AZD-5423
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AZD-5423
AZD-5423 is a nonsteroidal glucocorticoid and phase II experimental drug being developed by AstraZeneca and disclosed at the spring 2013 American Chemical Society meeting in New Orleans to treat respiratory diseases and in particular chronic obstructive pulmonary disease. It has completed a phase II clinical trial. See also * Dagrocorat * Fosdagrocorat * Mapracorat Mapracorat (INN, code names BOL-303242-X, ZK-245186) is an anti-inflammatory drug belonging to the experimental class of selective glucocorticoid receptor agonists (SEGRAs). It is in clinical trials for the topical treatment of atopic dermatiti ... References External links AZD-5423 - AdisInsight Phenylethanolamine ethers Glucocorticoids Indazoles Trifluoromethyl compounds Respiratory agents Acetamides Fluoroarenes {{respiratory-system-drug-stub ...
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Fosdagrocorat
Fosdagrocorat (developmental code names PF-04171327 and PF-4171327; also known as dagrocorat 2-(dihydrogen phosphate)) is a nonsteroidal but steroid-like selective glucocorticoid receptor modulator (SGRM) which was under development for the treatment of rheumatoid arthritis but was never marketed. It is the C2 dihydrogen phosphate ester of dagrocorat, and acts as a prodrug of dagrocorat with improved pharmacokinetics. The drug reached phase II clinical trials prior to the discontinuation of its development. See also * AZD-5423 * Mapracorat Mapracorat (INN, code names BOL-303242-X, ZK-245186) is an anti-inflammatory drug belonging to the experimental class of selective glucocorticoid receptor agonists (SEGRAs). It is in clinical trials for the topical treatment of atopic dermatiti ... * Dagrocorat References External links Fosdagrocorat - AdisInsight Anti-inflammatory agents Carboxamides Glucocorticoids Phenanthrenes Phenyl compounds Phosphate esters Prodrugs ...
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Dagrocorat
Dagrocorat (developmental code names PF-00251802, PF-251802) is a nonsteroidal but steroid-like selective glucocorticoid receptor modulator (SGRM) which was under development for the treatment of rheumatoid arthritis but was never marketed.https://www.who.int/medicines/publications/druginformation/innlists/PL111.pdf It is described as a partial agonist and "dissociable" agonist of the glucocorticoid receptor. The drug reached phase I clinical trials prior to the discontinuation of its development. The C2α dihydrogen phosphate ester of dagrocorat, fosdagrocorat, was also under investigation, but its development was terminated as well. See also * AZD-5423 * Mapracorat * Fosdagrocorat Fosdagrocorat (developmental code names PF-04171327 and PF-4171327; also known as dagrocorat 2-(dihydrogen phosphate)) is a nonsteroidal but steroid-like selective glucocorticoid receptor modulator (SGRM) which was under development for the treat ... References External links Dagrocorat - Adis ...
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Mapracorat
Mapracorat (INN, code names BOL-303242-X, ZK-245186) is an anti-inflammatory drug belonging to the experimental class of selective glucocorticoid receptor agonists (SEGRAs). It is in clinical trials for the topical treatment of atopic dermatitis, inflammation following cataract surgery, and allergic conjunctivitis. Preliminary investigation for the treatment of keratoconjunctivitis sicca has been conducted in cellular models. Clinical trials Phase II clinical trials with mapracorat started in summer 2009. One trial was a double blind dose finding study for an ointment against atopic dermatitis. It tested concentrations of 0.01%, 0.03% and 0.1% versus placebo over four weeks in around 64 patients. This trial was conducted by Intendis, a part of Bayer HealthCare Pharmaceuticals specialized on dermatology, and completed in September or October 2010. The other trial, also with a double blind design, evaluated an ophthalmic suspension for the treatment of inflammation following ca ...
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Nonsteroidal
A nonsteroidal compound is a drug that is not a steroid nor a steroid derivative. Nonsteroidal anti-inflammatory drugs (NSAIDs) are distinguished from corticosteroids as a class of anti-inflammatory agents. List of nonsteroidal steroid receptor modulators Examples include the following: * Estrogens: benzestrol, bifluranol, estrobin (DBE), diethylstilbestrol (stilbestrol), dienestrol, erteberel, fosfestrol, hexestrol (dihydroxystilbestrol), methallenestril, methestrol, methestrol dipropionate, paroxypropione, prinaberel, and triphenylethylene, as well as many xenoestrogens * : acolbifene, afimoxifene, arzoxifene, bazedoxifene, broparestrol, chlorotrianisene, clomifene, clomifenoxide, cyclofenil, droloxifene, enclomifene, endoxifen, ethamoxytriphetol, fispemifene, idoxifene, lasofoxifene, levormeloxifene, miproxifene, nafoxidine, nitromifene, ormeloxifene, ospemifene, panomifene, pipendoxifene, raloxifene, tamoxifen, toremifene, trioxifene, zindoxifene, zuclomifene * An ...
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Glucocorticoid
Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebrate animal cell. The name "glucocorticoid" is a portmanteau (glucose + cortex + steroid) and is composed from its role in regulation of glucose metabolism, synthesis in the adrenal cortex, and its steroidal structure (see structure below). Glucocorticoids are part of the feedback mechanism in the immune system, which reduces certain aspects of immune function, such as inflammation. They are therefore used in medicine to treat diseases caused by an overactive immune system, such as allergies, asthma, autoimmune diseases, and sepsis. Glucocorticoids have many diverse (pleiotropic) effects, including potentially harmful side effects. They also interfere with some of the abnormal mechanisms in cancer cells, so they are used in high doses to ...
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Phases Of Clinical Research
The phases of clinical research are the stages in which scientists conduct experiments with a health intervention to obtain sufficient evidence for a process considered effective as a medical treatment. For drug development, the clinical phases start with testing for safety in a few human subjects, then expand to many study participants (potentially tens of thousands) to determine if the treatment is effective. Clinical research is conducted on drug candidates, vaccine candidates, new medical devices, and new diagnostic assays. Summary Clinical trials testing potential medical products are commonly classified into four phases. The drug development process will normally proceed through all four phases over many years. If the drug successfully passes through Phases I, II, and III, it will usually be approved by the national regulatory authority for use in the general population. Phase IV trials are 'post-marketing' or 'surveillance' studies conducted to monitor safety over sever ...
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Experimental Drug
An experimental drug is a medicinal product (a drug or vaccine) that has not yet received approval from governmental regulatory authorities for routine use in human or veterinary medicine. A medicinal product may be approved for use in one disease or condition but still be considered experimental for other diseases or conditions. In 2018 the United States of America signed the legislation "Right to Try", this allows individuals who fit into the criteria to try experimental drugs that are not yet deemed safe. In the United States, the body responsible for approval is the U.S. Food and Drug Administration (FDA), which must grant the substance Investigational New Drug (IND) status before it can be tested in human clinical trials. IND status requires the drug's sponsor to submit an IND application that includes data from laboratory and animal testing for safety and efficacy. A drug that is made from a living organism or its products undergoes the same approval process but is called a ...
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AstraZeneca
AstraZeneca plc () is a British-Swedish multinational pharmaceutical and biotechnology company with its headquarters at the Cambridge Biomedical Campus in Cambridge, England. It has a portfolio of products for major diseases in areas including oncology, cardiovascular, gastrointestinal, infection, neuroscience, respiratory, and inflammation. It has been involved in developing the Oxford–AstraZeneca COVID-19 vaccine. The company was founded in 1999 through the merger of the Swedish Astra AB and the British Zeneca Group (itself formed by the demerger of the pharmaceutical operations of Imperial Chemical Industries in 1993). Since the merger it has been among the world's largest pharmaceutical companies and has made numerous corporate acquisitions, including Cambridge Antibody Technology (in 2006), MedImmune (in 2007), Spirogen (in 2013) and Definiens (by MedImmune in 2014). It has its research and development concentrated in three strategic centres: Cambridge, England; ...
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American Chemical Society
The American Chemical Society (ACS) is a scientific society based in the United States that supports scientific inquiry in the field of chemistry. Founded in 1876 at New York University, the ACS currently has more than 155,000 members at all degree levels and in all fields of chemistry, chemical engineering, and related fields. It is one of the world's largest scientific societies by membership. The ACS is a 501(c) organization, 501(c)(3) non-profit organization and holds a congressional charter under Title 36 of the United States Code. Its headquarters are located in Washington, D.C., and it has a large concentration of staff in Columbus, Ohio. The ACS is a leading source of scientific information through its peer-reviewed scientific journals, national conferences, and the Chemical Abstracts Service. Its publications division produces over 60 Scientific journal, scholarly journals including the prestigious ''Journal of the American Chemical Society'', as well as the weekly tra ...
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Chronic Obstructive Pulmonary Disease
Chronic obstructive pulmonary disease (COPD) is a type of progressive lung disease characterized by long-term respiratory symptoms and airflow limitation. The main symptoms include shortness of breath and a cough, which may or may not produce mucus. COPD progressively worsens, with everyday activities such as walking or dressing becoming difficult. While COPD is incurable, it is preventable and treatable. The two most common conditions of COPD are emphysema and chronic bronchitis and they have been the two classic COPD phenotypes. Emphysema is defined as enlarged airspaces ( alveoli) whose walls have broken down resulting in permanent damage to the lung tissue. Chronic bronchitis is defined as a productive cough that is present for at least three months each year for two years. Both of these conditions can exist without airflow limitation when they are not classed as COPD. Emphysema is just one of the structural abnormalities that can limit airflow and can exist without ai ...
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Phenylethanolamine Ethers
Phenylethanolamine (sometimes abbreviated PEOH), or β-hydroxyphenethylamine, is a trace amine with a structure similar to those of other trace phenethylamines as well as the catecholamine neurotransmitters dopamine, norepinephrine, and epinephrine. As an organic compound, phenylethanolamine is a β-hydroxylated phenethylamine that is also structurally related to a number of synthetic drugs in the substituted phenethylamine class. In common with these compounds, phenylethanolamine has strong cardiovascular activity and, under the name ''Apophedrin'', has been used as a drug to produce topical vasoconstriction.''The Merck Index, 10th Ed.'' (1983), p. 1051, Merck & Co., Rahway. In appearance, phenylethanolamine is a white solid. Phenylethanolamine is perhaps best known in the field of bioscience as part of the enzyme name " phenylethanolamine N-methyl transferase", referring to an enzyme which is responsible for the conversion of norepinephrine into epinephrine, as well as other ...
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Glucocorticoids
Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebrate animal cell. The name "glucocorticoid" is a portmanteau (glucose + cortex + steroid) and is composed from its role in regulation of glucose metabolism, synthesis in the adrenal cortex, and its steroidal structure (see structure below). Glucocorticoids are part of the feedback mechanism in the immune system, which reduces certain aspects of immune function, such as inflammation. They are therefore used in medicine to treat diseases caused by an overactive immune system, such as allergies, asthma, autoimmune diseases, and sepsis. Glucocorticoids have many diverse (pleiotropic) effects, including potentially harmful side effects. They also interfere with some of the abnormal mechanisms in cancer cells, so they are used in high doses to tr ...
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