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

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Showing 131 - 140 of 430 results

Ethamsylate (2,5-dihydroxy-benzene-sulfonate diethylammonium salt) is a synthetic hemostatic drug indicated in cases of capillary bleeding. Ethamsylate acts on the first step of hemostasis by improving platelet adhesiveness and restoring capillary resistance. In addition it inhibits prostaglandin biosynthesis. Well-controlled clinical trials clearly showed the therapeutic efficacy of ethamsylate in dysfunctional uterine bleeding, with the magnitude of blood-loss reduction being directly proportional to the severity of the menorrhagia. Other well-controlled clinical trials showed therapeutic efficacy of ethamsylate in periventricular hemorrhage in very low birth weight babies and surgical or postsurgical capillary bleeding.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Nitrovin (hydrochloride salt) is a discontinued food additive that was used in veterinarian practice to promote growth. Nitrovin was shown to inhibit Salmonella growth both in vitro and in vivo (in chickens).
Status:
Possibly Marketed Outside US
Source:
ALCOPAR
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hydroxynaphthoic acid is a salt part of discontinued drug Bephenium hydroxynaphthoate. It was also shown to have anti-diabetic effect in mice, acting as a chemical chaperone and reducing ER stress.
Status:
Possibly Marketed Outside US
Source:
Zaldaride maleate by Ciba-Geigy (Novartis)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Zaldaride is a calmodulin antagonist known to produce inhibition of calmodulin-dependent voltage-gated ion channels including those of Ca2 , Na , and K . Zaldaride was also observed to inhibit nicotinic acetylcholine receptor (nAChR) channel currents. Zaldaride has been studied in clinical trials as a potential treatment for travelers diarrhea.
Status:
Possibly Marketed Outside US
Source:
NCT03130634: Phase 4 Interventional Completed Metastatic Colorectal Cancer
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Silymarin, a plant-derived flavonoid from the plant Silybum marianum, is considered the most potential drug to treat almost all kind of liver diseases, particularly alcoholic liver disease, acute and chronic viral hepatitis and toxins-mediated liver dysfunctions. The main component of the silymarin complex is silybin, synonymous with silibinin, sometimes incorrectly called silybinin, which is a mixture of two diastereomers A and B in approximately 1:1 proportion. The drug possess hepatoprotective and antioxidant activity. The hepatoprotective effect is due to stimulation of synthesis of structural and functional proteins and phospholipids, as well as acceleration of the regeneration of hepatocytes. Antioxidant effect is determined by interaction of bioflavones with free radicals in the liver and its detoxication. In such manner the process of peroxidation of the lipids is interrupted and further liver destruction is prevented. Side effect is a mild laxative effect has occasionally been observed.
Status:
Possibly Marketed Outside US
Source:
NCT02307396: Phase 4 Interventional Completed Schizophrenia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Sulpiride is an atypical antipsychotic drug (although some texts have referred to it as a typical antipsychotic) of the benzamide class used mainly in the treatment of psychosis associated with schizophrenia and major depressive disorder, and sometimes used in low dosage to treat anxiety and mild depression. Sulpiride is commonly used in Europe, Russia and Japan. Sulpiride is a selective antagonist at dopamine D2 and D3 receptors. This action dominates in doses exceeding 600 mg daily. In doses of 600 to 1,600 mg sulpiride shows mild sedating and antipsychotic activity. Its antipsychotic potency compared to chlorpromazine is only 0.2 (1/5). In low doses (in particular 50 to 200 mg daily) its prominent feature is antagonism of presynaptic inhibitory dopamine receptors accounting for some antidepressant activity and a stimulating effect. Therefore, it is in these doses used as a second line antidepressant. Racemic and L-sulpiride significantly decreased stimulated serum gastrin concentration, but they did not affect fasting serum gastrin or basal and stimulated gastric acidity. D-sulpiride significantly decreased gastric acid secretion, without affecting serum gastrin levels.
Indoxacarb is a new oxadiazine insecticide discovered and developed by DuPont. The indoxacarb racemate contains two enantiomers (S : R), designated DPX-KN128 and DPX-KN127, but only the S enantiomer has insecticidal activity. It inhibits insect neuronal voltage-dependent sodium channels. Indoxacarb is an active component of Merck Activyl® used in the treatment of flea and tick in dogs and cats. DuPont™ Steward® WG is a water dispersible granule stomach and contact insecticide powered by Indoxacarb for control of various insect pests on a variety of crops.
Status:
Possibly Marketed Outside US
Source:
NCT00734123: Phase 4 Interventional Unknown status Atherosclerosis
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Rimonabant (also known as SR141716; trade names Acomplia, Zimulti) was an anorectic antiobesity drug that was first approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects. Rimonabant is an inverse agonist for the cannabinoid receptor CB1 and was the first drug approved in that class. There is considerable evidence that the endocannabinoid (endogenous cannabinoid) system plays a significant role in appetitive drive and associated behaviors. It is, therefore, reasonable to hypothesize that the attenuation of the activity of this system would have therapeutic benefit in treating disorders that might have a component of excess appetitive drive or over-activity of the endocannabinoid system, such as obesity, ethanol and other drug abuse, and a variety of central nervous system and other disorders. Data from clinical trials submitted to regulatory authorities showed that rimonabant caused depressive disorders or mood alterations in up to 10% of subjects and suicidal ideation in around 1%, and in Europe, it was contraindicated for people with any psychiatric disorder, including depressed or suicidal people. Additionally, nausea and upper respiratory tract infections were very common (occurring in more than 10% of people) adverse effects; common adverse effects (occurring in between 1% and 10% of people) included gastroenteritis, anxiety, irritability, insomnia and other sleep disorders, hot flushes, diarrhea, vomiting, dry or itchy skin, tendonitis, muscle cramps and spasms, fatigue, flu-like symptoms, and increased risk of falling.
Status:
Possibly Marketed Outside US
Source:
NCT00994461: Phase 4 Interventional Completed Healthy Volunteers
(2009)
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



Loxoprofen (INN) is a non-steroidal anti-inflammatory drug in the propionic acid derivatives group. It is marketed in Brazil, Mexico and Japan by Sankyo as its sodium salt, loxoprofen sodium, under the trade name Loxonin, Argentina as Oxeno and in India as Loxomac. It is available in these countries for oral administration, and a transdermal preparation was approved for sale in Japan on January 2006. It is usually used to treat rheumatoid arthritis and osteoarthritis. It is also used to reduce pain and inflammation after surgery, wounds and tooth removal, as well as to bring down fever or ease pain induced by acute inflammation of upper respiratory tract Loxoprofen is a prodrug. When administered orally, loxoprofen sodium hydrate is absorbed from the gastrointestinal tract as an unchanged compound with only a modest gastric-mucosal irritation. It is then rapidly biotransformed into the active metabolite trans-OH form (SRS coordination) with a potent inhibitory effect on prostaglandin biosynthesis to exert its pharmacologic effects. Inhibition of prostaglandin biosynthesis constitutes the mechanism of action of this drug, the site of action being cyclooxygenase.
Bucindolol is a third-generation, non-selective β-adrenergic receptor blocker, that acts on both β-1 and β-2 receptors. Bucindolol’s additional α-1 antagonistic activity contributes to its mild vasodilator effect. It was rejected by the FDA for the heart failure, because of the unreviewed submissions deal with comparative effectiveness, clinical pharmacology, some aspects of pharmacogenetic data, and toxicology/metabolism. In addition, bucindolol is in the phase II of clinical trial for the treatment of atrial fibrillation.

Showing 131 - 140 of 430 results