Abstract: The present invention relates to a composition for topical application for preventing hair loss, androgenic alopecia (AA) and stimulating hair growth having dutasteride. The composition for topical application for preventing hair loss and stimulating hair growth according to the present invention provides equal or superior hair loss prevention and hair growth stimulating effects while using much smaller dosage than the conventional compositions (oral dosage form) which use finasteride and dutasteride.

Abstract: The present invention relates to a solid pharmaceutical preparation of 3-Fluoro-4-[7-methoxy-3-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-oxo-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl]-benzonitrile, a method of making same, and medical uses thereof.

Abstract: The invention provides novel pharmaceutical compositions of berberine or a derivative or analog of berberine, or a salt thereof, in combination with one or more omega-3 fatty acids or esters thereof, and methods of their use in treating inflammatory bowel disease.

Abstract: This present invention relates to a method of treating a autoimmune, respiratory and/or inflammatory disease or condition (e.g., psoriasis, rheumatoid arthritis, asthma, COPD). The method comprises administering a PI3K Delta inhibitor or a dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor. The present invention also relates to pharmaceutical compositions containing a PI3K Delta or dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor.

Abstract: The invention relates to methods for preventing or treating resistance to EGFR inhibitors in cancer patients. More particularly, after performing a screen for small molecules potentially capable of countering cancer resistance to EGFR TKI, inventors identified the multikinase inhibitor sorafenib, which has the property, in combination with EGFR TKI, to prevent the enrichment of tumor cells containing mutations responsible for NSCLC resistance to first and third generation EGFR TKI. These data indicate that this multikinase inhibitor can prevent resistance to several generations of EGFR TKI. These in vitro data were confirmed in an in vivo xenograft mouse model of NSCLC. Finally these data were reproduced in cancer cells using SC-1, a sorafenib analogue.

Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds, and methods of using such compounds for treatment of joint damage or joint injury in a mammal, and for inducing differentiation of mesenchymal stem cells into chondrocytes.

Abstract: Disclosed is a pharmaceutical composition for preventing or treating cancer, containing streptonigrin and an mTOR inhibitor as active ingredients; and a composition for inhibiting angiogenesis, containing streptonigrin and a vascular endothelial growth factor (VEGF) inhibitor as active ingredients. Also disclosed is a cancer treatment method using streptonigrin and an mTOR inhibitor, a use in the preparation of anticancer drugs and a composition to be used in cancer prevention or treatment; and a method for inhibiting angiogenesis by using streptonigrin and a VEGF inhibitor, a use in the preparation of drugs for inhibiting angiogenesis and a composition to be used in angiogenesis inhibition. When a renal cancer cell line is treated with streptonigrin, which is a TGase2 inhibitor, in combination with rapamycin, which is an mTOR inhibitor, a cancer cell death effect can be exhibited to be greater than that when cancer cells are treated with each thereof, individually.

Abstract: Methods for the treatment of Alzheimer's disease psychosis, or a symptom thereof, comprising administering pimavanserin. Also provided herein are methods for the treatment of delusions and/or hallucinations in a human with dementia comprising administering pimavanserin, or a pharmaceutically acceptable salt thereof. Also provided herein are methods for reducing NPI-NH score in a human with Alzheimer's Disease comprising administering pimavanserin, or a pharmaceutically acceptable salt thereof. Also provided herein are methods for reducing agitated behavior or aggressive behavior in a human with dementia comprising administering pimavanserin, or a pharmaceutically acceptable salt thereof.

Abstract: Provided herein are lyophilized formulations of 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide or a stereisomer or mixture of stereisomers, pharmaceutically acceptable salt, tautomer, prodrug, solvate, hydrate, co-crystal, clathrate, or polymorph thereof. Methods of using the formulations and dosage forms for treating, managing, and/or preventing cancer are also provided herein.

Abstract: A method of promoting increased cellular hydration in a multicellular organism that is capable of intracellular water permeation includes the step of causing the multicellular organism to ingest an aqueous solution that contains an amount of a carbohydrate clathrate component. There is also a step of enhancing the intracellular permeation. The multicellular organism contains aquaporins, and the causing step involves interaction of the composition with the aquaporins. The cellular hydration promoted and caused by the method is corroborated by a test that uses human-aquaporin-expressed frog oocytes. The test uses single cell Xenopus laevis frog oocytes having expressed human aquaporin AGP1 water channels. There is also a beverage composition that increases lifespan in the multicellular organism, and a beverage composition that promotes cellular hydration when ingested by a multicellular organism.

Abstract: The present technology is directed to one or more compositions comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology also relates to one or more compositions and oral formulations comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology also relates to one or more methods of using compositions comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof. The present technology additionally relates to one or more pharmaceutical kits containing a composition comprising serdexmethylphenidate conjugates and unconjugated d-methylphenidate and/or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to the use of a calcium release-activated calcium (CRAC) channel modulator, such as N-[4-(3,5-dicyclopropyl-1H-pyrazol-1-yl)phenyl]-2-(quinolin-6-yl)acetamide (Compound (A)) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing such a CRAC channel modulator for the treatment of esophageal cancer.

Abstract: The present invention relates to pharmaceutical compositions comprising a quinolone carboxylic acid derivative antimicrobial agent and an effervescent agent. These compositions have improved gastrointestinal tolerability and/or reduced potential to cause gastrointestinal side effects. These compositions are useful for oral administration, for treating, preventing, or reducing the risk of microbial infections.

Abstract: An aqueous drug in which the chemical decomposition of the compound represented by formula (1) or of a salt thereof is inhibited, and a method for producing said aqueous drug. An aqueous drug provided with: a solution (liquid A) that contains the compound represented by formula (1) or a salt thereof and that has a pH of 5.3 or less; and a dilution liquid (liquid B) that is mixed with the liquid A in order to prepare a solution to be administered.

Abstract: Conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to an HSP90 targeting moiety via a linker have been designed. Nanoparticles and microparticles comprising such conjugates can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or other diseases.

Abstract: The invention relates to (among other things) a method comprising the steps of (a) administering to a patient a PARP-inhibiting amount of a PARP inhibitor; and (b) administering to the patient a topoisomerase I-inhibiting amount of a long-acting topoisomerase I inhibitor.

Abstract: A transdermal therapeutic system for the transdermal administration of buprenorphine comprising a buprenorphine-containing self-adhesive layer structure having (A) a buprenorphine-impermeable backing layer, and (B) a buprenorphine-containing pressure-sensitive adhesive layer on the backing layer. The buprenorphine-containing adhesive layer comprises (a) at least one polymer-based pressure-sensitive adhesive, (b) an analgesically effective amount of buprenorphine base or a pharmaceutically acceptable salt thereof, (c) a viscosity-increasing substance in an amount of about 0.1% to about 8% of the buprenorphine-containing pressure-sensitive adhesive layer, and (d) a carboxylic acid selected from oleic acid, linoleic acid, linolenic acid, levulinic acid and mixtures thereof. The amount of the carboxylic acid is sufficient so that the analgesically effective amount of buprenorphine is solubilized in the carboxylic acid to form a mixture including the viscosity-increasing substance.

Abstract: Pharmaceutical compositions of one or more opioid antagonists or phosphodiesterase 5 (PDE5) inhibitors are disclosed.

Abstract: The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related disorders.

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: 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: Delayed-release pharmaceutical compositions prepared by hot-melt extrusion are provided, where the compositions comprise an azole anti-fungal drug having poor water solubility, an enteric polymer and a non-enteric polymer, and wherein the pharmaceutical composition may be orally administered to a patient in either the fed or fasted state. Preferably, the delayed-release pharmaceutical compositions prepared by hot-melt extrusion comprise posaconazole, HPMC-AS and HPC. Preferably, following oral administration of the pharmaceutical compositions, there is no substantial difference in the pharmacokinetic parameters (Tmax, Cmax, AUC0-t and/or AUC0-infinity) of the azole anti-fungal drug, regardless of whether the pharmaceutical compositions are administered to a subject in the fed or fasted state.

Abstract: Disclosed herein are compounds that can bind to tubulin and activate GEF-H1. Methods of using these compounds for treating cancer are also disclosed.

Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.

Abstract: The present disclosure relates to pharmaceutical compositions comprising N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino)-benzamide and a polymer, dosage forms comprising the formulation and methods of treating subjects having cancer.

Abstract: The present invention covers 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and R6 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with 10 dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.

Abstract: The invention relates to the methods for identifying resistance to cancer therapy, by identification of an E63K NRAS mutation, a G12V NRAS mutation or a gain of copy number of NRAS gene. A further aspect of the invention relates to methods of treatment that may overcome such resistance mechanisms, involving the use of an EGFR inhibitor in combination with a MEK inhibitor for the treatment of cancers involving an NRAS mutation selected from E63K, G12V, G12R, G12A, G12D, G12S and G12C, and/or cancer involving a gain of copy number of NRAS gene.

Abstract: There is provided a daily dosage regimen for treating pulmonary arterial hypertension. The regimen takes the form of two discrete dosage forms. Each dosage form includes an amount of about 600 mg to about 800 mg of (S)-ethyl 8-(2-amino-6-((R)-1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-3-carboxylate. There is also another method for providing a daily dosage regimen. There is also provided several methods for treating pulmonary arterial hypertension. There is provided a method for reducing the level of serotonin biosynthesis by at least 50%. There is also provided a method for achieving an AUC0-tau of ?2530 ng·hr/mL of (S)-8-(2-amino-6-((R)-1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-3-carboxylic acid. There is provided a method of achieving a >50% reduction in urinary 5-HIAA.

Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.

Abstract: The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of compound formula (I).

Abstract: The present invention relates to the use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination.

Abstract: Described inter alia are compounds according to formula (I): or a pharmaceutically acceptable salt thereof, and uses in methods for the modulation of flap endonuclease 1 (FEN1), Xeroderma Pigmentosum Complementation Group G protein (XPG), Exonuclease 1 (EXO1) and/or GEN1.

Abstract: Disclosed are methods for treating a cancer in a patient. The method comprises: (a) defining a set of substances targeting pathogenic genes identified by screening of a sample of cancer cells from a patient by NGS or other technique, (b) identifying two or more target genes in the cancer cells, each of which containing an actionable mutation and (c) testing, using in vitro culture cell experiments, the efficacy of one or more substances (administered sequentially or concurrently) targeting the actionable mutation for each of the two or more target genes identified and (d) designating potential efficacious therapeutic options that will be used to treat the patient's cancer.

Abstract: A method of treating a pediatric cancer in a subject in need thereof. The method includes administering to the subject a therapeutically effective amount of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, or a pharmaceutically acceptable salt thereof, or a combination thereof.

Abstract: Combination therapies for treatment of cancer are provided. The disclosed methods comprise administration of a PKM2 activator and an anti-cancer drug having a mechanism of action that increases production of reactive oxygen species in cancer cells to a patient in need thereof.

Abstract: Provided are formulations and dosage forms of cis-4-[2-{[(3S,4R)-3-fluorooxan-4-yl]amino}-8-(2,4,6-trichloroanilino)-9H-purin-9-yl]-1-methylcyclohexane-1-carboxamide, alternatively named (1s,4s)-4-(2-(((3S,4R)-3-fluorotetrahydro-2H-pyran-4-yl)amino)-8-((2,4,6-trichlorophenyl)amino)-9H-purin-9-yl)-1-methylcyclohexane-1-carboxamide, or a pharmaceutically acceptable salt, tautomer, solvate, hydrate, co-crystal, clathrate, or polymorph thereof.

Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.

Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising a phosphodiesterase type 5 inhibitor and/or a salt thereof, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.

Abstract: The present invention relates to therapeutic combinations of anti-bacterial agents linezolid, bedaquiline and pretomanid, and optionally with pyrazinamide, in a short-course oral dosage regimen for the treatment of tuberculosis.

Abstract: Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis.

Abstract: Provided are immediate or prolonged administration of certain potassium ATP (KATP) channel openers to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of KATP channel openers that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering KATP channel openers with other drugs to treat diseases of humans and animals.

Abstract: This invention relates to a pharmaceutical combination comprising (a) a third generation EGFR tyrosine kinase inhibitor and (b) a Raf inhibitor, particularly for use in the treatment of a cancer, particularly a lung cancer. This invention also relates to uses of such a combination for the preparation of a medicament for the treatment of a cancer; methods of treating a cancer in a subject in need thereof comprising administering to said subject a jointly therapeutically effective amount of said combination; pharmaceutical compositions comprising such combination and commercial packages thereto.

Abstract: A method of forming a dietary supplement can include steps of creating a composition of matter comprising sakae naa and CDP; and providing the composition of matter in a liquid or solid form. Providing the composition of matter can include filling a container with the composition of matter.

Abstract: A method of forming a dietary supplement can include steps of creating a composition of matter comprising sakae naa and GPC; and providing the composition of matter in a liquid or solid form. Providing the composition of matter can include filling a container with the composition of matter.

Abstract: A method of forming a dietary supplement can include steps of creating a composition of matter comprising kava and CDP; and providing the composition of matter in a liquid or solid form. Providing the composition of matter can include filling a container with the composition of matter.

Abstract: A method of forming a dietary supplement can include steps of creating a composition of matter comprising kava and GPC; and providing the composition of matter in a liquid or solid form. Providing the composition of matter can include filling a container with the composition of matter.

Abstract: A method of forming a dietary supplement can include steps of creating a composition of matter comprising CDP and GPC; and providing the composition of matter in a liquid or solid form. Providing the composition of matter can include filling a container with the composition of matter.

Abstract: The present invention is directed to the combination therapy of multiple myeloma with a BET inhibitor and a Bcl-2 inhibitor.

Abstract: Embodiments include a system including a sealed prefilled drug-reservoir. The drug-reservoir may include a unit dosage of treprostinil in a sterile fluid composition. The composition may not include an antimicrobial preservative. The treprostinil may be present at a dosage of between 0.1 mg/mL and 25 mg/mL. In addition, the treprostinil may be treprostinil sodium Furthermore, the composition may include sodium chloride. The composition may also include a sodium ion from sodium chloride in a concentration from 3000 to 4500 ppm. The composition may not include metacresol.

Abstract: The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.