Abstract: Compositions and methods for determining circulating biomolecules before, during, and/or after treatment of a patient with an anti-cancer or anti-tumor drug (or putative drug) are described. Methods of treatments based on the compositions and methods described herein are also provided. Noninvasive methods and kits are provided for assessing the efficacy of an anti-cancer therapy for killing or damaging cancer cells. Embodiments are used to determine the cancer-killing efficacy of an anti-cancer drug in a patient, to optimize the selection of an anti-cancer drug for treatment of a patient, to adjust the dosage of an anti-cancer drug for treatment of a particular cancer in a patient and for identifying useful anti-cancer therapeutics for any one particular type of cancer.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.

Abstract: Drug-eluting devices and methods for the treatment of tumors of the pancreas, biliary system, gallbladder, liver, small bowel, or colon, are provided. Methods include deploying a drug-eluting device having a film which includes a mixture of a degradable polymer and a chemotherapeutic drug, wherein the film has a thickness from about 2 ?m to about 1000 ?m, into a tissue site and releasing a therapeutically effective amount of the chemotherapeutic drug from the film to treat the tumor, wherein the release of the therapeutically effective amount of the drug from the film is controlled by in vivo degradation of the polymer at the tissue site.

Abstract: Compositions comprising a therapeutic agent encapsulated by an edible plant-derived microvesicle are provided. Methods of treating an inflammatory disorder and methods of treating a cancer are further provided and include administering an effective amount of a composition comprising a therapeutic agent encapsulated by an edible plant-derived microvesicle to a subject. Further provided are methods of diagnosing a colon cancer that include the steps of administering an edible plant-derived microvesicle incorporating a detectable label to a subject and then determining an amount of the detectable label in an intestine of the subject.

Abstract: A coating material including a bio-absorbable cross-linked material and a cellular uptake inhibitor. The bio-absorbable cross-linked material includes two or more fatty acids cross-linked into a substantially random configuration by ester bonds. The coating material may be adhered to a medical device. A medical device system including a medical device and a coating is also included.

Abstract: The invention provides active agents, such as paclitaxel, rapamycin, or 17-DMAG, encapsulated by safe poly(ethylene glycol)-block-poly(lactic acid) (“PEG-b-PLA”) micelles. The compositions provide effective solubilization of drug combinations, such as paclitaxel, rapamycin, and 17-DMAG, as well as others described herein. A significant advantage of PEG-b-PLA as a carrier is that it is less toxic than Cremophor® EL or DMSO, which are used in currently known compositions. Additionally, PEG-b-PLA micelles are easier to handle than DMSO and they do not possess a foul odor, which is a problem with formulations currently in clinical trials. Accordingly, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity. It was also found that larger doses of individual drugs in micelle formulations can be administered compared to non-micelle formulations.

Abstract: The present invention provides a method for stimulating hair growth in a mammalian species or converting vellus hair or intermediate hair to terminal hair or stimulating hair follicles to increase hair growth and one or more properties selected from the group consisting of luster, sheen, brilliance, gloss, glow, shine or patina of hair associated with the follicles or increasing one or more of: length, thickness, number, and density, of eyelash hair or eyebrow hair comprising applying to the skin of a patient a composition comprising an effective amount of an EP3 agonist or an EP4 agonist prodrug or a mixture thereof. Such compositions which are used in treating the skin or scalp of a human or non-human animal may comprise an effective amount of 3, 7 or 3 and 7 thia prostanoic acid. A mixture of 3,7-dithia PGE1 and 3,7-dithia PGE1-isopropyl ester is preferred for this treatment.

Abstract: The present invention provides compositions comprising nanoparticles comprising: 1) a drug, such as a hydrophobic drug derivative; and 2) a carrier protein. Also provided are methods of treating diseases (such as cancer) using the compositions, as well as kits and unit dosages.

Abstract: A crystalline from of 13[(N-tert-butoxycarbonyl)-2?-O-hexanoyl-3-phenylisoserinyl]-10-deacetylbaccatin III.

Abstract: In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful selection of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered.

Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing a PGAM1 mediated condition such as cancer or tumor growth comprising administering an effective amount of PGAM1 inhibitor, for example, an anthracene-9,10-dione derivative to a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, head and neck cancer, and leukemia, 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: An equipment assembly for preparing, harvesting and collecting particles is disclosed. The assembly comprises a tandem filter system with one or more high pressure filters, one or more low pressure filters and one or more collection vessel. Particles can be prepared, harvested and collected continuously, semi-continuously or in a batch-type operation. A tandem filter system and its method of use are also disclosed. Particles made with the assembly and according the instant methods are also disclosed. The assembly provides improved particle harvesting and collection over other systems and permits continuous particle formation, in particular by dispersion of a solute-containing process fluid within a supercritical anti-solvent.

Abstract: A nanoparticulate composition is disclosed for the targeted therapeutic treatment of tumours. The stable self assembled nanocomposition according to the invention comprises (i) a carrier and targeting system comprising an optionally modified polyanion, and optionally a polycation, which may also be modified; at least one targeting agent which is linked to either the polycation/modified polycation or the polyanion/modified polyanion, or both or to the surface of the nanoparticle; (ii) paclitaxel as active compound; and optionally (iii) at least one complexing agent, a metal ion and a stabilizer/formulating agent or a PEGylating agent. The invention furthermore relates to a process for the preparation of the above-mentioned composition, the therapeutic uses thereof, and pharmaceutical compositions containing the nanocomposition according to the invention.

Abstract: The present invention relates to pharmaceutical compositions of various pharmaceutical actives, especially lyophilic and hydrophilic actives containing Diethylene glycol monoethyl ether or other alkyl derivatives thereof as a primary vehicle and/or to pharmaceutical compositions utilizing Diethylene glycol monoethyl ether or other alkyl derivatives thereof as a primary vehicle or as a solvent system in preparation of such pharmaceutical compositions. The pharmaceutical compositions of the present invention are safe, non-toxic, exhibits enhanced physical stability compared to conventional formulations containing such pharmaceutical actives and are suitable for use as injectables for intravenous and intramuscular administration, as well as for use as a preformed solution/liquid for filling in and preparation of capsules, tablets, nasal sprays, gargles, dermal applications, gels, topicals, liquid oral dosage forms and other dosage forms.

Abstract: A nanoparticulate composition is disclosed for the targeted therapeutic treatment of tumours. The stable self assembled nanocomposition according to the invention comprises (i) a carrier and targeting system comprising an optionally modified polyanion, and optionally a polycation, which may also be modified; at least one targeting agent which is linked to either the polycation/modified polycation or the polyanion/modified polyanion, or both or to the surface of the nanoparticle; (ii) an active compound selected from the group of docetaxel and its pharmaceutically acceptable salts and derivatives especially its hydrates, especially docetaxel trihydrate and docetaxel trihydrate monohydrochloride; and optionally (iii) at least one complexing agent, a metal ion and a stabilizer/formulating agent, or a PEGylating agent.

Abstract: The present application relates to compositions comprising and methods of using a liposome comprising a pHLIP polypeptide, wherein a lipid bilayer of the liposome is substantially free of the pHLIP polypeptide.

Abstract: The present invention relates to compositions for the treatment of cancerous tissues in warm-blooded animals containing one or two anticancer agents attached to polymeric carriers having monomer units derived from one or more of N-(2-carboxypropyl)methacrylamide (2-CPMA), N-(3-carboxypropyl)methacrylamide (3-CPMA), N-(2-aminopropyl)methacrylamide (2-APMA) and/or N-(3-aminopropyl)methacrylamide (3-APMA) are also included. Anticancer agents in compositions can be attached to said polymeric carrier by side-chains which can be susceptible to hydrolysis by lysosomal enzymes intracellularly. Compositions can also include a targeting ligand attached to the polymeric carrier, optionally through a second linker.

Abstract: This application provides a high throughput method of making nanoparticles that utilizes plates comprising wells (e.g., 96-well plates).

Abstract: The present invention relates to N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives of the formula (I), (II), (III) or (IV) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such N-substituted amino-benzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives, and the use of such N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives for therapeutic purposes. The N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives are GlyT1 inhibitors.

Abstract: Provided herein are polymeric particles and compounds and processes that can be used to prepare polymer-based particles and methods of using those particles to localize or concentrate a subsequently delivered agent to an in vivo site.

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 disclosure is directed toward composite materials comprising high aspect ratio habits of drug crystals which can be partially or fully extending into a substrate, and additionally, can be projecting from a substrate at an angle of about 20° to about 90°. The present disclosure is directed toward medical devices, such as medical balloons, comprising said composite and methods of using and making the same. The described composite can be used for the local treatment of vascular disease. The present disclosure is also directed toward paclitaxel crystals with a hollow acicular habit.

Abstract: The present invention provides compositions for the treatment of cancer. The compositions include liposomes containing a phosphatidylcholine lipid, a sterol, a PEG-lipid, and a taxane. The PEG-lipid constitutes from about 2 to about 8 mol % of the lipids in the liposome. The taxane is docetaxel esterified at the 2?-O position with a heterocyclyl-(C2-5alkanoic acid). Methods for preparation of liposomal taxanes and treatment of cancer with liposomal taxanes are also disclosed.

Abstract: A method of evaluating response to a taxane drug and/or anthracycline drug, the method comprising measuring a level of a TNF biomarker in a biological sample comprising the cancer cell after contacting the cancer cell with the taxane drug and/or anthracycline drug.

Abstract: A biodegradable in vivo supporting device is disclosed. The in vivo supporting device comprises a biodegradable metal scaffold and a biodegradable polymer coating covering at least a portion of the biodegradable metal scaffold, wherein the biodegradable polymer coating has a degradation rate that is faster than the degradation rate of the biodegradable metal scaffold.

Abstract: The present invention provides methods for the treatment of tumors, comprising administration of an effective amount of at least one taxoid and an effective amount of at least one benzimidazol carbamate compound of formula (I). The invention also provides a method for the treatment of tumors insensitive to one or more anti-mitotic drugs, the method comprising administering a effective amount of at least one benzimidazole carbamate compound of formula (I). Also provide are compositions for carrying out methods of the invention.

Abstract: Disclosed are compositions and synthesis methods that pertain to biocompatible polymeric capsules capable of undergoing backbone degradation and cargo release upon exposure to biologically relevant concentrations of hydrogen peroxide (50-100 ?M of H2O2). In the invention, bio-responsive polyester bearing boronic ester triggers groups that degrade upon exposure to low concentrations of H2O2. The degradation is induced by transformation of a boronic ester to a phenol, which undergoes a quinone methide rearrangement to break down the polyester backbone.

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: A compound having the formula: wherein X is S, SO or SO2; one of R1, R2, and R3 is O and the others of R1, R2 and R3 are independently, the same or different, CH2, or CR13 wherein, R13 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)mOR15, wherein R15 is an alkyl group or an aryl group and m is an integer in the range of 1 to 10, and one of R5, R6, and R7 is O and the others of R5, R6 and R7 are independently, the same or different, CH2, or CR14 wherein, R14 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)nOR16, wherein R16 is an alkyl group or an aryl group and n is an integer in the range of 1 to 10; R4 and R8 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group, a C1-C3 alkoxy group, an aryloxy group, or —(CH2)qOR17, wherein R17 is an alkyl group or an aryl group and q is an integer in the range of 1 to 10, provided that R4 is not a C1-C3 alkoxy g

Abstract: The present invention refers to a method for inducing tumor apoptosis by influencing the ROS (reactive oxygen species) signaling pathway in tumor cells. Increasing the level of ROS leads to the selective inactivation of a tumor cell catalase and subsequently to an apoptosis of these cells. The level of ROS can be increased by increasing the level of nitric oxide through inhibition of the enzymes nitric oxide dioxygenase or arginase. According to the present invention inhibitors of the nitric oxide dioxygenase or arginase can be used for the manufacture of a medicament for the treatment of cancer. The present invention further provides a method for identifying compounds which can be used for the treatment of cancer, wherein the method allows to specifically identify compounds which induce apoptosis through the ROS signaling pathway. The present invention also provides a kit for identifying compounds which induce tumor apoptosis by inactivating a catalase on the tumor cell surface.

Abstract: Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization.

Abstract: A combination treatment taking advantage of the synergistic effect of inhibiting ?-synuclein expression and chemotherapeutic agents to provide improved treatment of cancers, preferably stage III/IV cancers. A method for identifying improved cancer treatments.

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: Compounds of structural formula (I) useful for the treatment or prophylaxis of viral infection, particularly viral influenza are provided Pharmaceutical preparations thereof and methods for their preparation are also described. The therapeutic effect is achieved via inhibition of viral neuraminidases, also known as viral sialidases. These neuraminidases are classified under the GH34 family of viral enzymes.

Abstract: The invention relates generally to an implantable medical device for delivering a therapeutic agent to the body tissue of a patient, and a method for making such a medical device. In particular, the invention pertains to an implantable medical device, such as an intravascular stent, having a coating comprising a first coating composition comprising a therapeutic agent and, optionally, a polymer; and a second coating composition comprising a metallic material.

Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.

Abstract: The present invention is directed to nanoparticulate active agent compositions comprising lysozyme as a surface stabilizer. Also encompassed by the invention are pharmaceutical compositions comprising a nanoparticulate active agent composition of the invention and methods of making and using such nanoparticulate and pharmaceutical compositions.

Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.

Abstract: The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and/or stem cells).

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: Metallocene compounds and pharmaceutical compositions containing these metallocene compounds are disclosed and described. Methods of treating cancer employing such metallocene compounds and pharmaceutical compositions also are provided.

Abstract: The invention relates to a preparation for restenosis prevention. The preparations for restenosis prevention known as yet do not reach sufficient active agent concentrations in the affected sections of the vascular walls as higher doses cause undesirable side effects. The present invention is a preparation to which at least one antihyperplastic agent is added that has a distribution ratio between butanol and water .gtoreq.0.5. The lipophilic active agent is absorbed by the vascular wall fast and in sufficient quantity. The preparation may be a liquid that can pass through capillaries and may contain a contrast agent so that the active agent is transferred into the vascular wall without any additional effort while the usually required contrast radiograms are taken. The preparation may also be applied to a catheter.

Abstract: The invention relates to a preparation for restenosis prevention. The preparations for restenosis prevention known as yet do not reach sufficient active agent concentrations in the affected sections of the vascular walls as higher doses cause undesirable side effects. The present invention is a preparation to which at least one antihyperplastic agent is added that has a distribution ratio between butanol and water .gtoreq.0.5. The lipophilic active agent is absorbed by the vascular wall fast and in sufficient quantity. The preparation may be a liquid that can pass through capillaries and may contain a contrast agent so that the active agent is transferred into the vascular wall without any additional effort while the usually required contrast radiograms are taken. The preparation may also be applied to a catheter.

Abstract: The present invention is directed to an amorphous form of cabazitaxel, which can be prepared by dissolving a solid form of cabazitaxel in an organic solvent, and removing the organic solvent to dryness. The amorphous form of cabazitaxel is characterized by DSC as in FIG. 1 and/or X-ray powder diffraction pattern as in FIG. 2.

Abstract: The invention relates to a preparation for restenosis prevention. The preparations for restenosis prevention known as yet do not reach sufficient active agent concentrations in the affected sections of the vascular walls as higher doses cause undesirable side effects. The present invention is a preparation to which at least one antihyperplastic agent is added that has a distribution ratio between butanol and water .gtoreq.0.5. The lipophilic active agent is absorbed by the vascular wall fast and in sufficient quantity. The preparation may be a liquid that can pass through capillaries and may contain a contrast agent so that the active agent is transferred into the vascular wall without any additional effort while the usually required contrast radiograms are taken. The preparation may also be applied to a catheter.

Abstract: Formulations for the oral administration of therapeutic agents, methods for administering therapeutic agents using the formulations, and methods for treating conditions and diseases using the formulations.

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: Bioactive hydroforming luminal liner compositions are formed of an absorbable crystalline amphiphilic polyether-ester-urethane dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.

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.