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

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Showing 2901 - 2910 of 4713 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Tasosartan is a long-acting angiotensin II (AngII) receptor blocker. Tasosartan is infrequently in the treatment of hypertension and heart failure. The manufacturer withdrew it from FDA review after phase III clinical trials showed elevated transaminases. Tasosartan blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor that mediates most, if not all, of the important actions of Ang II. Tasosartan binds reversibly to the AT1 receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance.
Status:
Possibly Marketed Outside US
Source:
Japan:Malotilate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Malotilate (NKK-105) is a drug used in the treatment of liver disease. Malotilate selectively inhibits the 5-lipoxygenase. Malotilate prevented increases in serum markers of type III and IV collagen synthesis as well as accumulation of the collagens, laminin and fibronectin in the liver.
Temoporfin is a photosensitizer (based on chlorin) used in photodynamic therapy for the treatment of squamous cell carcinoma of the head and neck. It is marketed in the European Union under the brand name Foscan. It is used in patients in whom other treatments have stopped working, and who are not suitable for radiotherapy (treatment with radiation), surgery or systemic chemotherapy (medicines used to treat cancer; ‘systemic’ means that they are given as treatments throughout the body). When Foscan is injected, temoporfin is distributed within the body, including within the tumour. When it is illuminated with laser light of a specific wavelength, temoporfin is activated and reacts with oxygen in the cells to create a highly reactive and toxic type of oxygen. This kills the cells by reacting with and destroying their components, such as their proteins and DNA. By restricting the illumination to the tumour, cell damage is limited to the tumour cells, leaving other areas of the body unaffected. The U.S. Food and Drug Administration (FDA) declined to approve Foscan in 2000. The EU approved its use in June 2001.
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.
A potent, selective and orally active receptor antagonist of leukotriene D4, verlukast (MK-571), was discovered and developed from a styrylquinoline lead structure based on a hypothetical model of the leukotriene D4 receptor. MK-571 blocks the action of LTD4 in animals and man, and is effective in a number of animal models of antigen-induced bronchoconstriction at plasma concentration at or below 2 ug/mL. MK-571 also blocks antigen-induced asthmatic responses in man. MK-571 is a potent and selective leukotriene D4 (LTD4) antagonist and ABCC multidrug resistance protein 1(MRP1) inhibitor. The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G-protein coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor. MK-571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. MK-571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors.
Status:
Possibly Marketed Outside US
Source:
NCT02646397: Phase 4 Interventional Unknown status Chronic Kidney Disease
(2016)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Benidipine is an orally triple L-, T-, and N-type calcium channel blocker for the treatment of hypertension and angina pectoris synthesized and developed by Kyowa Hakko Kogyo Co., Ltd. Benidipine, approved in Japan in November 1991, has become one of the three best selling CCBs and is highly useful as a potent, long-lasting antihypertensive and antianginal agent.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Zatosetron is a potent, selective, orally effective 5HT3 receptor antagonist. It has been studied in the treatment of emesis, migraine and anxiety.
Status:
Possibly Marketed Outside US
Source:
Japan:Ancitabine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Cyclocytidine (also known as Ancitabine) is the prodrug of cytarabine, which is structurally similar to human deoxycytidine to be incorporated into human DNA and then kills the cell. Cyclocytidine was introduced as an antineoplastic agent for the treatment of lymphatic leukemia, sinus acceleration and an increase in systemic blood pressure. Cyclocytidine in combination with amsacrine were effective retrieval therapy for pediatric patients with acute nonlymphoblastic leukemia who were in relapse or unresponsive to frontline therapy.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Cinromide possesses antiepileptic activity in various animal models. However, in the experiments for human, this drug had a very limited clinical usefulness and was withdrawn from testing by its manufacturer. The lack of an antiepileptic response may have been due to factors other than species differences but indicates that a positive result of a drug in animal models is not the sole factor necessary to predict beneficial antiepileptic activity in humans. In addition, cinromide was studied for the patients with Lennox-Gastaut Syndrome, as a result, there was no difference between cinromide and placebo in terms of seizure reduction or global evaluations.
Status:
Possibly Marketed Outside US
Source:
Japan:Bevantolol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Bevantolol (INN) was a drug candidate for angina and hypertension that acted as both a beta blocker and a calcium channel blocker. Animal experiments confirm both agonist and antagonist effects on alpha-receptors, in addition to antagonist activity at beta-1 receptors. By binding and antagonizing beta-1 receptors Bevantolol inhibits the normal normal epinephrine-mediated sympathetic actions such as increased heart rate. This has the effect of decreasing preload and blood pressure. Bevantolol was discovered and developed by Warner-Lambert but in January 1989 the company announced that it had withdrawn the New Drug Application. As of 2016 it wasn't marketed in the US, UK, or Europe.

Showing 2901 - 2910 of 4713 results