anthonyyazdaniml/gliner-biomed-curated-corpus huggingface dataset:
Macitentan

Endothelin (ET)-1 and its receptors (ETA and ETB) mediate a variety of deleterious effects, such as vasoconstriction, fibrosis, proliferation, hypertrophy, and inflammation. In disease conditions such as PAH, the local ET system is upregulated and is involved in vascular hypertrophy and in organ damage.

Macitentan is an endothelin receptor antagonist that inhibits the binding of ET-1 to both ETA and ETB receptors. Macitentan displays high affinity and sustained occupancy of the ET receptors in human pulmonary arterial smooth muscle cells. One of the metabolites of macitentan is also pharmacologically active at the ET receptors and is estimated to be about 20% as potent as the parent drug in vitro. The clinical impact of dual endothelin blockage is unknown. 

Tadalafil

Tadalafil is an inhibitor of phosphodiesterase type 5 (PDE5), the enzyme responsible for the degradation of cyclic guanosine monophosphate (cGMP). PAH is associated with impaired release of nitric oxide by the vascular endothelium and consequent reduction of cGMP concentrations in the pulmonary vascular smooth muscle. PDE5 is the predominant phosphodiesterase in the pulmonary vasculature. Inhibition of PDE5 by tadalafil increases the concentrations of cGMP resulting in relaxation of pulmonary vascular smooth muscle cells and vasodilation of the pulmonary vascular bed.

Studies in vitro have shown that tadalafil is a selective inhibitor of PDE5. PDE5 is an enzyme found in corpus cavernosum, vascular smooth muscle, visceral smooth muscle, skeletal muscle, platelets, kidney, lung, and cerebellum. The effect of tadalafil is more potent on PDE5 than on other phosphodiesterases. Tadalafil is > 10,000-fold more potent for PDE5 than for PDE1, PDE2, PDE4 and PDE7, enzymes which are found in the heart, brain, blood vessels, liver, and other organs. Tadalafil is > 10,000-fold more potent for PDE5 than for PDE3, an enzyme found in the heart and blood vessels. This selectivity for PDE5 over PDE3 is important because PDE3 is an enzyme involved in cardiac contractility. Additionally, tadalafil is approximately 700-fold more potent for PDE5 than for PDE6, an enzyme which is found in the retina and is responsible for phototransduction. Tadalafil is also > 9,000-fold more potent for PDE5 than for PDE8, PDE9 and PDE10.
BACKGROUND & AIMS: Early enteral nutrition (EEN) potentially improves immune-related outcomes via the maintenance of intestinal immunity; however, the effects of EEN on clinical outcomes, including infectious complications, are controversial. Therefore, we herein investigated whether EEN affected persistent inflammation, immunosuppression, and catabolism syndrome (PICS), which represents the immunocompromised state after critical illness.
METHODS: This retrospective cohort study utilized the administrative claims database of inpatients and laboratory findings. Patients admitted to and treated in the intensive care unit (ICU) for more than 3 consecutive days were included. The primary outcome, a composite of PICS or mortality on day 14 after admission, was compared between the EEN group, which received enteral nutrition (EN) on the first 3 days (day 0, 1, or 2), and the late enteral nutrition (LEN) group, which did not receive EN on the first 3 days, but then received EN on days 3 through 7, using a propensity score-matched analysis. Secondary outcomes included the composite outcome on day 28, in-hospital mortality, the Barthel index, and laboratory data. Patients who met at least two of the following conditions were diagnosed with PICS: CRP >2.0 mg/dL, albumin <3.0 g/dL, and a lymphocyte count <800/μL.
RESULTS: A total of 7530 matched pairs were generated after propensity score matching. The primary outcome was significantly lower in the EEN group (risk difference -3.0%, 95% confidence interval (CI) -4.5 to -1.4%), whereas mortality did not significantly differ. The 28-day composite outcome was similar in the 2 groups (risk difference -1.5%, 95% CI -2.8% to -0.2%, no significant difference in mortality). There was no significant difference in in-hospital mortality between the EEN and LEN groups; however, the Barthel index at discharge was higher in the EEN group (the medians, 50 vs 45, P = 0.001). Laboratory data showed lower Albumin and CRP on day 14 in the EEN group, but no other significant differences.
CONCLUSIONS: In patients admitted to the ICU, EEN was associated with a lower incidence of PICS on days 14 and 28, but was not associated with mortality. This positive association was not observed in sepsis, cardiac diseases, or gastrointestinal diseases.
FIELD: chemical-pharmaceutical industry, gynecology. SUBSTANCE: preparation consists of the first component, i. e. biogenic estrogen, synthetic estrogen and gestagen and if necessary one or some additional components. The latter consist of pharmaceutically acceptable placebo or biogenic or synthetic gestagen or estrogen, or of combination of three agents, or combination of synthetic estrogens and gestagen and also of pharmaceutical container for contraception. Invention provides a new combination of substances for by stage intake at decreased amount of hormones to be administrated. EFFECT: enhanced effectiveness of preparation. 8 cl, 6 tbl, 13 ex
Comparative clinical trials of otitis media were conducted in nearly 400 children between the ages of 6 months to 10 years. Streptococcus pneumoniae was isolated from 47% of the patients, Haemophilus influenzae from 34%, Moraxella catarrhalis from 15% and S. pyogenes from 4%.

The overall response rate of Streptococcus pneumoniae to cefixime was approximately 10% lower and that of Haemophilus influenzae or Moraxella catarrhalis approximately 7% higher (12% when beta-lactamase positive isolates of H. influenzae are included) than the response rates of these organisms to the active control drugs.

In these studies, patients were randomized and treated with either cefixime at dose regimens of 4 mg/kg twice a day or 8 mg/kg once a day, or with a comparator. Sixty-nine to 70% of the patients in each group had resolution of signs and symptoms of otitis media when evaluated 2 to 4 weeks post-treatment, but persistent effusion was found in 15% of the patients. When evaluated at the completion of therapy, 17% of patients receiving cefixime and 14% of patients receiving effective comparative drugs (18% including those patients who had Haemophilus influenzae resistant to the control drug and who received the control antibacterial drug) were considered to be treatment failures. By the 2 to 4 week follow-up, a total of 30%-31% of patients had evidence of either treatment failure or recurrent disease.
P-QST has been shown to be able to phenotype patients with CP into nociceptive patterns according to degree of central sensitization. As a tool to identify baseline nociceptive pattern in patients with painful CP, P-QST will be performed at baseline prior to planned invasive treatment with endoscopic therapy or decompressive surgery. We will evaluate the ability of P-QST to predict response to invasive treatment for painful CP, and to develop a predictive model for individualized prediction of treatment response.

Patients will undergo pre-procedure P-QST testing before undergoing scheduled invasive treatment as directed by their treating gastroenterologist. The date of first endoscopic therapy or surgery will be used to calculate follow-up timepoints, which will be scheduled at 3, 6, and 12 months after the first endotherapy session or surgery. At each follow-up time point, patients will answer questions about their pain. In addition, patients will complete patient reported outcome tools (HADS, PCS instruments) and the Patient Global Impression of Change. Serum and urine samples will be obtained at baseline and at 6-month follow-up timepoints.
1. Technical Result Increase in efficiency of treatment or prevention of atherosclerosis. 2. Essence A compound of the formula Wherein Ar1, Ar2, R1, R26 have the values indicated in the description; pharmaceutical composition for treatment or prevention of atherosclerosis comprises said compound and pharmaceutically acceptable carrier; pharmaceutical composition can additionally comprise cholesterol biosynthesis inhibitor, in particular lovastatin, simvastatin, atorvastatin, etc. 3. Field of Application Medicine.
A high throughput screening and isolation system identifies rare enhancer mixtures from a candidate pool of penetration enhancer combinations. The combinations are screened for high penetration but low irritation potential using a unique data mining method to find new potent and safe chemical penetration enhancer combinations. The members of a library of chemical penetration enhancer combinations are screened with a high throughput device to identify “hot spots”, particular combinations that show higher chemical penetration enhancement compared to neighboring compositions. The irritation potentials of the hot spot combinations are measured to identify combinations that also show low irritation potential. A active component, such as a drug, is then combined with the combination in a formulation which is tested for the ability of the drug to penetrate into or through skin. It is then assessed whether the formulation can deliver the quantity of drug required, and animal tests are conducted to confirm in vivo the ability of the chemical penetration enhancer combinations to facilitate transport of sufficient active molecules across the skin to achieve therapeutic levels of the active molecule in the animal's blood. The invention provides specific unique and rare mixtures of chemical penetration enhancers that enhance skin permeability to hydrophilic macromolecules by more than 50-fold without inducing skin irritation, such as combinations of sodium laurel ether sulfate and 1-phenyl piperazine, and combinations of N-lauryl sarcosine and Span 20/sorbitan monolaurate.
Use of an antibody or its derivative for preparation of a medicament for passive immunization of an individual for preventing and/or treating allergic reactions in the individual caused by exposure to a birch pollen allergen. The antibody is capable of binding to Bet v 1 fragment comprising amino acid residues at position 30-59 of a defined sequence of 31 amino acids (SEQ ID No. 1) given in the specification or amino acid residues at position 75- 104 of a defined sequence of 31 amino acids (SEQ ID No. 2) given in the specification. Independent claims are included for the following: (1) antibody or its derivative capable of binding to a fragment of Bet v 1, comprising the fragment of Bet v 1 including an amino acid residues at position 30-59 of SEQ ID No. 1 or amino acid residues at position 75-104 of SEQ ID No. 2; (2) vaccine formulation comprising the above antibody; (3) nucleic acid molecule comprising a base sequence of SEQ ID No. 3-298 as provided in figure 2 given in the patent specification; (4) polypeptide coded by the above nucleic acid molecule; and (5) antibody or its fragment comprising the above polypeptide. ACTIVITY : Antiallergic. In a test for measuring inhibition of mouse immunoglobulin (Ig)E binding to rBet v 1 using murine model, the rBet v 1-specific IgG antibodies exhibited inhibition rate of 54.6% compared to control (1%). MECHANISM OF ACTION : Vaccine.
FIELD: medicine, pharmacy. SUBSTANCE: invention relates to compositions showing adaptogenic effect. Composition presents a complex comprising shizandra fruits powder, lyophilized bee mother milk, propolis dry extract, potassium iodide, iron gluconate, maltodextrin, anhydrous colloidal silica and magnesium stearate. Complex exhibits high biological availability and promotes to recovery and enhancement of body protective forces. EFFECT: enhanced effectiveness of complex, valuable medicinal properties. 2 cl
In a controlled trial of Vyvanse in children ages 6 to 12 years, mean weight loss from baseline after 4 weeks of therapy was -0.9, -1.9, and -2.5 lbs., respectively, for patients receiving 30 mg, 50 mg, and 70 mg of Vyvanse, compared to a 1 lb weight gain for patients receiving placebo. Higher doses were associated with greater weight loss with 4 weeks of treatment. Careful follow-up for weight in children ages 6 to 12 years who received Vyvanse over 12 months suggests that consistently medicated children (i.e. treatment for 7 days per week throughout the year) have a slowing in growth rate, measured by body weight as demonstrated by an age- and sex-normalized mean change from baseline in percentile, of -13.4 over 1 year (average percentiles at baseline and 12 months were 60.6 and 47.2, respectively). In a 4-week controlled trial of Vyvanse in adolescents ages 13 to 17 years, mean weight loss from baseline to endpoint was -2.7, -4.3, and -4.8 lbs., respectively, for patients receiving 30 mg, 50 mg, and 70 mg of Vyvanse, compared to a 2.0 lb weight gain for patients receiving placebo.

Careful follow-up of weight and height in children ages 7 to 10 years who were randomized to either methylphenidate or non-medication treatment groups over 14 months, as well as in naturalistic subgroups of newly methylphenidate-treated and non-medication treated children over 36 months (to the ages of 10 to 13 years), suggests that consistently medicated children (i.e. treatment for 7 days per week throughout the year) have a temporary slowing in growth rate (on average, a total of about 2 cm less growth in height and 2.7 kg less growth in weight over 3 years), without evidence of growth rebound during this period of development. In a controlled trial of amphetamine (d- to l-enantiomer ratio of 3:1) in adolescents, mean weight change from baseline within the initial 4 weeks of therapy was -1.1 lbs. and -2.8 lbs., respectively, for patients receiving 10 mg and 20 mg of amphetamine. Higher doses were associated with greater weight loss within the initial 4 weeks of treatment.

Therefore, growth should be monitored during treatment with stimulants, and patients who are not growing or gaining weight as expected may need to have their treatment interrupted.
<P>PROBLEM TO BE SOLVED: To provide a new safe Maillard reaction inhibitor, and further to provide a skin care preparation, drink or food.  <P>SOLUTION: This Maillard reaction inhibitor is characterized by containing the extract of a plant selected from the group consisting of Thujopsis dolabrata, Uncaria gambir Roxburgh, Reynoutria japonica, Pyrola japonica Klenze, Prunus armeniaca, Celosia cristata L., Mucuna birdwoodiana Tutcher, Betula pendula L., Crataegus oxyacantha L., Achilleamillefolium L., Ilex latifolia Thunb., Houttuynia cordata Thunberg, Potenilla tormentilla, Thujopsis dolabrata, Ophiopogon japonicus Gawler, Vitis vinifera L., Polygonum aviculare, Sapindus mukurossi Gaertner, Chaenomelis fructus, Ganoderma lucidum, and Anthemis nobilis L., and rosmarinic acid. In addition, the Maillard reaction inhibitor is used for the skin care preparation, drink or food. This Maillard reaction inhibitor can be utilized for inhibiting the Maillard reaction, further imparts gloss and tension to skin, is effective for preventing and treating the skin, can be used for preventing and treating Maillard reaction-related diseases such as complications originated from diabetes, and can also be expected to have an aging-resistant effect and the like. The Maillard reaction inhibitor has high safety, even when used as an internal use or external use.  <P>COPYRIGHT: (C)2003,JPO
All participants will be in the health coaching group. Participants on study will receive a health coach for 6 months.
Metastasis has a major part in the severity of disease and lethality of cancer. Circulating tumour cells (CTCs) represent a reservoir of metastatic precursors in circulation, most of which cannot survive due to hostile conditions in the bloodstream. Surviving cells colonise a secondary site based on a combination of physical, metabolic, and oxidative stress protection states required for that environment. Recent advances in CTC isolation methods and high-resolution 'omics technologies are revealing specific metabolic pathways that support this selection of CTCs. In this review, we discuss recent advances in our understanding of CTC biology and discoveries of adaptations in metabolic pathways during their selection. Understanding these traits and delineating mechanisms by which they confer acquired resistance or vulnerability in CTCs is crucial for developing successful prognostic and therapeutic strategies in cancer.
<P>PROBLEM TO BE SOLVED: To provide a new metastin homolog and use thereof.  <P>SOLUTION: There is provided a peptide comprising an amino acid sequence enumerated by sequence number 3 or 4. The peptide may have an amidated C terminal. The polynucleotide encodes the peptide. The expression construct comprises the polynucleotide and produces the peptide. The host cell comprises the expression construct and produces the peptide. The pharmaceutical composition for preventing or treating diseases comprises at least one of the peptide, the polynucleotide, the expression construct and the host cell. The antibody is specifically bound to the peptide. The kit for diagnosing diseases comprises the antibody. The method for preventing or treating diseases of human or animals except human includes a step for administration of at least one of the pharmaceutical composition and the antibody.  <P>COPYRIGHT: (C)2010,JPO&INPIT
Levothyroxine is a milestone in the treatment of all causes of hypothyroidism. From 19th century till today, Levothyroxine experienced a great advancement, from hypodermic injections of an extract of the thyroid gland of a sheep to novel formulations, known to circumvent malabsorption issue. However, the rate of patients on suboptimal therapy is still high. Current Guidelines are clear, daily Levothyroxine dosage should be calculated based on body weight. However, we are still far away from the possibility to administer the right dosage to the right patient, for several reasons. We retrace the history of treatment with levothyroxine, pointing out strengths and weaknesses of different formulations, with particular attention to what keeps us away from tailored therapy. In the age of digitalization, the pharmaceutical industry has been giving rising importance to Digital therapeutics, that are known to be effective in reaching target therapies. By combining current knowledge of hypothyroidism therapy with cutting-edge technology, we also hypothesized what could be the future strategies to be developed in this field.
Dental anxiety and fear of pain during procedures are major barriers to oral health care, especially among children. Traditional local anesthesia injections can be distressing for pediatric patients. The fear of needle and dental pain are perhaps among the top reasons for avoidance of dental care. Photomodulation (PBM) is a promising non-tissue penetrating (i.e. minimally invasive) approach for achieving tooth and soft tissue anesthesia/analgesia in dental patients.Investigators plan to use an intra-oral PBM device with a tip comprising of a series of photonic emitters with specific wavelengths that can go through the tooth structure and bone, blocking the nerve conduction like local anesthetics. Research has shown that one burst of light application (for about 20 second) can provide up to 15-20 minutes of pain relief. This could significantly reduce dental anxiety and facilitate access to care and the implications of such an alternative to needles will be a gamechanger especially in pediatric dentistry. The proposed randomzied clinical trials will evaluate if photobiomodulation (PBM) with the near-infrared device produces dental analgesia comparable to local anesthetic injection in pediatric patients. This will be a series of three prospective, clinical studies in 200 school-aged children aged 6-12 years requiring routine dental procedures. The first trial will test the effectiveness of PBM in tooth and soft tissue analgesia by assessing response to diagnostic approaches such as cold pulp testing and gingival probing. The second trial will assess the pre-emptive analgesic effect of PBM on soft tissues at the site of injection prior to local anesthesia infiltration to reduce the discomfort of injection, and the third trial will assess effectiveness of PBM in providing tooth analgesia (compared to routinely used topical anesthesia/local infiltration) for simple restorative procedures in primary teeth.
FIELD: pharmacy. SUBSTANCE: composition comprises mixture of itraconazole and phosphoric acid prepared by melting, pharmaceutically acceptable carrier and surface-active substance. The mass ratio of itraconazole to phosphoric acid is from 1 : 0.1 to 1 : 10. Composition provides the enhanced solubility of itraconazole in an aqueous solution from mixture prepared by melting as compared with solid intraconazole and the following enhancement of bioavailability of itraconazole in vitro. EFFECT: improved preparing method, enhanced and valuable medicinal properties of composition. 4 cl, 1 dwg, 1 tbl, 11 ex
The present invention provides for compounds of formula (I)-(XIII), as well as pharmaceutically acceptable salts thereof, metabolites thereof, pro-drugs thereof, and pharmaceutical kits that include such compounds. The present invention also provides for the compounds of formula (I)-(XIII) for use in medical therapy or diagnosis. The present invention also provides for the use of the compounds of formula (I)-(XIII) in treating cancer in mammals (e.g., humans), as well inhibiting tumor cell growth in such mammals. The present invention also provides for methods of inhibiting FAS. The methods include contacting FAS with an effective amount of a compound of formula (I)-(XIII). The present invention also provides for methods of inhibiting the TE domain of the FAS. The methods include contacting the thioesterase TE domain of the FAS with an effective amount of a compound of formula (I)-(XIII). The present invention also provides for methods of treating cancer in mammals, as well as methods of inhibiting tumor cell growth in such mammals. The methods include administering a compound of formula (I)-(XIII) to a mammal in need of such treatment.
FIELD: cosmetology. SUBSTANCE: cosmetic composition is stable and, anhydrous, in fact, and it possesses antiperspirant and deodorizing activity. It is free from universal jelling agents, such as fatty alcohol and wax of castor oil, and contains at least one active cosmetic substance selected from a group of substances possessing antiperspirant and deodorizing action, which are metal salts in dispersed form suspended in composition, at least one volatile siliconorganic composition including linear and cyclic compounds or their mixtures, at least one siliconorganic composition with linear chain selected from dimethykone, dimethykone copolymer with multiatomic alcohol and/or phenyltrimethykone, and at least one jelling agent which contains hexanediol-behenyl beeswax. Invention also deals with a packed cosmetic composition. EFFECT: production of stable, anhydrous, in fact, free from universal jelling agents, without visible residues at application and after drying cosmetic compositions. 14 cl, 8 ex