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

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Showing 421 - 430 of 740 results

Status:
Possibly Marketed Outside US
Source:
NCT03388853: Phase 4 Interventional Completed COPD
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Doxofylline (7-(1, 3-dioxalan-2-ylmethyl) theophylline) is a novel xanthine bronchodilator which differs from theophylline in that it contains a dioxalane group in position 7. Doxofylline is indicated for the treatment of bronchial asthma, pulmonary disease with spastic bronchial component and Chronic Obstructive Pulmonary Disease (COPD). Doxofylline does not directly inhibit any of the known HDAC enzymes, and did not inhibit any phosphodiesterase (PDE) enzyme sub types or act as an antagonist at any of the known adenosine receptors, except for PDE2A(1), and adenosine A(2A) and only at the highest tested concentration (10(-4) M). Doxofylline has greatly decreased affinity towards adenosine A1 and A2 receptors, which explain its better safety profile. Moreover, it does not interfere with calcium influx into the cells nor antagonize calcium channel blockers. Doxofylline has been shown to be a more potent bronchodilator with fewer side effects than theophylline. This drug should not be administered together with other xanthine derivatives, including beverages and foods containing caffeine.
Roxatidine is an histamine H2-receptor antagonist. Roxatidine is a potent and selective inhibitor of basal and stimulated gastric acid secretion through competitive blockade of H2-receptors. Total pepsin secretion is reduced in a dose-dependent manner. There is an independent mucosal protection action. Roxatidine is indicated for the treatment of peptic ulcer, gastro-oesophageal reflux disease, gastritis, upper gastrointestinal haemorrhage and Zollinger-Ellison syndrome also it can be used as a premedication before anaesthesia. Roxatidine possessed a robust estrogenic activity.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)

Methadyl Acetate is a narcotic analgesic with a long onset and duration of action. Methadyl Acetate is primarily a mu-type opioid receptor agonist and the drug decreases a patient's opioid use by preventing opioid withdrawal. Levacetylmethadol, the enantiomer of Methadyl Acetate, was approved in 1993 by the U.S. Food and Drug Administration for use in the treatment of opioid dependence. In 2001, levacetylmethadol was removed from the U.S. market due to reports of life-threatening ventricular rhythm disorders.
Status:
Possibly Marketed Outside US
Source:
NCT02027337: Phase 4 Interventional Unknown status Polycystic Ovarian Syndrome
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cyproterone belongs to a group of medications known as steroidal antiandrogens. It suppresses testosterone and its metabolites. It has approximately three-fold lower potency as an antagonist of the androgen receptor relative to cyproterone acetate. Cyproterone acetate is used to treat advanced prostate cancer and acne.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Demegestone, a norprogesterone derivative, is a progesterone receptor agonist that was previously used to treat luteal insufficiency. It was marketed in France as Lutionex, but has since been discontinued. Demegestone has also been studied in combination with estrogens as an oral contraceptive and treatment for infertility. Demegestone did not exercise androgenic activity. Demegestone is the potent inhibitor of estrone sulfatase activity.
Status:
Possibly Marketed Outside US
Source:
NCT01577043: Phase 4 Interventional Completed Acute Diarrhea
(2011)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Racecadotril (acetorphan) is an oral enkephalinase inhibitor for use in the treatment of acute diarrhea. Racecadotril reduces hypersecretion of water and electrolytes into the intestinal lumen, by preventing the degradation of endogenous enkephalins. Treatment with racecadotril reduces the incidence and duration of acute diarrhea and reduces diarrhea-associated symptoms compared with placebo in adults. Racecadotril treatment also results in significant reductions in stool output compared with placebo in infants and young children aged 2 months to 4 years with acute diarrhea. Both rotavirus-negative and rotavirus-positive infections appear to respond to treatment in the pediatric populations investigated for this infection. Racecadotril shows similar or slightly reduced efficacy to loperamide in the treatment of diarrhea in adults and children aged up to 10 years. However, in comparative trials, racecadotril was associated with fewer adverse events than loperamide, in particular, post-treatment constipation. Racecadotril is available in France (where it was first introduced in ~1990) and other European countries (including Germany, Italy, the UK, Spain and the Czech Republic) as well as most of South America and some South East Asian countries (including China, India and Thailand), but not in the United States.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)


Deprodone is a steroid that was approved in Japan for the treatment of inflammatory skin disorders. The drug is marketed under the name Eclar and contains 0.3% of the prodrug, deprodone propionate.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Flumedroxone is a progestative agent. It is a pregnane derivative substituted at C-6 by a trifluoromethyl group. It was tested whether flumedroxone had prophylactic value in migraine. No benefit was found in males, or in females with no history of menstrual exacerbation of migraine. In women whose migraine was worse around the time of menstruation flumedroxone resulted in statistically fewer headaches of less severity. With the dose used in this trial side-effects were frequent, the commonest being polymenorrhagia, which occurred in half the women of reproductive age.
Status:
Possibly Marketed Outside US
Source:
NCT01321034: Phase 4 Interventional Completed Hypercholesterolemia
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Laropiprant is a drug, which was used in combination with nicotinic acid (also known as niacin) and was known under tradename: tredaptive. Tredaptive was indicated as adjunctive therapy to diet for use in patients with primary hypercholesterolaemia (heterozygous familial and non-familial) or mixed dyslipidaemia. The marketing authorisation for Tredaptive has been withdrawn at the request of the marketing-authorisation holder due to increases in side effects with no cardiovascular benefit. Laropiprant is a selective antagonist of the prostaglandin D(2) (PGD(2)) receptor subtype 1 (DP1). It also has the affinity to interact with thromboxane A2 receptor (TP), although it is approximately 190-fold less potent when compared to DP1. Activation of TP has been shown to induce platelet aggregation in vitro, whereas activation of human platelet DP1 inhibits platelet aggregation. These in vitro data indicate that laropiprant may alter platelet function either by enhancement of platelet reactivity through DP1 antagonism or by inhibition of platelet aggregation through TP antagonism. Also were clinical trials phase II for the laropiprant alone, there were shown, that drug did not demonstrate efficacy in asthmatic patients or patients with allergic rhinitis.
Status:
Possibly Marketed Outside US
Source:
NCT02307396: Phase 4 Interventional Completed Schizophrenia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Zuclopenthixol is indicated the management of the manifestations of schizophrenia and other mental illnesses with disturbances in thinking, emotional reactions and behaviour. It is also used to treat the manic phase of manic depressive illness. Zuclopenthixol, a thioxanthene derivative, has high affinity for both dopamine D1 receptors and dopamine D2 receptors. Zuclopenthixol also has high affinity for α1-adrenergic and 5-HT2 receptors. Zuclopenthixol (CLOPIXOL®) is avavilable in the form of tablets and solution for intramuscular injections.

Showing 421 - 430 of 740 results