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

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Showing 1361 - 1370 of 13240 results

Prinomastat is a synthetic hydroxamic acid derivative with potential antineoplastic activity. Prinomastat inhibits matrix metalloproteinases (MMPs) (specifically, MMP-2, 9, 13, and 14), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. As a lipophilic agent, prinomastat crosses the blood-brain barrier. Pfizer conducted multicenter, randomized, double-bind, placebo-controlled trials to evaluate the safety and efficacy of prinomastat in combination with standard chemotherapy in patients with advanced hormone refractory prostate cancer and non-small cell lung cancer. However, this study has been terminated for the reason that Prinomastat did not improve the outcome of chemotherapy in non-small cell Lung cancer patients.
Status:
Investigational
Source:
INN:thiacetarsamide sodium [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Thiacetarsamide is a drug containing trivalent arsenic. In the USA it was used for the treatment of Heartworm Infection in dogs and cats under tradename Caparsolate, however, it was discontinued because of the availability of safer alternatives. The mechanism of action for thiacetarsamide is modulation of glucose uptake and metabolism; inhibition of glutathione reductase, and alteration of the structure and function of the surface of the intestinal epithelium of the parasites.
Status:
Investigational
Source:
NCT01051921: Phase 2 Interventional Completed Hepatitis C
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


CTS-1027 (Ro-1130830) is a hydroxamic acid matrix metalloprotease (MMP) inhibitor. CTS-1027 was originally designed as a strong inhibitor of MMP-2, -3, -8, -9, -12, -13 and -14, without inhibiting MMP-1 and MMP-7. CTS-1027 was proved to be safe in clinical trials for osteoarthritis conducted by Roche. CTS-1027 was then licensed from Roche to Conatus Pharmaceuticals and was investigated as a protector from liver fibrosis in hepatitis C virus patients. The development of the drug was discontinued due to laboratory abnormalities and adverse events in a subset of clinical trial participants.
Status:
Investigational
Source:
NCT01107522: Phase 1 Interventional Active, not recruiting Solid Tumors, Glioblastoma, Recurrent Malignant Gliomas
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Carboxyamidotriazole (L651582) is a carboxyamide-amino-imidazole compound originally developed as a coccidiostat, an antiprotozoal agent that acts upon Coccidia parasites. Carboxyamidotriazole (L651582) is an orally-active agent with potential antineoplastic activity. Carboxyamidotriazole binds to and inhibits non-voltage-operated Ca2 channels, blocking both Ca2 influx into cells and Ca2 release from intracellular stores and resulting in the disruption of calcium channel-mediated signal transduction and inhibition of vascular endothelial growth factor (VEGF) signaling, endothelial proliferation, and angiogenesis. This agent may also inhibit tumor cell growth, invasion, and metastasis.
Status:
Investigational
Source:
NCT00169559: Phase 2 Interventional Completed Dyslipidaemias
(2003)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

GW 590735 is a selective and potent agonist of peroxisome proliferator-activated receptor alpha (PPARα), a ligand-activated transcription factor that plays a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein. GW 590735 was in phase II clinical trial for the treatment of dyslipidemia, but that study was discontinued.
Status:
Investigational
Source:
INN:besunide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Besunide was studied as a diuretic agent.
Status:
Investigational
Source:
INN:piriprost
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Piriprost (U-60, 257) is a structural analog of prostaglandin I2 (PGI2) with low IP receptor-mediated activity. It inhibits 5-LO (5-lipoxygenase). Piriprost inhibits the release of histamine and leukotrienes, implicating its role in inflammation and allergic responses. However, it was shown, that piriprost did not influence the airway responses after allergen in asthma. Nevertheless, even more, the drug was irritant to the respiratory tract than was placebo.
Status:
Investigational
Source:
INN:edonentan
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Edonentan (BMS 207940) is a highly selective biphenylsulfonamide endothelin A receptor antagonist. (11)C- and (18)F-labeled analogs of edonentan were evaluated of novel PET radioligands for imaging the endothelin-A receptor. Edonentan was in clinical trials for the treatment of heart failure however its development has been discontinued.
Status:
Investigational
Source:
NCT04388475: Phase 2 Interventional Active, not recruiting Recurrent Malignant Glioma
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


AstraZeneca developed disufenton (NXY-059), a free radical trapping agent, for the treatment of ischaemic stroke and other brain injuries. Nevertheless, large clinical trial (3306 versus 1722 patients) was neutral, providing no evidence for the efficacy of disufenton sodium in patients with stroke. One study using rat cortical brain slices concluded that NXY-059 improved neuronal survival. However, another study in mouse neuroblastoma cells reported no effect. Another study reported that NXY-059 restored endothelial blood-brain. Histological analyses revealed several therapeutic advantages associated with disufenton sodium treatment following acute acoustic trauma, including reductions in inner and outer hair cell loss; reductions in acute acoustic trauma-induced loss of calretinin-positive afferent nerve fibers in the spiral lamina; and reductions in fibrocyte loss within the spiral ligament. However, AstraZeneca terminated the development program.
Status:
Investigational
Source:
INN:pelanserin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Pelanserin is an antagonist of the serotonin 5-HT2 receptor and blocks alpha 1-adrenoceptor. Experiments on dogs have revealed that pelanserin showed adequate pharmacokinetic and pharmacodynamics profiles as an antihypertensive agent that is why the drug possessed potential therapeutic usefulness in the treatment of hypertension. Pelanserin was undergoing phase II clinical trials by Cinvestav in Mexico; however, these studied were discontinued.

Showing 1361 - 1370 of 13240 results