U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1451 - 1460 of 1638 results

Cobalt is a transition metal, naturally ocurring in the minerals cobaltite, smaltite, and erythrite, and is often associated with nickel, silver, lead, copper, and iron ores, from which it is most frequently obtained as a by-product. Depending on the considered species, cobalt has multiple industrial applications including the production of alloys and hard metal, diamond polishing, drying agents, pigments and catalysts. Cobalt is an essential component of Vitamin B12 (hydroxycolalamin). Cobalt functions as a co-factor in enzyme catalysed reactions and is involved in the production of erythropoietin, a hormone that stimulates the formation of erythrocytes. Cobalt salts were used to treat anemia and stimulate erythropoiesis, but was withdrawn from market since Co(II) cations are genotoxic in vitro and in vivo, and carcinogenic in rodents. Hovewer, Co salts are reported to be used by athletes as a doping
Cobalt is a transition metal, naturally ocurring in the minerals cobaltite, smaltite, and erythrite, and is often associated with nickel, silver, lead, copper, and iron ores, from which it is most frequently obtained as a by-product. Depending on the considered species, cobalt has multiple industrial applications including the production of alloys and hard metal, diamond polishing, drying agents, pigments and catalysts. Cobalt is an essential component of Vitamin B12 (hydroxycolalamin). Cobalt functions as a co-factor in enzyme catalysed reactions and is involved in the production of erythropoietin, a hormone that stimulates the formation of erythrocytes. Cobalt salts were used to treat anemia and stimulate erythropoiesis, but was withdrawn from market since Co(II) cations are genotoxic in vitro and in vivo, and carcinogenic in rodents. Hovewer, Co salts are reported to be used by athletes as a doping
Infigratinib (BGJ398), a potent, orally bioavailable, small-molecule pan-FGFR kinase inhibitor. FGFR genetic alterations are the most significant predictors for BGJ398 sensitivity. It is currently in phase 2 trials for Cholangiocarcinoma, Glioblastoma and Solid tumors. Detected adverse events were hyperphosphatemia, fatigue, constipation, cough and nausea. Other adverse events were generally mild and included stomatitis, hair loss, decreased appetite, and fatigue.
Status:
US Previously Marketed
First approved in 2017

Class (Stereo):
CHEMICAL (ABSOLUTE)



Macimorelin (AEZS 130) is an orally active, small-molecule, peptidomimetic growth hormone secretagogue receptor (GHSR1A) agonist (ghrelin analogue), being developed by AEterna Zentaris for the diagnosis of adult growth hormone deficiency (AGHD; somatotropin deficiency), and for the treatment of cachexia associated with chronic disease such as AIDS and cancer. Macimorelin was approved by the FDA in December 2017 under the market name Macrilen for oral solution. Macimorelin stimulates GH release by activating growth hormone secretagogue receptors present in the pituitary and hypothalamus. Macimorelin has been granted orphan drug designation by the FDA for diagnosis of AGHD.
Indacaterol is an ultra-long-acting beta-adrenoceptor agonist developed by Novartis. It was approved by the European Medicines Agency (EMA) under the trade name Onbrez Breezhaler on November 30, 2009, and by the United States Food and Drug Administration (FDA), under the trade name Arcapta Neohaler, on July 1, 2011. It needs to be taken only once a day, unlike the related drugs formoterol and salmeterol. It is licensed only for the treatment of chronic obstructive pulmonary disease (COPD) (long-term data in patients with asthma are thus far lacking). It is delivered as an aerosol formulation through a dry powder inhaler.
Status:
US Previously Marketed
First approved in 1986

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Pirbuterol (trade name Maxair) is a short-acting β2 adrenoreceptor agonist with bronchodilating action used in the treatment of asthma. The pharmacologic effects of beta-adrenergic agonist drugs, including pirbuterol, are at least in proof attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-adenosine monophosphate (c-AMP). Increased c-AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. Pirbuterol is used in asthma for reversal of acute bronchospasm, and also as a maintenance medication to prevent future attacks. It should be used in patients 12 years of age and older with or without concurrent theophylline and/or inhaled corticosteroid. After inhalation of doses up to 800 μg (twice the maximum recommended dose) systemic blood levels of pirbuterol are below the limit of assay sensitivity (2–5 ng/ml). A mean of 51% of the dose is recovered in urine as pirbuterol plus its sulfate conjugate following administration by aerosol. Pirbuterol is not metabolized by catechol-O-methyltransferase.
Status:
US Previously Marketed
Source:
GUANABENZ ACETATE by CHARTWELL RX
(1998)
Source URL:
First approved in 1982

Class (Stereo):
CHEMICAL (ACHIRAL)



Guanabenz, an antihypertensive agent for oral administration-, is an aminoguanidine derivative, 2,'6-dichlorobenzylideneamina-guanidine acetate. It is white to an almost white powder having not more than a slight odor. Sparingly soluble in water and in 0.1 N hydrochloric acid; soluble in alcohol and in propylene glycol. Guanabenz is an orally active central alpha-2 adrenergic agonist. Its antihypertensive action appears to be mediated via stimulation of central alpha-adrenergic receptors, resulting in a decrease of sympathetic outflow from the brain at the bulbar level to the peripheral circulatory system. In clinical trials, guanabenz acetate, given orally to hypertensive patients, effectively controlled blood pressure without any significant effect on glomerular filtration rate, renal blood flow, body fluid volume or body weight. The Myelin Repair Foundation and the National Institutes of Health (National Institute of Neurological Disorders and Stroke) are developing guanabenz for the treatment of multiple sclerosis. Unlike the currently available treatment for multiple sclerosis that suppresses the immune system, guanabenz, an FDA approved the drug for the treatment of high blood pressure, has a potential to reduce the loss of myelin by protecting and repairing myelin-producing cells in the brain from damage. Phase I development is underway in the US.
Status:
US Previously Marketed
First approved in 1981

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Saralasin is an angiotensin II analogue which was developed for the treatment of hypertension in 1970s. For many years saralasin was supposed to be angiotensin receptors blocker, but recent studies have revealed that its pharmacological action can be explained by agonistic behavior toward angiotensin II receptor. The drug was approved by FDA under the name Sarenin, however, it is no longer available on the market.
Lysing is an essential basic amino-acid encoded by codone AAA and AAG, and used in the biosynthesis of proteins. The daily requirement for lysine is 38 mg/kg body weight. The most rich source of lysine is fish, beef, chicken. In a clinical study lysine supplements was found to be an effective for reduction of occurrence, severity and healing time for recurrent HSV infection, however Cochrane Review concluded that the evidence is insufficient. Lysine was investigated for improving anxiety, ameliorating angina prectoris. Lysine acetylsalicylate has been used to treat pain and to detoxify the body after heroin use. Lysine clonixinate has been used for its analgesic properties for the treatment of migraine headaches and other painful conditions. However, limited clinical trials exist for these conditions.

Showing 1451 - 1460 of 1638 results