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

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Showing 71 - 80 of 1320 results

Status:
Investigational
Source:
Hum Exp Toxicol. May 1996;15(5):369-75.: Not Applicable Human clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
NCT00384423: Phase 2 Interventional Completed Alzheimer's Disease
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

PRX-03140 is a partial agonist of the 5-HT4 receptor that is being developed by EPIX Pharmaceuticals for Alzheimer's disease. In vitro shows potent binding to 5-HT4 receptor and increased cAMP production in human embryonic kidney-293 cells expressing recombinant rat 5-HT(4) receptors. In the clinical trial, PRX-03140 was associated with a statistically significant improvement in the Alzheimer’s Disease Assessment Scale.
Status:
Investigational
Source:
NCT01054118: Phase 1 Interventional Completed Diabetes Mellitus, Type 2
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Arena Pharmaceuticals was developing APD-597 (JNJ-38431055), a small molecule, an orally active agonist of the G-protein coupled receptor 119 (GPR119), for the treatment of Type 2 diabetes mellitus. JNJ-38431055 was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. In addition, extensive in vivo studies showed a more favorable metabolic profile that may avoid the generation of long-lasting metabolites with the potential to accumulate in clinical studies. In humans, single-dose oral JNJ-38431055 increased postmeal plasma glucagon-like peptide 1 (GLP-1), glucose-dependent insulinotropic peptide (GIP), and peptide YY (PYY) concentrations but did not significantly decrease glucose excursion or increase insulin secretion. However, in a graded glucose infusion study, JNJ-38431055 was shown to induce a higher insulin secretion rate (ISR) relative to placebo at elevated plasma glucose levels. These studies provide evidence for the potential efficacy of JNJ-38431055 as an antidiabetes agent in humans.
Status:
Investigational
Source:
NCT02499497: Phase 2 Interventional Completed Prostate Cancer
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LY2452473 is a selective androgen receptor modulator (SARM), with potential tissue-selective androgenic/anti-androgenic activity. Upon oral administration, LY2452473 acts as an agonist in select tissues and organs, including skeletal muscle, bone and the penis, thereby binding to and activating androgen receptor (AR) while acting as an antagonist in the prostate, thereby blocking AR activation and AR-mediated cellular proliferation. This may improve muscle mass and strength, bone formation, and erectile dysfunction while not stimulating growth of the prostate. Eli Lilly was developing LY 2452473/tadalafil combination for the treatment of erectile dysfunction. In addition, Eli Lilly is studying the use of a targeted LY 2452473 therapy, as a possible improvement in quality of life for prostate cancer patients who have undergone radical prostatectomy.
Status:
Investigational
Source:
NCT01291108: Phase 2 Interventional Completed Glaucoma, Open-Angle
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Simenepag (AGN-210676) is a a small molecule selective prostaglandin EP2 agonist with EC50 of 5 nM. Allergan was developing simenepag for the treatment of glaucoma and ocular hypertension.
Status:
Investigational
Source:
NCT00934089: Phase 2 Interventional Completed Glaucoma, Open-Angle
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Taprenepag isopropyl (also known as PF-04217329) a prodrug of CP-544326 (active acid metabolite), a potent and selective EP(2) receptor agonist. Taprenepag isopropyl was studied in a clinical trials phase II involving patients with primary open angle glaucoma. According to Pfizer’s pipelines in May 2011, the study was discontinued.
Status:
Investigational
Source:
NCT01607385: Phase 1 Interventional Completed Diabetes Mellitus, Type 2
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

GSK-1614235 (mizagliflozin) is a sodium glucose co-transporter type 1 (SGLT1) inhibitor that has been investigated for treatment in type 2 diabetes. It is thought to suppress glucose absorption from the intestine in a way that is different from conventional type 2 diabetes drugs, thereby improving postprandial hyperglycemia. Phase 1 studies have been completed.
Status:
Investigational
Source:
NCT01110499: Phase 2 Interventional Completed Ocular Hypertension
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Aganepag isopropyl, an IOP-lowering agent, is an antiglaucoma agent. It is a selective EP2 receptor agonist.
Status:
Investigational
Source:
INN:ezlopitant
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ezlopitant (CJ-11974) is a non-peptide neurokinin-1 receptor antagonist. Pfizer was developing ezlopitant for the potential treatment of irritable bowel syndrome and chemotherapy-induced emesis. Development of ezlopitant has been discontinued.
Status:
Investigational
Source:
INN:dexclamol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dexclamol is a sedative agent. It was found to potentiate the anesthetic actions of halothane. In potentiating the effects of halothane, dexclamol behaved both qualitatively and quantitatively in a manner similar to droperidol. Dexclamol, however, was approximately 37 times less potent than droperidol in antagonizing the vasopressor effects of epinephrine. The neuroleptic agent (+)-dexclamol, but not (-)-dexclamol, affects central dopamine (DA) and norepinephrine (NE) turnover and indicates a stereochemical specificity with respect to antagonism of central DA and NE receptors. Dexclamol was as effective as droperidol at the same dose in inducing neurolepsy and in supplementing nitrous oxide anaesthesia. Changes in heart rate, respiratory rate and rectal temperature in the animals treated with dexclamol were not different from those observed in the animals treated with droperidol.