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Restrict the search for
nonoxynol-9
to a specific field?
Status:
Investigational
Source:
NCT01063907: Phase 1/Phase 2 Interventional Completed Multiple Myeloma
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
KW-2478 is a novel and potent non-ansamycin inhibitor of heat shock protein 90 designed to overcome the limitations, including low water solubility and hepatotoxicity, of 17-allylamino-17-demethoxygeldanamycin (17-AAG). KW-2478 exerts a strong antitumor activity against multiple myeloma (MM) cells with various chromosomal translocations. KW-2478 inhibits cell growth and apoptosis associated with Hsp90 client protein degradation. Recent study results have revealed that KW-2478 is able to deplete Hsp90 client Cdk9 and the phosphorylated 4E-BP1, a transcriptional kinase and a transcription inhibitor respectively, leading to reduced expression of FGFR3, c-Maf, and cyclin D1. KW-2478 suppresses tumor growth and induces the degradation of client proteins in tumors in NCI-H929 s.c. inoculated model at doses of 100 mg/kg or more. KW-2478 reduces both serum M protein and MM tumor burden in the bone marrow in OPM-2/GFP i.v. inoculated mouse model at doses of 100 mg/kg.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tetrazolast (also known as MDL 26,024GO) is a tetrazoloquinoline derivative patented by Merrell Dow Pharmaceuticals, Inc. as an antiallergic and antiasthmatic agent. Tetrazolast was shown to be an orally absorbed mediator release inhibitor in the rat passive cutaneous anaphylaxis and passive peritoneal anaphylaxis tests. In addition, the compound was shown to both elicit and inhibit elicitation of the Bezold-Jarisch reflex in the dog. Tetrazolast also significantly reduced Ascaris-induced changes in pulmonary mechanics in cynomolgus monkeys. The compound inhibited both early and late phase antigen induced-changes in Ascaris-sensitive sheep, as well as the increased airway hyperreactivity which normally follows antigen challenge.
Status:
Investigational
Source:
NCT00485394: Phase 2 Interventional Unknown status Age-Related Macular Degeneration
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Othera Pharmaceuticals developed OT-551 as an antioxidant and anti-inflammatory agent. OT-551 downregulates the overexpression of the protein complex nuclear factor (NF)-kappa B. It is known that NF-kappa B is highly activated when oxidative stress, inflammation, and angiogenesis occurs. OT-551 was studied in phase II clinical trial for the treatment of age-related macular degeneration. In addition, the drug was studied for the treatment of cataracts and dry eyes; however, these studies were discontinued. Besides, phase II clinical trial for the treatment of geographic atrophy has shown that OT-551 might have limited or no benefit as a treatment for this disease.
Status:
Investigational
Source:
NCT00336713: Phase 3 Interventional Completed Depressive Disorder
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sanofi aventis developed saredutant (also known as SR 48968C) as a tachykinin neurokinin-2 (NK2) receptor antagonist for the treatment of depressive disorders and generalized anxiety disorder. This drug participated in phase III clinical trials in patients with a generalized anxiety disorder and as Combination Treatment for major depressive disorder, however, the drug failed to meet efficacy endpoints. It is known that NK-2 receptor mediates airway obstruction that is why saredutant was studied as a potential treatment of asthma. However, all studies of the drug were discontinued.
Status:
Investigational
Source:
NCT02573870: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Batefenterol, previously known as GSK961081, a bifunctional muscarinic (M2 and M3 receptors) antagonist β2-agonist that is developed for chronic obstructive pulmonary disease (COPD). The drug has successfully completed phase II clinical trials with clinically significant improvements in lung function. No new or unexpected safety signals were observed in this COPD population. The conclusion from the trial was following that batefenterol 300 µg might represent the optimal dose for Phase III studies.
Status:
Investigational
Source:
NCT04187144: Phase 3 Interventional Completed Urinary Tract Infections
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Gepotidacin (formerly GSK2140944) is a novel, first-in-class, triazaacenaphthylene antibacterial that selectively inhibits bacterial DNA gyrase and topoisomerase IV by a unique mechanism, one that is not utilized by any currently approved human therapeutic agent. As a consequence of its novel mode of action, gepotidacin is active in vitro against target pathogens carrying resistance determinants to established antibacterials, including fluoroquinolones. Gepotidacin has demonstrated in vitro activity against key pathogens, including drug-resistant strains, associated with a range of conventional and biothreat infections. GlaxoSmithKline is developing Gepotidacin for the treatment of gonorrhoea and skin and soft tissue infections.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Recilisib (also known as EX-RAD or ON-01210) is a radioprotectant, which means that this compound can protect cells from harmful effects of ionizing radiation. Unlike other radioprotectors, recilisib is not a free-radical scavenger or responsible for cell cycle arrest. Recilisib was suggested to have a different radiation protection mechanism involving DNA repair pathways. This compound has been studied as prophylactic (use prior to radiation exposure) and therapeutic (after exposure to radiation) drug. In studies with healthy volunteers, recilisib was rapidly absorbed and well-tolerated, with only mild adverse events. Phase I clinical trials have been completed.
Status:
Investigational
Source:
NCT04673396: Phase 1 Interventional Unknown status Solid Tumor
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Endothal (also known as Endothall), a herbicide for terrestrial and aquatic plants, is a potent, selective protein phosphatase 2A (PP2A) inhibitor. It also inhibits protein phosphatase 1 (PP1). Endothall is considered safe in drinking water, but in case of consumption for a long period, it can cause stomach or intestinal problems.
Status:
Investigational
Source:
NCT00606749: Phase 2 Interventional Completed Pemphigus Vulgaris
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
ITX-5061, an arylketoamide derivative, is a scavenger receptor B1 antagonist and a potent hepatitis C virus (HCV) entry inhibitor. It entered phase I clinical trial in liver transplant recipients with HCV but the trial was terminated.
Status:
Investigational
Source:
NCT00861549: Phase 1 Interventional Completed Healthy
(2008)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Phencynonate (PHH) is a novel anticholinergic compound. It is structurally similar to scopolamine, possesses both muscarinic and nicotinic antagonistic properties as well as anti-NMDA properties. It has been developed as a safe and effective drug for the prevention of motion sickness in tablet form, it also demonstrates clear anticonvulsant effectiveness after soman poisoning in a rat model. S-isomer was more effective against motion sickness and had not anxiogenic action at therapeutic doses. S-isomer has the higher affinity and activity for mAChR in cerebral cortex and acted as a competitive mAChR antagonist. PHH was able to suppress chronic unpredictable mild stress (CUMS)-induced oxidative stress and enhance the antioxidant capacity and antioxidant proteins activity, such as superoxide dismutase 2 (SOD2) and peroxiredoxin 6 (Prdx6). PHH ameliorated CUMS-induced depressive phenotypes by up-regulating SIRT6 deacetylation activity. PHH-mediating SIRT6 pathway is required for antidepressant response and PHH can be used as a novel therapeutic to effectively treat depression. Phencynonate is in phase III clinical trials for the treatment of vertigo.