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Restrict the search for
vitamin a
to a specific field?
Status:
Investigational
Source:
INN:carfloglitazar [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Edatrexate (10-ethyl-10-deazaaminopterin or 10-EDAM) is an analog of methotrexate with improved pre-clinical antitumor activity, more selective cellular uptake, and with the more extensive formation of intracellular polyglutamate metabolites. This drug is a new dihydrofolate reductase inhibitor, which was studied in phase II clinical trial for the patients with different cancers. The studies were discontinued, for example, in advanced renal cell carcinoma edatrexate in the investigated dose and schedule had minimal activity and was toxic. In case of non-small-cell lung cancer, the dosing schedule of edatrexate did not appear to be improved compared to other chemotherapeutic regimens. In addition, edatrexate was involved in the experiment for the treatemnt of rheumatoid arthritis, but this study was also discontinued.
Status:
Investigational
Source:
NCT04573322: Phase 1/Phase 2 Interventional Completed SARS-CoV-2 (Covid19)
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Transcrocetinate (TSC) is a novel compound that offers promise as a treatment for conditions caused by hypoxia or ischemia. Unlike crocetin, it worked well in the more severe hemorrhagic shock model. Although many of the earlier studies with TSC involved the treatment of the ischemic conditions of hemorrhagic shock in both rats and swine, a few other studies involved treating purely hypoxic situations. One study showed that TSC was capable of promoting survival in rats breathing 10% oxygen. TSC also was able to increase arterial PO2 values in a rat model of acute respiratory distress syndrome (ARDS) caused by injection of oleic acid. The drug acts via a mechanism that has not been previously exploited in a pharmaceutical. TSC increases the rate of oxygen diffusion between the erythrocytes and the tissues by altering the 'structure' of water in blood plasma. It does this by causing additional hydrogen bonds to form among the water molecules. Animal toxicology studies have demonstrated that high levels of TSC are well-tolerated, and a Phase I clinical study has shown that TSC is also safe in humans. Delayed TSC treatment improves outcomes in experimental models of both ischemic and hemorrhagic stroke. TSC may be a safe and beneficial therapeutic modality for early stroke intervention, irrespective of the type of stroke involved. Transcrocetinate is in phase III clinical trial for the treatment of glioblastoma.
Status:
Investigational
Source:
NCT03961529: Phase 3 Interventional Completed Atopic Dermatitis
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Molinazone is a benzotriazinone derivative patented by chemical and pharmaceutical companies Farbenfabriken Bayer A.-G. and Bristol-Myers Co. as an analgesic and muscle relaxant
Status:
Investigational
Source:
NCT00387946: Phase 3 Interventional Completed Smoking Cessation
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Dianicline binds with high affinity to the rat and human alpha4beta2 nicotinic acetylcholine receptor (nAChR) subtypes and displays selectivity for the alpha4beta2 nAChR. Electrophysiological experiments indicate that dianicline is a partial agonist at the human alpha4beta2 nAChR subtype. Pretreatment with dianicline reduces the dopamine-releasing and discriminative effects of nicotine. Dianicline shows activity in animal models of nicotine dependence at doses devoid of unwanted side effects typically observed with nicotine. Dianicline did not increase cigarette smoking abstinence rates beyond the initial phase of treatment. However, self-reported craving and nicotine withdrawal symptoms were reduced. The most common adverse event for subjects receiving dianicline was nausea. Other gastrointestinal disorders also tended to be more frequent in the dianicline group, including diarrhea.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ciprokinen is a renin inhibitor discovered by Roche. Ciprokinen inhibited human renin in a buffer and human plasma with an IC50 of 0.07 and 0.65 nmol/L, respectively. In animal models, acute and chronic administration of ciprokinen lead to a reduction in arterial blood pressure. Development of ciprokinen was discontinued at a preclinical stage.
Status:
Investigational
Source:
NCT01631201: Phase 2 Interventional Completed Chlamydia Trachomatis Infection
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Rifalazil (also known as KRM-1648) is a derivative of the antibiotic rifamycin. This orally administered ansamycin is under evaluation for treatment of various bacterial infections. Rifalazil kills bacterial cells by blocking off the β-subunit in RNA polymerase. This drug was originally developed as a therapeutic agent to replace rifampin in the treatment of tuberculosis. It also showed potential to treat indications caused by chlamydia trachomatis and chlamydia pneumoniae. Furthermore, it has been suggested as a potential drug in the treatment of gastric ulcer disease (which is caused by Helicobacter pylori) and antibiotic-associated colitis. Phase II studies evaluated the efficacy and safety of this drug in patients with chlamydia trachomatis and chlamydia seropositive patients. A phase 3 study was initiated including chlamydia seropositive patients. However, the development of rifalazil was terminated in 2013 due to severe side effects.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cefedrolor is a broad-spectrum cephalexin antibiotic patented by pharmaceutical company Bristol-Myers Co.
Status:
Investigational
Source:
NCT00486876: Phase 2 Interventional Completed Irritable Bowel Syndrome
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Dextofisopam, a non-serotonergic agent currently being evaluated for the treatment of irritable bowel syndrome (IBS), is the R-enantiomer of racemic tofisopam, a molecule marketed and used safely outside the United States for over three decades for multiple indications including IBS. Dextofisopam represents a novel, first-in-class opportunity with a positive proof-of-concept study in an arena where there are few compounds with unique approaches or positive efficacy results. By structure, Dextofisopam is a member of the homophthalazine class; Dextofisopam binds to specific receptors in areas of the brain affecting autonomic function, including gastrointestinal (GI) function. Unlike the two 5-HT3 or 5-HT4 mediated IBS therapies currently available, both with significant safety concerns, Dextofisopam novel non-serotonergic activity offers a unique and innovative approach to IBS treatment. Recent studies have indicated that
dextofisopam binds to a novel binding site within the
central nervous system that may be responsible for
mediating its actions. This receptor has been characterized
as the 2,3-benzodiazepine receptor, which is
distinct from the classical 1,4 or 1,5-benzodiazepine
receptor. Dextofisopam has no significant binding at
other receptors or ion channels
