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

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Showing 711 - 720 of 4227 results

Eflucimibe is a new and potent Acyl coenzyme A:cholesterol acyltransferases inhibitor. Eflucimibe effectively decreased plasma cholesterol in cholesterol-fed animals. In animal models, drug restores normolipodemia in endogenous hypercholesterolemic rabbits and prevents the progression of atherosclerosis by decreasing the number of macrophages in the foam cells. Eflucimibe has been in phase II clinical trials for the treatment of atherosclerosis and hyperlipidemia. However, this research has been discontinued.
Status:
Investigational
Source:
NCT02267525: Phase 2 Interventional Completed Gastroparesis
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Velusetrag (TD-5108) is a potent, selective high intrinsic activity serotonin 5-HT(4) receptor agonist. Velusetrag has achieved proof-of-concept in patients with chronic idiopathic constipation and was on phase II of clinical trial for the treatment of Alzheimer's disease and constipation, when studies were discontinued. In addition, velusetrag is on the phase II of clinical trial for the treatment of gastroparesis.
Status:
Investigational
Source:
NCT02226939: Phase 2 Interventional Completed Liver Cirrhosis
(2002)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Ciluprevir (BILN-2061) is a selective inhibitor of the HCV NS3 serine protease, which was developed by Boehringer Ingelheim for the treatment of hepatitis C infection. The drug was discontinued in phase II due to adverse events such as cardiac toxicity (demonstrated in animals). In the cell-based replicon assay, ciluprevir inhibited HCV RNA replication at low nanomolar levels. It had inhibitory rate constant (Ki) values of 0.3 and 0.66 nM for the NS3 proteases of HCV genotypes 1a and -1b, respectively.
Status:
Investigational
Source:
NCT00896363: Phase 2 Interventional Completed Depressive Disorder
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



GSK-163090 is potent, selective, and orally active 5-HT1A/B/D receptor antagonist. GSK163090 was found to combine potent in vivo activity with a strong preclinical developability profile, and on this basis it was selected as a drug candidate with the aim of assessing its potential as a fast-onset antidepressant/anxiolytic. GSK-163090 had been in phase II clinical trials by GlaxoSmithKline for the treatment of major depressive disorder (MDD) and anxiety disorders. However, this research has been discontinued.
Status:
Investigational
Source:
INN:beloxepin
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Beloxepin (or ADL6906), a novel dual norepinephrine reuptake inhibitor and serotonin receptor antagonist, was investigated for the treatment of the pain and Major depressive disorder, but these studies were discontinued.
Status:
Investigational
Source:
INN:mivotilate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Mivotilate is an orally active hepatoprotective agent for the treatment of liver cirrhosis and hepatitis-B infection. Mivotilate was shown to exert multiple effects on the hepatic cytochrome P450 system, particularly to inhibit CYP2E1 expression and to up-regulate the CYP1A1 expression. The low oral bioavailability of Mivotilate in rats could be primarily attributed to poor absorption and considerable hepatic and gastrointestinal first-pass effects. The thermal reversible microemulsion system of YH439 greatly enhances the bioavailability of YH439 after oral administration. Mivotilate prevents mutagenesis caused by agents such as benzopyrene and reduces skin tumours induced by these agents.
Status:
Investigational
Source:
INN:ametantrone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Ametantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylamino residues at positions 1 and 4; along with other anthraquinones and anthracyclines, it shares a polycyclic intercalating moiety and charged side chains that stabilize DNA binding. Ametantrone is anticancer drug candidate targeting DNA. Ametantrone is a topoisomerase II inhibitor of the anthrapyrazole family. Ametantrone induces interstrand DNA cross-links in HeLa S3 cells. These cross-links were observed only in cellular system suggesting that metabolism of the drugs is a necessary step leading to DNA cross-linking. Ametantrone appeared to be very well tolerated and easy to handle. A dose-schedule of 135 mg/m2 q 2–3 weeks was recommended for phase II studies in solid tumors.
Status:
Investigational
Source:
NCT00681239: Phase 3 Interventional Completed Epilepsy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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:
NCT00479427: Phase 2 Interventional Completed Osteoarthritis
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



GW842166 is a pyrimidine cannabinoid 2 (CB2) receptor agonist that was being developed by GlaxoSmithKline for the treatment of inflammatory pain. It has potent analgesic, anti-inflammatory and anti-hyperalgesic actions in animal models, but without cannabis-like behavioural effects due to its extremely low affinity for the CB1 receptor. GW842166 shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63nM, respectively. GW842166 is in Phase 2 trial.