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

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Showing 951 - 960 of 13240 results

Status:
Investigational
Source:
NCT01872078: Phase 2 Interventional Completed Polycystic Ovary Syndrome (PCOS), Female Endocrine Disorder
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Pavinetant, also known as MLE-4901, AZD-4901, AZD-2624, is a small molecule, orally active, selective neurokinin-3 (NK3) receptor antagonist developed for schizophrenia, hot flashes, and Polycystic ovary syndrome. The development for schizophrenia was discontinued due to lack of effectiveness. Phase II trials for polycystic ovary syndrome and for hot flashes showed the clinical risks exceeded benefits, in addition, abnormal liver function was observed, and that is why these studies were also discontinued.
Status:
Investigational
Source:
NCT03865927: Phase 2 Interventional Completed Idiopathic Pulmonary Fibrosis
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



GKT137831, a novel pyrazolopyridinedione derivative, a dual inhibitor of NADPH oxidases (NOX) 1 and NOX4, reduces inflammation in the ischemic retina by dampening the pro-inflammatory phenotype of retinal immune cells as well as macroglial Müller cells and neurons. In patients with diabetic kidney disease, GKT137831 demonstrated an excellent safety profile and statistically significant reduction in both liver enzyme and inflammatory marker levels in multiple phase I and phase II clinical studies. GKT137831 may be of significant benefit for patients with systemic sclerosis as studies in experimental models show that the compound may reduce the abnormal growth of connective tissue (fibrosis) and improve survival. GKT137831 was granted Orphan Drug designation for the treatment of systemic sclerosis from the FDA and the EMA. GKT-137831 acts as a Nox4 and Nox1 inhibitor ((Ki 100–150 nM). GKT-137831 attenuates hypoxia-induced pulmonary vascular cell proliferation. Also a potent inhibitor of fibrosis and hepatocyte apoptosis.
Status:
Investigational
Source:
NCT01150812: Phase 1 Interventional Terminated Thrombin Inhibition
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01247168: Phase 1 Interventional Completed Refractory Solid Tumors
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

AZD-2461 is an oral inhibitor of PARP-1, which was developed by AstraZeneca as a potential anti-cancer medicine. The drug was tested in phase I clinical patients against solid tumosr, but its development was discontinued.
Status:
Investigational
Source:
NCT00723021: Phase 2 Interventional Completed Asthma
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


PF-4191834 is a noniron chelating, non-redox inhibitor of the 5-lipoxygenase enzyme (5-LOX) that is being developed as an oral anti-inflammatory therapy for the treatment of asthma. Enzyme assay results demonstrate that PF-4191834 has an improved potency compared with its predecessor CJ-13610 and of zileuton. It was able to reduce pain and inflammation in an adjuvant-induced arthritis model in rats. PF-4191834 offers the potential to test the hypothesis that chronic inhibition of the 5-LOX enzyme will provide maximal efficacy for this target in inflammatory diseases such as asthma, chronic obstructive pulmonary disease, pain, and perhaps lupus. PF-4191834 had been in phase II clinical trial for the treatment of pain. Development was terminated in March 2011.
Status:
Investigational
Source:
NCT02434744: Phase 2 Interventional Completed Type 2 Diabetes Mellitus
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT02210000: Phase 2 Interventional Completed Gastroparesis
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

GlaxoSmithKline is developing Camicinal (GSK 962040), an oral motilin receptor agonist for the treatment of gastroparesis. Camicinal is being evaluated in phase II for diabetic gastroparesis and gastroparesis. Camicinal is well tolerated in multiple trials with no serious drug-related adverse events or changes in ECG chemistry when given as a single oral dose of up to 125 mg. Although larger studies are soon to be reported, current evidence shows that adverse events occurred evenly between the placebo and treatment groups, and was generally mild. Camicinal has been previously shown to increase gastric emptying in volunteers after repeat dosing over 14 days with no tolerance effect in patients with gastroparesis and type 1 diabetes. Camicinal meets the criteria of an ideal motilin agonist. The compound activates long-lasting cholinergic contractility at low doses in the antrum with greater efficacy than current therapeutic options.
Status:
Investigational
Source:
NCT00992745: Phase 1 Interventional Completed Prostate Cancer
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Iofolastat I-123 is a radiolabeled iodobenzylamine derivative developed by Molecular Insight Pharmaceuticals, Inc as molecular imaging pharmaceuticals for prostate cancer. Iofolastat I123 selectively binds prostate-specific membrane antigen (PSMA), which allows imaging of PSMA-expressing prostate cancer cells. In Phase I clinical trial Iofolastat I-123 localized to lesions in bone and soft tissue that correlated with radiologic evidence of metastatic prostate cancer. Minimal uptake of one of Iofolastat I-123 as seen in the prostate gland of healthy volunteers, suggesting the possibility of visualizing disease in that organ.
Status:
Investigational
Source:
NCT00482664: Phase 2 Interventional Completed Sexual Dysfunction, Physiological
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

CP-866087 is a mu opioid receptor antagonist, discovered by Pfizer. The compound was able to antagonize the effect of morphine in a rodent tail flick assay and produced a dose-dependent decrease in alcohol intake in alcohol-preferring rats. The compound was investigated in clinical trials for the treatment of obesity, alcoholism and female sexual arousal disorder. In the later study, although improvements were seen with CP-866,087 in the key efficacy endpoints, there was no clinical treatment benefit over placebo.
Status:
Investigational
Source:
NCT00808288: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

PF-00610355 is ultra long-acting beta 2 adrenergic receptor-agonists that is being developed for ‘once daily’ treatment of asthma. Plasma pharmacokinetics of orally inhaled PF-00610355 are consistent and exhibit a sustained plateau after single/multiple doses, but plasma exposure is reduced in asthmatic patients compared with healthy volunteers. Although substantial increases in heart rate were observed in healthy volunteers, both pharmacokinetic as well as pharmacodynamic differences between healthy volunteers and chronic obstructive pulmonary disease (COPD) patients (the systemic exposure of PF-00610355 is substantially lower in COPD than in healthy volunteers) explain the modest effect of PF-00610355 on heart rate in the patient population. PF-00610355 had been in phase II clinical trials for the treatment of asthma and chronic obstructive pulmonary disease. However, this development was discontinued.