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

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Showing 81 - 90 of 816 results

(R)-Mequitazine or V0162 (10-[(3R)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine) is an anticholinergic enantiomer of mequitazine, an existing oral racemic antihistamine commercialized for over 30 years. (R)-Mequitazine was found to be an antagonist at muscarinic acetylcholine receptors behaving as an inverse agonist. (R)-Mequitazine was investigated in clinical trials for the treatment of chronic obstructive pulmonary disease, asthma and urinary incontinence.
Status:
Investigational
Source:
NCT01730768: Phase 2 Interventional Completed Schizophrenia
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03404570: Phase 2 Interventional Completed Palmar Hyperhidrosis
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dexmecamylamine (TC-5214, also known, as S isomer of mecamylamine) is a positive allosteric modulator of α4β2 neuronal nicotinic receptors, rather than an open-channel blocker. It was evaluated as a potential adjunct treatment for patients with major depressive disorder (MDD). TC-5214 was generally well tolerated, however, the studies were not supportive of an antidepressant effect for TC-5214 in patients with MDD and inadequate response to prior antidepressant therapy. The Phase 2b clinical trial of TC-5214 for the treatment for overactive bladder (OAB) revealed the high dose of TC-5214 demonstrated mixed results on the co-primary endpoints by providing a statistically significant reduction in micturition frequency and an improvement that did not reach statistical significance on episodes of urinary incontinence. As a consequence of these results, this drug was discontinuing further development of TC-5214 in OAB. The study for using TC-5214 in patients with refractory hypertension was also terminated.
Status:
Investigational
Source:
NCT02573870: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Batefenterol, previously known as GSK961081, a bifunctional muscarinic (M2 and M3 receptors) antagonist β2-agonist that is developed for chronic obstructive pulmonary disease (COPD). The drug has successfully completed phase II clinical trials with clinically significant improvements in lung function. No new or unexpected safety signals were observed in this COPD population. The conclusion from the trial was following that batefenterol 300 µg might represent the optimal dose for Phase III studies.
NGX267 is a partial muscarinic receptor agonist with functionally specific M1 and M3 receptor activity, developed by Torrey Pines Therapeutics(TPTX) for the treatment of Xerostomia, Alzheimer’s disease and cognitive deficits in schizophrenia. NGX-267 had been in phase II clinical trials for the treatment of Xerostomia, however, all researchers on this drug candidate were discontinued.
Status:
Investigational
Source:
NCT01852110: Phase 2 Interventional Terminated Alzheimer's Disease
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT01033487: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

PF-03635659 is a potent, very long dissociative half-life (slow off-rate, >1440 min) muscarinic M3 antagonist. Spirometry data from healthy volunteers in phase I clinical studies illustrate that PF-03635659 provides efficacious 24 h bronchodilation from a single inhaled dose, thus confirming the suitability of PF-03635659 as a novel once-daily inhaled muscarinic M3 receptor antagonist for the treatment of chronic obstructive pulmonary disease (COPD). Safety (tachycardia) and toleration (dry mouth) data from the multidose phase I studies indicate an adverse event profile that is at least noninferior to tiotropium bromide. PF-03635659 had been in phase II clinical trial for the treatment of chronic obstructive pulmonary disease.
Status:
Investigational
Source:
NCT01714713: Phase 3 Interventional Completed Schizophrenia
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Encenicline (EVP-6124; MT-4666) acts as a potent partial and selective agonist at alpha-7 nicotinic acetylcholine receptor. Encenicline significantly improved memory function in animal models. FORUM Pharmaceuticals (formerly EnVivo Pharmaceuticals) is developing encenicline for the treatment of cognition disorders such as schizophrenia and for Alzheimer's disease.
Status:
Investigational
Source:
NCT00752830: Phase 1 Interventional Completed Healthy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

AZD0328, a spirofuropyridine, is a selective alpha7 nicotinic receptor agonist. This drug participated in clinical trials phase II in patients with schizophrenia. However, studies were terminated because the drug didn’t meet the current target product profile. Besides AZD0328 has been studied in phase I for the treatment of Alzheimer's disease.
Status:
Investigational
Source:
NCT01678755: Phase 2 Interventional Completed Schizophrenia
(2012)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)