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

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Showing 381 - 390 of 13240 results

Status:
Investigational
Source:
INN:prizidilol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Prizidilol (also known as SKF 92657) is arylpyridazinylhydrazine derivative patented by Smith Kline and French Laboratories Ltd. as an antihypertensive agent. In clinical trials, Supine and standing blood pressure measured 24--27 h after drug intake was reduced Slight but significant decreases in heart rate were seen after moderate doses of prizidilol. A more pronounced blood pressure reduction was noticed 2--7 h after drug administration. Prizidilol was well tolerated, although dizziness and tiredness were reported by four patients and edema by two.
Status:
Investigational
Source:
NCT03285711: Phase 2 Interventional Completed Lupus Membranous Nephropathy
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03698383: Phase 2 Interventional Unknown status HER2-positive Breast Cancer
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR, originally being developed by Wyeth. Upon intravenous administration, gedatolisib inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K. Significant antitumor efficacy and a favorable pharmacokinetic/safety profile justified clinical evaluation of Gedatolisib. Gedatolisb is in phase II clinical trials by Pfizer for the treatment of acute myeloid leukaemia. Gedatolisb is in phase I clinical trials for the treatment of solid tumours.
Status:
Investigational
Source:
NCT03180528: Phase 2 Interventional Completed Skin Basal Cell Carcinoma
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

METHYLPARABEN SUBEROHYDROXAMIC ACID PHENYL ESTER (more known as Remetinostat), a histone deacetylase (HDAC) inhibitor, was developed for the treatment of cutaneous T cell lymphoma (CTCL). This drug is participating in phase II clinical trial to evaluate the efficacy, safety, and tolerability to skin lesions in patients with early-stage cutaneous T-cell lymphoma. In May 2019 was announced the positive results from phase II trial of remetinostat in basal cell carcinoma (BCC) patients. Initial results suggest that remetinostat gel offers a potentially effective and well-tolerated, non-surgical intervention for the treatment of localized BCCs. The unique design of remetinostat enables topical application, making it active only in the skin. As soon as it reaches the blood stream, it is degraded, avoiding the side effects associated with other HDAC inhibitors. Besides, remetinostat was studied as the treatment of plaque psoriasis; however, this study was discontinued.
Status:
Investigational
Source:
INN:dexamisole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dexamisole is the dextro-isomer of tetramisole, a broad spectrum anthelmintic. Dexamisole significantly improves mood and psychotonicity. In adrenergically innervated blood vessels dexamisole inhibits neuronal uptake of norepinephrine more than levamisole. Dexamisole antagonized the reserpine-induced hypothermia but was ineffective in the apomorphine-induced hypothermia in mice. It reduced ptosis produced by reserpine in mice but this effect was very weak. The effect of dexamisole on the amphetamine-induced hyperactivity depended upon the animal species. Dexamisole reduced the duration of immobility in the despair test in rats. It did not modify the 5-HTP-induced head twitch reaction in mice but produced stimulation of the hind limb flexor reflex in spinal rats. The latter effect was blocked by phenoxybenzamine but not by cyproheptadine and metergoline. Dexamisole also exerted a sedative and hypothermic effect. The above findings indicate that the pharmacological profile of dexamisole resembles in some respects that of tricyclic antidepressants; they also point out that this drug has a central noradrenergic activity.
Status:
Investigational
Source:
INN:fampronil [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:flavodilol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


FLAVODILOL is an antihypertensive agent.
Status:
Investigational
Source:
INN:talibegron [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Talibegron (ZD2079) is a β3 adrenoceptor agonist and insulin sensitiser. It was developed as a potential treatment for obesity and non-insulin-dependent diabetes mellitus. Talibegron hydrochloride had been in phase II clinical trials by AstraZeneca for the treatment of type 2 diabetes and obesity. However, this research has been discontinued.
Status:
Investigational
Source:
INN:pirodomast
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pirodomast is Thromboxane A (TXA2) synthetase inhibitor. Pirodomast can inhibit leukotriene (LT) D4, C4, E4 formation and Thromboxane B2 (TXB2) activities. It was weak or ineffective as an antagonist of histamine, methacholine, serotonin, LTC4 or platelet activating factor induced bronchospasms in guinea pigs. Also, pirodomast was not a bronchodilator or calcium influx blocker and had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is, therefore, a potential antiallergic agent that inhibits leukotriene (LT) release. Pirodomast inhibited tryptase proteolytic activity in-vitro. In experimental studies in vivo, pirodomast blocked antigen-induced immediate and late asthmatic responses in allergic sheep. Pirodomast inhibited antigen-induced airway hyperresponsiveness to both histamine and carbachol in allergic sheep. Pirodomast was being investigated for use in asthma and allergic rhinitis.
Status:
Investigational
Source:
NCT02916056: Phase 3 Interventional Terminated Alzheimer's Disease
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Azeliragon is an orally bioavailable small molecule that inhibits the receptor for advanced glycation endproducts (RAGE). RAGE has been proposed to contribute to Alzheimer's disease pathology by promoting vascular leakage, promoting influx of peripheral amyloid beta into brain, mediating amyloid beta induced oxidative stress, mediating AGE induced hyperphosphorylation of tau and amyloid beta mediated neuronal death. Azeliragon is in Phase III clinical trial for the treatment of mild Alzheimer's disease.