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

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Showing 49511 - 49520 of 55039 results

Status:
Investigational
Source:
NCT03648489: Phase 2 Interventional Completed Ovarian Cancer
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sapanisertib is an oral dual inhibitor of mTORC1/mTORC2, discovered by Intellikine for the treatment of cancer. The drug is being tested in phase II of clinical trials for different cancers among which are sarcoma, hepatocellular carcinoma, etc. The drug is currently developed by Takeda with breast cancer, renal cancer and endometrial cancer being the main target indications.
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:
NCT01877694: Phase 2 Interventional Completed Bacterial Conjunctivitis
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Auriclosene (previously known as NVC-422) is a broad-spectrum, fast-acting topical anti-infective agent against microbial pathogens, including antibiotic-resistant microbes. It has been investigated in phase II clinical trials for the treatment of bacterial conjunctivitis and as a topical gel in children with impetigo. In addition, using a guinea pig model was shown, that auriclosene was effective in the treatment of dermatophytosis, including onychomycosis.
Status:
Investigational
Source:
INN:furegrelate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Furegrelate (previously known as U-63557A), a selective orally active thromboxane synthase inhibitor, with potential for the treatment of various diseases including hypertension, thrombosis, and renal disorders, arrhythmias, but these studies were discontinued.
Status:
Investigational
Source:
INN:furofenac
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Furofenac (also known as SAS 650), a drug that has antiplatelet-aggregation activity and anti-inflammatory activity combined with low ulcerogenic power. It was shown that the furofenac mechanism of action involved the modulation of the platelet cyclooxygenase pathway.
Status:
Investigational
Source:
INN:furofenac
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Furofenac (also known as SAS 650), a drug that has antiplatelet-aggregation activity and anti-inflammatory activity combined with low ulcerogenic power. It was shown that the furofenac mechanism of action involved the modulation of the platelet cyclooxygenase pathway.
Status:
Investigational
Source:
INN:pibrozelesin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pibrozelesin (KW-2189) is a semisynthetic water-soluble derivative of the antineoplastic antibiotic duocarmycin B2. Activated by carboxyl esterase, pibrozelesin alkylates DNA by binding to adenine-thymine (A-T)-rich sequences in the minor groove of DNA, thereby inhibiting DNA replication and inducing apoptosis. KW-2189 induced DNA strand breaks in H69 cells in a concentration-dependent manner. DNA cleavage is one of the major mechanisms of KW-2189-mediated cytotoxicity. KW-2189 showed evidence of anti-tumor activity in hepatocellular carcinoma (HCC). However, because of significant and prolonged hematologic toxicity, when given as a single dose every 6 weeks, further development of this drug in HCC is not possible. Pibrozelesin had been in phase II clinical trial for the treatment of advanced malignant melanoma and advanced renal cell carcinoma. No activity in metastatic renal cell carcinoma was demonstrated and the lack of significant antitumor activity in advanced malignant melanoma treatment was shown.
Status:
Investigational
Source:
INN:oxmetidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxmetidine is an H2-receptor antagonist that was studied as a gastrointestinal agent. Oxmetidine possesses efficacy in the treatment of peptic ulcers. However, information about the further development of this drug is not available.
Status:
Investigational
Source:
INN:haletazole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Halethazole has been studied as an active antifungal compound.
Status:
Investigational
Source:
NCT01908699: Phase 3 Interventional Completed Pulmonary Arterial Hypertension
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Esuberaprost (314d) is an active enantiomer of beraprost, a prostacyclin analog. The pharmacologic action of esuberaprost is mediated by specifically binding to PGI2 receptors in smooth muscle cells (the blood vessel’s endothelium) and platelets. Upon binding, the compound widened blood vessels, preventing the formation of blood clots, and lowering blood pressure in the lungs. As a result, it was expected to improve the symptoms of pulmonary arterial hypertension. United Therapeutics announced it has ended its Phase 3 BEAT trial testing esuberaprost as an add-on therapy to its product Tyvaso (inhaled treprostinil) for clinically symptomatic patients with pulmonary arterial hypertension (PAH). According to a company press release, the study failed to reach its main endpoint of delaying the time to first clinical worsening events.

Showing 49511 - 49520 of 55039 results