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

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Showing 141 - 150 of 175 results

Status:
US Approved OTC
Source:
21 CFR 331.11(i)(2) antacid:calcium-containing calcium (mono or dibasic salt)
Source URL:
First marketed in 1921
Source:
Syrup of Calcium Iodide N.F.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Calcium lactate is the salt that consists of two lactate anions for each calcium cation (Ca2+); this salt is used as a calcium supplement to treat hypocalcemia. However, as a source of free calcium, this salt is less convenient than calcium citrate. Calcium lactate inhalation powder also called as PUR118 participated in phase I clinical trials to determine whether this formulation was safe and tolerable in a population of subjects with Cystic Fibrosis (CF). PUR118 also was used in another clinical trials to evaluate its effect on ozone-induced airway Inflammation in healthy normal volunteers in case of Chronic Obstructive Pulmonary Disease (COPD). The obtained results revealed that PUR118 reduced the severity of acute exacerbations in COPD and CF and had the beneficial impacts on mortality, morbidity, and quality of life in affected individuals. However, both studies were discontinued.
Status:
US Approved OTC
Source:
21 CFR 331.11(i)(2) antacid:calcium-containing calcium (mono or dibasic salt)
Source URL:
First marketed in 1921
Source:
Syrup of Calcium Iodide N.F.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Calcium lactate is the salt that consists of two lactate anions for each calcium cation (Ca2+); this salt is used as a calcium supplement to treat hypocalcemia. However, as a source of free calcium, this salt is less convenient than calcium citrate. Calcium lactate inhalation powder also called as PUR118 participated in phase I clinical trials to determine whether this formulation was safe and tolerable in a population of subjects with Cystic Fibrosis (CF). PUR118 also was used in another clinical trials to evaluate its effect on ozone-induced airway Inflammation in healthy normal volunteers in case of Chronic Obstructive Pulmonary Disease (COPD). The obtained results revealed that PUR118 reduced the severity of acute exacerbations in COPD and CF and had the beneficial impacts on mortality, morbidity, and quality of life in affected individuals. However, both studies were discontinued.
Status:
Investigational
Source:
NCT01543919: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



PH-797804 is a diarylpyridinone inhibitor of p38alpha mitogen-activated protein. The drug was developed by Pfizer for the treatment of inflammatory diseases. PH-797804 is being tested in phase II of clinical trials in patients with COPD, osteoarthritis, rheumatoid arthritis and post-herpetic neuralgia.
Status:
Investigational
Source:
NCT00345774: Phase 2 Interventional Completed Pulmonary Hypertension
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



5-((4-(6-Chlorothieno[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl)methyl)-2-fluorobenzonitrile monofumarate (PRX-08066) is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist that causes selective vasodilation of pulmonary arteries. This drug was discovered and developed by Predix (later Epix) Pharmaceuticals and is being researched for the treatment of pulmonary arterial hypertension. In animal studies, PRX-08066 has been found to reduce several key indicators of pulmonary arterial hypertension and improved cardiac output, with similar efficacy to established drugs for this condition such as bosentan, sildenafil, beraprost and iloprost.
Status:
Investigational
Source:
NCT03679598: Phase 2 Interventional Completed Alpha-1 Antitrypsin Deficiency (AATD)
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Avelestat, also known as AZD9668, is a novel, oral inhibitor of neutrophil elastase (NE), an enzyme implicated in the signs, symptoms, and disease progression in NE-driven respiratory diseases such as bronchiectasis, Cystic Fibrosis and chronic obstructive pulmonary disease via its role in the inflammatory process, mucus overproduction, and lung tissue damage. Its development was discontinued due to unknown reasons. Nevertheless, this drug in the phase II of clinical trial as adjunctive therapy in improving insulin sensitivity of insulin-resistant type 2 diabetic subjects. The drug's clinical profile suggests that it will be well tolerated with few, if any, side effects, and the existence of simple methods that can indirectly measure its activity in vivo.
Status:
Investigational
Source:
NCT00479505: Phase 2 Interventional Completed Urinary Bladder, Overactive
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Gisadenafil is a phosphodiesterase V inhibitor in clinical development at Pfizer. It had been in phase II clinical trials for the treatment of Benign prostatic hyperplasia; Chronic obstructive pulmonary disease; Erectile dysfunction; Overactive bladder. Treatment-emergent adverse events were: headache, myalgia, dyspepsia, back pain.
Status:
Investigational
Source:
NCT01108913: Phase 2 Interventional Completed Chronic Obstructive Pulmonary Disease
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Bimosiamose, discovered by Encysive Pharmaceutical and presently being developed by Revotar Biopharmaceuticals, is an 863 g/mol molecular weight dimer with minimal carbohydrate content and is, to date, the leading selectin inhibitor in clinical development. It was developed as anti-inflammatory drug fir the treatment of acute chronic inflammatory disorders including COPD. This compound has shown promise in a phase IIa 'proof of concept' trial in patients with asthma, reducing airway recruitment of eosinophils after intravenous administration. In acute lung injury, neutrophils (a type of white blood cells, thus belonging to the group of cells of the body’s defence system-the immune system) are drawn to the small lung bloodvessels and migrate into the air sacs (alveoli). There they release substances, which cause the inflammation leading to further destruction of the lung tissue. Bimosiamose disodium is expected to hinder the migration of these neutrophils into the alveoli.
Status:
Investigational
Source:
NCT00671073: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Oglemilast (GRC-3886), is a potent and selective PDE4 inhibitor (IC50: 2.5 nM (PDE4B) and 1.7 nM (PDE4D)). Oglemilast is in phase II clinical trials for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Oglemilast was originally developed by Glenmark Pharmaceuticals, and licensed to Forest (acquired by Actavis in 2014) for the rights in North America in 2004. Teijin Pharma obtained the rights of the compound in Japan in 2005.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



GW-311616, a specific NE inhibitor, may act as a potential targeted drug for leukemia, which may have a profound impact on the future of leukemia-targeted therapy. GW-311616 hydrochloride is a potent, selective, intracellular, orally bioavailable and long duration inhibitor of human neutrophil elastase (HNE) with an IC50 value of 22nM. GW-311616 hydrochloride has been found to be selevtive over other human serine proteases with IC50 values of 22nM for HNE, >100uM for trypsin, cathepsin G, and plasmin, >3uM for chymotrypsin and tissue plasminogen activator. In HNE enzyme kinetic tests, GW-311616 has been reported to inhibit HNE with a Ki value of 0.13nM. In addition, GW-311616 has been revealed to inhibit HWB with an IC50 values of 0.67uM in HWB assay. Moreover, by measurement of intraneutrophil elastase activity, GW-311616 hydrochloride has been suggested to have a dose-response and duration of action in blood samples of dog. At present, although research on GW-311616 has being dropped at the preclinical stage, the beneficial profile of oral GW-311616 may make it usuful in the design of new drugs.
Status:
US Previously Marketed
First approved in 1984

Class (Stereo):
CHEMICAL (RACEMIC)



Bitolterol is a beta 2-adrenergic agonist. Since it in itself is biologically inactive, bitolterol is considered a pro-drug. When administered it is activated within the lung by esterase hydrolysis to the active compound colterol catecholamine N-t-butyl-arterenol. Bitolterol was marked under the name tornalate and was indicated to prevent and treat of reversible bronchospasm associated with asthma or chronic obstructive pulmonary diseases. But that drug was withdrawn from the market by Elan Pharmaceuticals in 2001.

Showing 141 - 150 of 175 results