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

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Showing 91 - 100 of 1608 results

Status:
Investigational
Source:
INN:toreforant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Toreforant (JNJ-38518168) is an orally active, selective histamine H4 receptor antagonist. Toreforant was investigated as an agent for the treatment of active rheumatoid arthritis. While some improvement in rheumatoid arthritis signs/symptoms through week 12 was observed in the phase IIa study, no efficacy was observed with toreforant at lower doses in a subsequent phase IIb study. Toreforant has been tested in clinical studies in patients with asthma and psoriasis. Toreforant failed to provide therapeutic benefit in population of patients with uncontrolled, eosinophilic, persistent asthma. Toreforant efficacy at 30 and 60 mg was greater than placebo but did not meet predefined success criterion in patients with moderate-to-severe psoriasis.
(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:
NCT00387413: Phase 1 Interventional Completed Hyperalgesia
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT00784875: Phase 2 Interventional Completed Primary Insomnia
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:rocastine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Rocastine (AHR-11325) is a potent, nonsedating antihistamine with a rapid onset of action. This H1-antagonist effectively protected guinea pigs challenged with a lethal dose of histamine. It has also been mentioned in patents as a candidate to treat eye conditions and cough/cold mixtures (in which the lack of sedative effects from a non-sedating antihistamine would be especially useful in children, because daytime sedation is especially undesirable in this group). However, information on current use is not available and other second-generation, non-sedative antihistamines are available.
Status:
Investigational
Source:
INN:trenizine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Trenizine is a diphenylmethyl piperazine derivative. It is a vasodilator, antiemetic, antihistamine and anti-anaphylactic agent.
Status:
Investigational
Source:
INN:oxadimedine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Oxadimedine, an antihistamine that was developed as a local anesthetic. Information about the current use of this compound is not available.
Status:
Investigational
Source:
INN:tazifylline
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Status:
Investigational
Source:
NCT01772199: Phase 2 Interventional Completed Multiple Sclerosis, Relapsing-Remitting
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

GlaxoSmithKline (GSK) was developing GSK-239512 as a histamine H3 receptor antagonist/inverse agonist as a monotherapy treatment for subjects with mild-to-moderate probable Alzheimer's disease (AD), multiple sclerosis and Schizophrenia. However, in March 2017, GSK globally discontinued the study of GSK-239512 at phase II.
Status:
Investigational
Source:
INN:methiomeprazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)