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

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Showing 871 - 880 of 24423 results

Status:
Investigational
Source:
NCT04172532: Phase 1/Phase 2 Interventional Recruiting Locally Advanced Pancreatic Adenocarcinoma
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Linifanib (ABT-869) is a structurally novel, receptor tyrosine kinase (RTK) inhibitor that is a potent inhibitor of members of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor families, but has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib (ABT-869) does not have a general antiproliferative effect due to its high dose requirement. However, it may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3). Linifanib (ABT-869) was in phase III clinical trial for the treatment of hepatocellular carcinoma, but the study failed to meet the primary end point.
Status:
Investigational
Source:
INN:cevoglitazar [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cevoglitazar is a dual agonist for the peroxisome proliferator-activated receptor (PPAR)-alpha and -gamma subtypes. Cevoglitazar was as effective as pioglitazone at improving glucose tolerance, normalizes intramyocellular lipids and reduces body weight gain and adiposity, independent of food intake. Metabolic profiling showed that in the muscle cevoglitazar improves the lipid profile via both PPARα‐ and PPARγ‐mediated mechanisms. Cevoglitazar only induced small changes to the lipid composition of visceral fat. In subcutaneous fat, however, cevoglitazar induced changes similar to those observed with fenofibrate suggesting export of fatty acids from this depot.
Status:
Investigational
Source:
INN:enflicoxib [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
INN:tioxaprofen
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


An oxazole compound, tioxaprofen, exerted a strong anti-mycotic activity against Trichophyton mentagrophytes and T. rubrum, which were major dermatophytes from patients. It was found that tioxaprofen was a potent uncoupling agent of mitochondrial respiration. Tioxaprofen inhibits the electron transport between cytochromes b and c1 in the mitochondrial respiratory chain. Tioxaprofen blocks the formation of thromboxane most probably by inhibition of cyclo-oxygenase.
Status:
Investigational
Source:
NCT03258502: Phase 2 Interventional Completed Respiratory Syncytial Virus Infections
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:oxarbazole
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Oxarbazole was developed as an antiasthmatic agent that inhibited the only bronchoconstriction induced by immune complexes. This drug has never been marketed.
Status:
Investigational
Source:
INN:niravoline [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Niravoline [RU 49679, RU 51599, niravolin], a novel aqueous diuretic with κ-opioid agonistic action. The drug was originally being developed by Hoechst Marion Roussel. Niravoline is a selective agonist of kappa-opioid receptors having potent aquaretic activity. Niravoline was studied with respect to the treatment of brain oedema, heart failure and liver cirrhosis. Niravoline, administered at moderate doses, safely induced a powerful aquaretic effect in patients with cirrhosis and ascites. Moderate doses of niravoline appeared to be a promising pharmacological tool in the treatment of water retention in patients with cirrhosis. The development of niravoline as an aquaretic for the treatment of cirrhosis with ascites and other hyponatraemic disorders has also been halted.
Status:
Investigational
Source:
INN:sumacetamol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Sumacetamol is a acetylaminothioalkanoate derivative patented by Sterwin A.-G. as an analgesic and antipyretic agent. Sumacetamol is used in combination with free paracetamol. In clinical trials, Sumacetamol failed to demonstrate superior efficacy in pain and swelling management compare to paracetamol but shows a longer duration of analgesia. The rates of reported adverse events were similar in paracetamol and Sumacetamol, although reports of mild to moderate drowsiness were more common after the Sumacetamol combination.
Status:
Investigational
Source:
NCT02209155: Phase 2 Interventional Terminated Episodic Cluster Headache
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dexverapamil (R-verapamil) is an enantiomer of verapamil. R-isomer behaved as an inhibitor of multidrug-resistant protein MRP1 (involved in the cancer cell multidrug resistance phenotype). It was developed by Knoll (BASF Pharma) as a chemosensitiser and/or modulator of multidrug resistance for use in combination with cancer chemotherapy. Dexverapamil was undergoing phase II clinical studies in France, Italy, Spain, United Kingdom and the US in patients with various cancers. It was also undergoing phase I clinical trials in Japan where it was licensed to Mitsui and Mitsui Toatsu Chemicals. However, development was discontinued. Dexverapamil (R-verapamil) has been developing by AGI therapeutics for the treatment of Irritable bowel syndrome however development was discontinued.