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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Source:
NCT01316315: Phase 1/Phase 2 Interventional Completed Asthma
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
N6022 is a novel, first-in-class drug with potent reversible inhibitory activity against S-nitrosoglutathione reductase (GSNOR) and a potential agent for the treatment of acute asthma and cystic fibrosis (CF). Decreased levels of GSNO in the lungs of asthmatics and cystic fibrosis patients have been attributed to increased GSNO catabolism via GSNO reductase (GSNOR) leading to loss of GSNO- and NO- mediated bronchodilatory and anti-inflammatory actions. N6022 restore GSNO levels by inhibiting GSNOR. Inhibition of GSNOR by N6022 has shown safety and efficacy in animal models of asthma, chronic obstructive pulmonary disease, and inflammatory bowel disease. N6022 reduced bronchoconstriction and pulmonary inflammation in a mouse model of asthma. The significant bronchodilatory and anti-inflammatory actions of N6022 in the airways are consistent with restoration of GSNO levels through GSNOR inhibition.
Status:
Investigational
Source:
NCT00615940: Phase 2 Interventional Completed Metastatic Breast Cancer
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Wilex developed WX-UK1 as a specific inhibitor of human trypsin-2, human trypsin-3 and urokinase-plasminogen activator. WX-UK1 participated in phase I clinical trial in combination with capecitabine in advanced malignancies to determine the safety, tolerability, maximum tolerated dose, pharmacokinetics, and pharmacodynamics. However, in April 2014, the clinical development of this drug was discontinued, as part of a company restructure.
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.
Status:
Investigational
Source:
NCT00325715: Phase 1 Interventional Completed Peptic Ulcer
(2006)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Allergan was developing the proton pump inhibitor AGN-201904 as an enteric-coated formulation for the treatment of gastric ulcer disease. AGN-201904 is a slowly absorbed, acid-stable pro-proton pump inhibitor (pro-PPI) rapidly converted to omeprazole in the systemic circulation giving a prolonged residence time. AGN-201904 has been used in trials studying the prevention of peptic ulcer.
Status:
Investigational
Source:
NCT02737722: Phase 1/Phase 2 Interventional Completed Diabetic Foot Infections
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
1-(3,5-BIS-O-(BUTOXYHYDROXYPHOSPHINYL)-2-DEOXY-D-ERYTHRO-PENTOFURANOSYL)-5-METHYL-2,4(1H,3H)-PYRIMIDINEDIONE (Nu-3), a Bisphosphocins, is being developed by Lakewood-Amedex (formerly Nu Pharmas), for the treatment of diabetic foot ulcer, lung infections, stomatitis. Nu-3, a novel synthetic broad-spectrum antimicrobial proven to be effective in killing a wide range of Gram-positive, Gram-negative and antibiotic-resistant bacteria, recently completed a Phase 1/2a clinical trial in patients, showing no treatment-related adverse events and a trend toward efficacy. Patients treated with 2% Nu-3 for seven days had a 65.5% reduction in ulcer area versus a 29.9% reduction in the placebo arm, as measured 14 days after treatment began. In addition, 62.5% of patients treated with 2% Nu-3 saw a reduction in the microbiological load, versus 20% in the placebo. Three additional Phase 2a adaptive arm clinical trials providing robust clinical data in areas of urgent medical need are expected to be completed by 2020.
Status:
Investigational
Source:
NCT00629239: Phase 2 Interventional Completed Chronic Obstructive Pulmonary Disease (COPD)
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
AZD4818 was developed by AstraZeneca as CCR1 receptor antagonist for the treatment of patients with chronic obstructive pulmonary disease. The study was discontinued, because of a lack of clinical efficacy.
Status:
Investigational
Source:
NCT03721744: Phase 2/Phase 3 Interventional Recruiting Metastatic Pancreatic Cancer
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Napabucasin (BBI608) is an orally administered small molecule that blocks stem cell activity in cancer cells by targeting the signal transducer and activator of transcription 3 pathway, which is over-activated in many types of cancer and has been shown to be an important pathway in cancer stem cell-mediated propagation of cancer. Napabucasin has already shown promising efficacy on different cancer types, both as a monotherapy and in combination with conventional chemotherapeutic agents. Early-phase trials have shown promising anti-tumor efficacy when patients are treated with napabucasin in combination with standard chemotherapy agents, and preclinical results suggest that napabucasin can synergize with chemotherapy agents, such as paclitaxel, to potentially overcome drug resistance. Encouraging phase Ib/II trial results warrant further clinical study with napabucasin and paclitaxel combination therapy, especially in malignancies where there is an urgent and unmet need for effective therapeutics, such as in patients with advanced pancreatic adenocarcinoma.
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Carfluzepic Acid is benzodiazepine derivative with tranquilizing, anticonvulsant, and anxiolytic activity patented by pharmaceutical company C. M. Industries S. A.
Status:
Investigational
Source:
NCT02294266: Phase 1 Interventional Completed Amphetamine-Related Disorders
(2014)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Mephedrone (4-methylmethcathinone) is a β-ketoamphetamine belonging to the family of synthetic cathinones, an emerging class of designer drugs known for their hallucinogenic and psychostimulant properties as well as for their abuse potential. Mephedrone is a stimulant of dopamine (DA) release and blocks its reuptake through its interaction with the dopamine transporter. Furthermore, it has some affinity for various 5-hydroxytryptamine (5-HT) receptor subtypes. Neurotoxic effect of mephedrone on 5-HT and DA systems remains controversial. Although some studies in animal models reported no damage to DA nerve endings in the striatum and no significant changes in brain monoamine levels, some others suggested a rapid reduction in 5-HT and DA transporter function. Persistent serotonergic deficits were observed after binge like treatment in a warm environment and in both serotonergic and dopaminergic nerve endings at high ambient temperature. Oxidative stress cytotoxicity and an increase in frontal cortex lipid peroxidation were also reported. Despite the re-classification of mephedrone as a Class B restricted substance by the United Kingdom and restrictive legislation by the United States, international policy regarding mephedrone control is still developing and interest in synthetic amphetamine-like drugs could drive the development of future mephedrone analogues.
Status:
Investigational
Source:
NCT01514461: Phase 3 Interventional Completed Familial Chylomicronemia Syndrome (FCS)
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
LCQ908 (Pradigastat) is a diacylglycerol acyltransferase-1 (DGAT-1) inhibitor. DGAT-1 is one of the two DGAT enzymes that catalyse the formation of triglycerides from diacylglycerol and acyl- coenzyme A. DGAT-1 catalyses the final committed step in processing dietary fatty acids into triglycerides carried on chylomicrons for transport around the body. Pradigastat may decrease the level of triglycerides in the blood and is intended for the first line treatment of FCS. It is administered orally at 10-40mg daily in addition to a low fat diet. Pradigastat is also in phase II clinical trials for type 2 diabetes and severe hypertriglyceridaemia (familial hyperchylomicronaemia phenotypes I and V). Pradigastat is a designated orphan drug in the EU. In a phase III clinical trial.
