further, a hydrogel matrix may comprise a polymer substantially crosslinked through disulfide bonds. The polymer may comprise a hydrophobic poly(amido amine) core and an amino-functionalized hydrophilic shell.

Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I: (I) wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.

Abstract: In one embodiment, the invention provides a new design of nanocarrier compositions that release their therapeutic load specifically at intraperitoneal cancers' site. These nanocarriers are administered intraperitoneally and comprise a plurality of porous nanoparticulates that (a) are loaded with one or more pharmaceutically-active agents alone or in combination with imaging agents thus providing a theranostic value and (b) that are encapsulated by and that support a lipid bilayer which is disrupted upon contact with a reactive oxygen species generated within the environment of the cancer. In other embodiments, the invention provides methods of treatment and pharmaceutical compositions comprising nanocarriers as described herein.

Abstract: A metal-salen complex compound, which exhibits excellent noninvasiveness and can be efficiently transferred to an affected site, a local anesthetic containing this metal-salen complex compound, and an antineoplastic drug containing this metal-salen complex compound are provided. Regarding the metal-salen complex compound, a metal atom part in each of two molecules of a metal-salen complex or a derivative of the metal-salen complex is dimerized via water, and the metal-salen complex compound is mixed with a base to produce an ointment.

Abstract: Provided are a BAB-type tri-block copolymer including a polylactic acid (A) that is a hydrophobic block and polyethylene glycol (B) that is a hydrophilic block, a method of preparing the BAB-type tri-block copolymer including synthesizing a polylactic acid (A)-polyethylene glycol (B) di-block copolymer by a ring opening polymerization of a lactic acid monomer using a hydroxyl group of polyethylene glycol (B) as a polymerization initiator; and synthesizing a BAB-type tri-block copolymer by reacting the AB-type di-block copolymer with polyethylene glycol (B) including at least one carboxyl group at one or more terminals thereof in the presence of a coupling agent and a catalyst, and a drug delivery system using the BAB-type tri-block copolymer.

Abstract: The present invention relates to oligooxopiperazines for reactivating p53. Methods of using the oligooxopiperazines are also disclosed.

Abstract: The combination of gallic acid, ellagic acid, and rubusoside was shown to inhibit angiogenesis by inhibition of pro-angiogenic factors. These three compounds were shown to be absorbed from the intestine making the compounds orally bioavailable. The ratio of the three compounds in the composition was a weight ratio of approximately 1:1.7:17.0 of gallic acid, ellagic acid, and rubusoside, respectively, resulting in a composition with 5% w/w gallic acid, 9% w/w ellagic acid, and 86% w/w rubusoside. This combination was also shown to reduce weight gain, fat accumulation, and serum cholesterol in mammals fed a high fat diet. It also reduced serum triglycerides and tended to reduce blood glucose in mammals on both normal and high fat diets. This three-compound composition (“GER”) can be used to treat diseases associated with angiogenesis and to decrease effects of a high fat diet.

Abstract: The present invention provides a lyophilized amrubicin formulation and a process thereof. In the process, the concentration of the aqueous solution before lyophilization is controlled to about 7.5 mg(potency)/mL or more. Thus, the formulation decreases the production of desaccharified compound and is stable to storage for a long period. The formulation is useful as a cancer chemotherapeutic agent.

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 the fabrication and uses of liposomal nanoparticles.

Abstract: Biomarkers of anthracycline cardiotoxicity are provided. In certain aspects, methods are provided for determining whether a subject will develop cardiotoxicity upon treatment with an anthracycline, such as doxorubicin, by measuring the level of Top2b expression in the subject. In further aspects, methods of a treating a subjects with anthracycline therapeutics and cardioprotective agents are provided.

Abstract: The disclosure provides a pharmaceutical composition. The pharmaceutical composition includes a chitosan with palmitoyl groups and an active agent. According to another embodiment, the pharmaceutical composition can further include a gelling accelerating agent. According to an embodiment of the disclosure, the active agent of the disclosure can be administered in the form of a nano-drug, liposome, micelle, or microparticle.

Abstract: Disclosed is a pH-sensitive hyaluronic acid derivative, comprising at least one repeat unit as shown in the following formula (I), wherein HA represents a unit comprising N-acetyl-D-glucosamine and D-glucuronic acid, q represents an integer of 2 to 10,000; A represents a biocleavable linkage comprising at least one of hydrazone, acetal, ketal and imine; M represents at least one of a hydrophobic fragment, a hydrophilic fragment, and an amphiphilic fragment, and p represents the number of [A-M] directly grafted onto each HA unit, p represents an integer of 0 to 4, and the p of each HA unit is not 0 at the same time.

Abstract: Inositol trisphosphate (ITPP) causes normalization of tumor vasculature and is a particularly effective cancer therapy when a second chemotherapeutic agent is administered following partial vascularization. ITPP also treats, alone or in combination, multi-drug resistant cancers. ITPP can also be used to reduce the amount of a second chemotherapeutic drug required for anticancer activity. In addition, ITPP enhances immune response and treats hyperproliferative disorders.

Abstract: Methods for treating or preventing cardiomyopathy in a subject by administering an ?1 adrenergic receptor agonist, wherein the treatment does not result in increased blood pressure are provided.