Abstract: Lipid nanoparticles and compositions thereof are disclosed herein. An exemplary nanoparticle composition includes an ionizable lipid, a phospholipid, a PEG-lipid, and a cholesterol modified with a hydroxyl group near the D-sterol ring. The disclosed nanoparticle compositions can target liver Kupffer cells and endothelial cells more preferentially than hepatocytes which should be beneficial in treating liver diseases in which dysfunctional Kupffer cells and endothelial cells are involved in disease pathogenesis.

Abstract: Currently available glutaminase inhibitors are generally poorly soluble, metabolically unstable, and/or require high doses, which together reduce their efficacy and therapeutic index. These can be formulated into nanoparticles and delivered safely and effectively for treatment of pancreatic cancer and other glutamine addicted cancers. Studies demonstrate that nanoparticle delivery of BPTES, relative to use of BPTES alone, can be safely administered and provides dramatically improved tumor drug exposure, resulting in greater efficacy. GLS inhibitors can be administered in higher concentrations with sub-100 nm nanoparticles, since the nanoparticles package the drug into “soluble” colloidal nanoparticles, and the nanoparticles deliver higher drug exposure selectively to the tumors due to the enhanced permeability and retention (EPR) effect. These factors result in sustained drug levels above the IC50 within the tumors for days, providing significantly enhanced efficacy compared to unencapsulated drug.

Abstract: Provided are methods of treating a cancer (such as lung cancer, breast cancer, pancreatic cancer, etc.) in an individual in need thereof, comprising administering to the individual a) an effective amount of a composition comprising nanoparticles comprising a taxane (such as paclitaxel) and an albumin (such as human serum albumin), and b) an effective amount of ABT-263.

Abstract: The present invention relates to a transdermal therapeutic system (TTS) comprising an active agent-containing layer structure comprising A) a backing layer and B) a biphasic matrix layer, the biphasic matrix layer having a) a continuous, outer phase having a composition comprising 70 to 100% by weight of at least one polymer, b) a discontinuous, inner phase having a composition comprising the active agent and a dissolver for the active agent in amount sufficient so that the active agent forms a solution with the dissolver in the inner phase and c) an emulsifier in an amount of 0.1 to 20% by weight based on the biphasic matrix layer, processes of manufacture and uses thereof, corresponding methods of treatments therewith.

Abstract: The present invention relates to a use of pinitol, D-chiro-inositol or an analog thereof in preventing, alleviating or treating premenstrual syndrome. According to the present disclosure, pinitol, D-chiro-inositol, or an analog thereof can be developed into a drug or a nutraceutical for prevention, alleviation, or treatment of premenstrual syndrome thanks to the alleviative effect thereof on the main symptoms of premenstrual syndrome inclusive of dysmenorrhea, a period of dysmenorrhea, and coldness of hands and feet, and may elicit few side effects when applied to the human body because they are derived from natural products.

Abstract: Embodiments of the present disclosure pertain to formulations for cancer treatment that include a particle loaded with diethylstilbestrol (DES) and a pharmaceutically acceptable carrier. The pharmaceutically acceptable carrier may also be loaded into the particle. The formulations may also include a stabilizer that is also loaded into the particle. The particles may be dispersed in an aqueous solution to form a nanosuspension that is adapted for subcutaneous administration and sustained release of DES. Additional embodiments pertain to methods of treating cancer in a subject by administering to the subject a formulation of the present disclosure. The subject may be a human suffering from prostate cancer. The administration of the formulations to the subject may bypass or minimize first pass metabolism. The administration may also minimize hepatic exposure of DES. Additional embodiments pertain to methods of making the formulations of the present disclosure by loading a particle with DES.

Abstract: The present invention is directed to methods and dosing regimens for the treatment of depression (preferably, treatment resistant depression), for the treatment of depression in a suicidal patient, and/or for the treatment and/or prevention of suicidality (e.g. suicidal ideations).

Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Abstract: Drug combinations and their use are disclosed. A first drug is administered in combination with a second drug. The first drug such as fenfluramine is characterized by the formation of a metabolite including 5-HT2B agonists such as norfenfluramine with known adverse side effects. The second drug is in the form of a CYP inhibitor such as cannabidiol which modulates the formation of metabolite down thereby making the first drug safer.

Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.

Abstract: The present invention provides a pharmaceutical composition containing gossypol and phenformin, capable of exhibiting a synergistic effect in the treatment of pancreatic cancer. When gossypol and phenformin are mixed in a concentration range provided in the present invention and the mixture is applied to the treatment of pancreatic cancer, apoptotic effects on pancreatic cancer are remarkably increased because of the co-administration thereof even in a concentration range in which a significant pancreatic cancer treatment effect cannot be achieved by the administration of gossypol or phenformin alone, such that pancreatic cancer can be effectively treated. Additionally, when an anti-cancer agent is mixed in addition to gossypol and phenformin and the mixture is applied to the treatment of pancreatic cancer, apoptotic effects on cancer cells can be remarkably increased such that pancreatic cancer can be effectively treated.

Abstract: Method of using ureidomustine (BO-1055), a water-soluble NDA cross-linking agent, in the treatment of small lung cell carcinoma (SCLC).

Abstract: Methods of treating or preventing cancer, diabetes, and/or obesity in a subject are provided. The methods comprise administering to a subject a therapeutically effective amount of an SLC25A1 inhibitor as described herein. Also provided herein are pharmaceutical compositions comprising an SLC25A1 inhibitor and a chemotherapeutic agent. Further provided herein are methods of inhibiting SLC25A1 in a cell.

Abstract: The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

Abstract: Pharmaceutical compositions that include aqueous suspensions of therapeutically effective quantity of a diaminopyrimidine compound (such as pyrimethamine) are provided herein. Methods for fabricating and using the compositions, and kits that include the compositions are also described.

Abstract: A composition for preventing, treating, reversing, protecting against ameliorating the injuring effect of an ionizing radiation upon living cells, tissues, organs, and organisms, comprising oil palm phenolics (OOP) or vegetation liquor extract obtained from aqueous stream of a palm oil milling effluent is provided.

Abstract: The present invention provides a method for treating or preventing gout in a subject afflicted therewith comprising administering a compound presented or an ester or salt thereof, so as to thereby treat or prevent the gout in the subject.

Abstract: A drug combination with antitumor effects contains styrene acid derivatives and antitumor medicaments with same or different specifications of unit preparations that can be simultaneously or separately administrated, as well as pharmaceutically acceptable carriers. The joint use of trans-styrene acid derivatives and antitumor drugs provides synergistic action, and the use of trans-styrene acid derivatives combined with a part of antitumor drugs can further exert the toxicity attenuation effects, showing a good clinical application prospect.

Abstract: The inventors have unexpectedly discovered that shock and/or potential multi-organ failure due to shock can be effectively treated by administration of liquid high-dose protease inhibitor formulations to a location upstream of where pancreatic proteases are introduced into the gastrointestinal tract. Most preferably, administration is directly to the stomach, for example, via nasogastric tube under a protocol effective to treat shock by such administration without the need of providing significant quantities of the protease inhibitor to the jejunum and/or ileum.

Abstract: The present invention relates to methods of treating overactive bladder and the symptoms associated therewith, for example, urinary urgency, frequency of micturitions, nocturia, and urgency urinary incontinence. One treatment method according to the present invention comprises treatment with the beta-3 adrenergic receptor agonist solabegron. Another treatment combination according to the invention comprises solabegron, and a muscarinic receptor antagonist which results in a synergistic effect on the symptoms associated with OAB.

Abstract: Methods of treating tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction with (1S,3S)-3-amino-4-(difluoromethylidene) cyclopentane-1-carboxylic acid or a pharmaceutically acceptable salt thereof are provided. Methods of treating tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction with (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid are provided. Also provided are therapeutic compositions that may be used to improve one or more symptoms of tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction.

Abstract: Fixed-dose combination drugs comprising an NSAID as a first drug component and a GABA-type calcium channel blocker as a second drug component are contemplated. Further contemplated aspects also include methods of administration of combination drugs and drugs contained herein.

Abstract: The present disclosure provides a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are defined herein. The disclosure also relates to a method for manufacturing the compounds of the disclosure, and its therapeutic uses. The present disclosure further provides pharmaceutical composition of the compounds of the disclosure and a combination of pharmacologically active agents and a compound of the disclosure.

Abstract: The present invention provides methods, compositions, and kits for treating anxiety-related disorders, including OCD and SAD, and for reducing anxiety, obsessive behavior, or compulsive behavior in subjects in need thereof.

Abstract: Disclosed are novel formulations of oral tetraiodothyronine (T4), characterised by the formation in aqueous media of soluble, bioavailable micellar nanoaggregates.

Abstract: The present invention relates to a composition for preventing or treating asthma, having, an active ingredient, a saturated or unsaturated fatty acid having 12 to 22 carbon atoms. The saturated or unsaturated fatty acid functions to inhibit or eliminate various asthma symptoms induced by ovalbumin. Specifically, the fatty acid inhibits the proliferation of leukocytes, neutrophils, lymphocytes and monocytes in BALF and serum, inhibits the proliferation of bronchial epithelial cells, reduces mucus in bronchioles, and reduces infiltration of inflammatory cells around bronchioles and blood vessels in a dose-dependent manner. Also, the fatty acid induces a decrease in the expression of IFN-?, IL-12p40, IL-4, IL-5, IL-13 and TNF-?, which are Th2 cell-related cytokines. Therefore, the fatty acid overcomes the side effects of current asthma therapeutic agents, has an excellent therapeutic effect without having toxicity, and may advantageously be used as a composition for preventing, treating or alleviating asthma.

Abstract: Novel compositions comprising omega-3 fatty acids and uses thereof are disclosed.

Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.

Abstract: The disclosure relates to compositions containing allyl isothiocyanate and methods of use thereof for stimulating tearing in a subject to treat dry eye.

Abstract: Provided are a long-acting prodrug of Rasagiline, which has application in the treatment of Central Nervous System diseases such as Parkinson's disease, preparation method and use thereof. The long-acting prodrug of Rasagiline has a structure of formula (I), wherein T is absent, or T is selected from each of R1 and R2 is independently selected from H, D, and alkyl; W is absent, or W is selected from (CH2)n, wherein n is an integer selected from 1 to 15; X is absent, or X is selected from (CH2)m, wherein m is an integer selected from 1 to 10; Y is absent, or Y is selected from —C(?O)NH—, —NHC(?O)—; R3 is selected from substituted or unsubstituted C1-C30 alkyl, substituted or unsubstituted C2-C30 alkenyl, substituted or unsubstituted C2-C30 alkynyl, substituted or unsubstituted C3-C30 cycloalkyl, cholane aliphatic group, —R3a—C(?O)O—R3b, —R3a—OC(?O)—R3b, —R3a—C(?O)NH—R3b, —R3a—NHC(?O)—R3b, —R3a—S(?O)1-2O—R3b and —R3a—OS(?O)1-2—R3b.

Abstract: This invention addresses tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73, AV2-73, or A2-73) in a method of treatment for neurodevelopmental disorders. Particular reference is made to the treatment of autism spectrum disorder, cerebral palsy, Rett syndrome, Angelman syndrome, Williams syndrome, pervasive developmental disorder not otherwise specified (PDD-NOS), childhood disintegrative disorder, and Smith-Magenis syndrome. Additional reference is made to multiple sclerosis.

Abstract: The present invention relates to: a 4-benzopyranone derivative and a pharmaceutically acceptable salt, solvate, racemate, or stereoisomer thereof; a composition for preventing, alleviating or treating TNF-related diseases, containing the same as an active ingredient; and a method for treating TNF-related diseases, a reagent composition for inhibiting TNF, and a method for inhibiting TNF, all of which use the same. The compositions can be orally administered so as not to cause injection side effects, do not cause immunological tolerance, and can effectively inhibit a TNF activity by being directly bound to TNF while facilitating co-administering with a conventional oral preparation and dosage control.

Abstract: A pathophysiological effect of a transient receptor potential cation channel, subfamily V, member 3 (TRPV3) on psoriasis, which can be used to develop a drug for preventing or treating psoriasis. The invention further discloses an application of Scutellarein as a TRPV3 inhibitor in preparing a drug for preventing or treating psoriasis. When a drug containing the TRPV3 inhibitor discovered according to the invention or provided by the invention is used for preventing or treating psoriasis, good prevention or treatment effects can be achieved.

Abstract: The present invention relates to pharmaceutical compositions formulated for transmucosal delivery, and in particular sublingual delivery, comprising at least one tocotrienol or derivative thereof together with one or more pharmaceutically acceptable excipients. The present further relates to the use of said compositions for treating or preventing post exercise muscle soreness, delayed onset muscle soreness, cardiac fibrosis, hypertension, inflammation, stroke, cancer, elevated cholesterol and/or triglycerides, baldness, hypertrophy, conditions resulting from radiation exposure, stabilizing and/or controlling blood glucose levels, and improving exercise endurance and capacity.

Abstract: The present invention relates to a composition for inhibiting the growth of cancer stem cells, which includes ciclesonide or a pharmaceutically acceptable salt thereof as an active ingredient, a pharmaceutical composition or food composition for inhibiting cancer metastasis, or treating or preventing cancer, which includes the composition, and the like. Ciclesonide of the present invention inhibits the growth of breast cancer cells and lung cancer cells, and inhibits the formation of breast cancer stem cells and lung cancer stem cells.

Abstract: A synergistic combination of Urolithin A (3,8-dihydroxy-dibenzo-alpha-pyrone) and Urolithin B (3-hydroxy-dibenzo-alpha-pyrone) is provided in a particular effective ratio, optionally in a nutraceutical or pharmaceutical composition. The composition is for use in treating cognitive deficits, including increasing cognitive function or cognitive capacity (nootropic activity). The composition is for use in treating or preventing a dementia-related disorder in a human subject, such as anxiety or Alzheimer's disease, and for inhibition of acetylcholinesterase (AChE).

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating pruritus, containing a pyrazole derivative as an active ingredient, and a screening method for detecting the same. A pharmaceutical composition for preventing or treating pruritus, according to the present invention, can relieve the symptoms of pruritus by inhibiting the activity of intracellular Mrgpr X1, and can relieve the symptoms of pruritus by inhibiting the activity of intracellular hH1R, thereby being usable also as a medicine for preventing or treating histamine-mediated pruritus. In addition, it has been confirmed through dry skin mouse model experimentation that the composition also has significant alleviation effects on dry skin, thereby being usable as a medicine for treating dry skin. Furthermore, the pharmaceutical composition according to the present invention can relieve the symptoms of pruritus caused by psoriasis, thereby being usable also as a medicine for treating psoriasis.

Abstract: The invention provides methods, compositions, and kits containing an alpha-adrenergic antagonist, such as phentolamine, for use in monotherapy or as part of a combination therapy to treat patients suffering from presbyopia, mydriasis, and/or other ocular disorders.

Abstract: A nasal pharmaceutical composition comprising a decongestant compound selected from xylometazoline or a pharmaceutically acceptable salt of xylometazoline, oxymetazoline or a pharmaceutically acceptable salt of oxymetazoline, menthol; dexpanthenol and hyaluronic acid or a pharmaceutically acceptable salt of hyaluronic acid.

Abstract: The present invention relates to an oral pharmaceutical composition comprising bendamustine in combination with a modified cyclodextrin, such as, e.g., methyl-ß-cyclodextrin or hydroxypropyl-ß-cyclodextrin. It has surprisingly been found in the context of the invention that such compositions exhibit a greatly improved oral bioavailability, which renders them particularly advantageous for oral therapeutic application, e.g., in the treatment of cancer.

Abstract: The invention is directed to a method of inhibiting prostate cancer cell proliferation using a substance that inhibits the activity of soluble adenylyl cyclase (sAC) protein. The invention also is directed to methods of diagnosing and prognosticating prostate cancer in a subject by evaluating sAC gene expression or sAC protein production in the subject.

Abstract: This invention provides a combination-drug composition and a combination use of pharmaceuticals for preventing and/or treating dyslipidemic conditions such as hyper-LDL cholesterolemia in mammals, including humans. This invention pertains to a drug composition for preventing and/or treating dyslipidemia and the like, the drug composition including the following: (R)-2-[3-[[N-(benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy] butyric acid, a salt thereof, or a solvate of either; and nicotinic acid and nicotinic-acid amide, collectively referred to as niacin, an ester derivative thereof, a salt thereof, or a solvate of any of these.

Abstract: An FGF21 production promoting agent containing, as an active ingredient, a compound represented by the following formula (1): wherein each of R1 and R2, which may be identical to or different from each other, represents, for example, a hydrogen atom; each of R3a, R3b, R4a, and R4b, which may be identical to or different from one another, represents, for example, a hydrogen atom or a halogen atom, or R3a and R3b or R4a and R4b may bond together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents, for example, a hydrogen atom or a C1-4 alkyl group); Y represents, for example, an oxygen atom, an S(O)l group (l is a number of from 0 to 2), or a carbonyl group; Z represents CH or N; n is a number of from 1 to 6; and m is a number from 2 to 6, a salt of the compound, or a solvate the compound or the salt.

Abstract: Methods of treating post-surgical pain are provided. The methods include administering to an individual a therapeutically effective amount of a compound of Formula I (Compound 1). The method can be used to treat post-surgical pain arising from any surgical procedure without the side effects associated with widely used analgesics such as opioids. Compound 1 can be formulated into many suitable dosage forms, including oral dosage forms such as tablets.

Abstract: Methods of treating diabetic neuropathy and pain associated with diabetes are provided. The methods include administering to an individual a therapeutically effective amount of a compound of Formula I (Compound 1). The method can be used to treat diabetic neuropathy pain arising from type I or type II diabetes. Compound 1 can be formulated into many suitable dosage forms, including oral dosage forms such as tablets.

Abstract: Methods of treating diabetic neuropathic pain and post-surgical pain are provided. The methods include administering to an individual a therapeutically effective amount of a compound of Formula I (Compound 1). The method can be used to treat diabetic neuropathy arising from any type of nerve damage, and can also be used to treat post-surgical pain arising from any surgical procedure without the side effects associated with widely used analgesics such as opioids. Compound 1 can be formulated into many suitable dosage forms, including oral dosage forms such as tablets.

Abstract: The present invention relates to a method for preparing a pharmaceutical composition for preventing or treating a cognitive impairment-related disease and a pharmaceutical composition for preventing or treating a cognitive impairment-related disease prepared by the same, and the pharmaceutical composition includes microparticles including donepezil and a biodegradable polymer, and the microparticles are in a form in which donepezil is uniformly distributed in a spherical biodegradable polymer. The present invention may maintain the effect of preventing or treating the cognitive impairment-related disease for 1 month by a single injection in order to eliminate the inconvenience of having to take the composition daily, and as the present invention is prepared by maintaining the average diameters of the particles at a predetermined micrometer size, a foreign body sensation and pain during administration into a patient as an injection is reduced, thereby enabling administration as an injection to be facilitated.

Abstract: Provided herein are stable amlodipine oral liquid formulations. Also provided herein are methods of using amlodipine oral liquid formulations for the treatment of certain diseases including hypertension and Coronary Artery Disease (CAD).

Abstract: Disclosed herein are compositions and methods for delivering adipose tissue browning agents and/or fat modulating agents.

Abstract: A method for treating gluten-related allergies and gluten intolerance is provided. The method includes administering to a patient an effective amount of a drug having loperamide as an active ingredient; specifically, wherein the patient suffers from gluten-related allergies and/or gluten intolerance.