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Restrict the search for
telotristat ethyl
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
AMOXECAINE is an local anaesthetic.
Status:
Investigational
Source:
JAN:BEPERIDIUM IODIDE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Beperidium (also known as SX-810 ) is a competitive antagonist against acetylcholine. Experiments on animal have shown that this compound exhibited spasmolytic and antiulcerative activities without exerting systemic antimuscarinic side effects.
Status:
Investigational
Source:
NCT00003523: Phase 2 Interventional Completed Ovarian Cancer
(1999)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Rubitecan [Orathecin™] is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral compound being developed for the treatment of pancreatic cancer and other solid tumours by SuperGen. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks.
Class (Stereo):
CHEMICAL (ACHIRAL)
Mofarotene is an analog of retinoic acid patented by a Swiss multinational healthcare company Hoffmann-La Roche as neoplasm inhibitors and agent for treating dermatoses. Like other retinoic acid agents, mofarotene binds to and activates retinoic acid receptors (RARs), thereby altering the expression of certain genes leading to cell differentiation and decreased cell proliferation in susceptible cells. Mofarotene has demonstrated considerable antitumor activity in a number of cancer cell lines. Mofarotene in combination with cisplatin and etoposide was studied in phase I clinical trials but further development was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Sulotroban is a phenoxyalkylcarboxylic acid derivative patented by Boehringer Mannheim G.m.b.H. as thrombocyte aggregation inhibitor and lipid-lowering agent. Sulotroban is the first thromboxane A2 receptor antagonist available for use in man. Its antagonistic profile appeared to be specific and competitive both for platelets and vascular or bronchial smooth muscle receptors. In preclinical models Administered as a single dose of 800 mg, sulotroban antagonized arachidonic acid-induced, collagen-induced, and U-46619-induced platelet aggregation. In clinical trials, Sulotroban shows superior efficacy to placebo in preventing acute problems during, or restenosis after, coronary angioplasty. Chronic dosage with the drug did not lead to any accumulation of its blocking effect on platelet function; the effect of each dose declined to zero 6-7 hours after dosing.
Status:
Investigational
Source:
NCT00505076: Phase 2 Interventional Completed Schizophrenia
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
MK 0777 is a selective GABAA α2/3 receptor partial agonist, for potential use in the treatment of Schizophrenia, Anxiety Disorder, and Generalized Anxiety Disorder. MK-0777 is functionally selective for the α2 and α3 subunits, with virtually no activity for the α1 and α5 subunits. Therefore, MK-0777 cause less sedation, interact less with alcohol, and exhibit less abuse potential and physical dependence than benzodiazepines. Unfortunately, in clinical trials, MK-0777 has little benefit for cognitive impairments in people with schizophrenia and anxiety disorder.
Status:
Investigational
Source:
NCT00000628: Phase 1 Interventional Completed HIV Infections
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (RACEMIC)
Pinokalant is the isoquinoline derivative. It is a broad-spectrum cation channel blocker which inhibits store-operated cation channels in human endothelial cells, mast cells, HL60 cells and in primary cultures of cortical and hippocampal neurons. Pinokalant inhibits voltage-operated calcium channels of the L- and N-subtypes in primary cultures of cortical neurons and shows some antagonism on the NMDA- and AMPA glutamate receptor subtypes. Pinokalant also acts as an antagonist at the delayed rectifier K+ channel in PC12 cells and cortical neurons. Pinokalant reduced in vivo lesion size as well as post mortem infarct size derived from 2,3,5-triphenyltetrazolium chloride-stained brain slices 24 hr after middle cerebral artery occlusion. Pinokalant has been evaluated as a potential neuroprotectant in rodent models of stroke.
Status:
Investigational
Source:
NCT00080015: Phase 2 Interventional Completed Small Cell Lung Cancer
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Diflomotecan is an E-ring modified camptothecin analogue, which possesses greater lactone stability in plasma compared with other topoisomerase I inhibitors. Diflomotecan was the first homocamptothecin to enter clinical studies. Phase I data are summarized for both the intravenous and oral schedules. The toxicity is primarily haematological while no severe gastrointestinal toxicity has been observed in contrast to other topoisomerase I inhibitors. Diflomotecan has a high oral bioavailability (72 - 95%) and the oral day 1 - 5 every 3 weeks regimen is recommended for Phase II testing because it is relatively well tolerated. Diflomotecan had been in Phase II clinical trials for the treatment of small cell lung cancer. However, this research has been discontinued.
