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Status:
Investigational
Source:
NCT00275197: Phase 2 Interventional Completed Depressive Disorder, Major
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Elzasonan (CP 448187) is a serotonin 1B/1D receptor antagonist. Elzasonan was primarily metabolized via oxidative N‐demethylation, N‐oxidation, and aryl hydroxylation. Pfizer was developing elzasonan for the treatment of anxiety and affective disorders however development has been discontinued.
Status:
Investigational
Source:
Eur J Cancer Clin Oncol. May 1986;22(5):601-5.: Phase 2 Human clinical trial Completed Breast Neoplasms
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Carubicin (also known as Carminomycin) is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. The drug is active against a variety of experimental tumors. Pharmacology studies in animals revealed that the drug bound largely to serum proteins and that it was widely distributed. In clinical trials The main toxic effect was myelosuppression but gastrointestinal intolerance and alopecia were also reported. Objective partial responses were seen in two of seven previously untreated patients with non-small cell lung cancer and one of three patients with squamous cell carcinoma of the head and neck previously untreated with chemotherapy.
Status:
Investigational
Source:
USAN:ISOMYLAMINE HYDROCHLORIDE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
ISOMYLAMINE is a spasmolytic and smooth muscle relaxant.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Nalmexone is an opioid partial agonist or mixed agonist-antagonist with both analgesic and narcotic antagonist properties. In preclinical models parenteral nalmexone was a moderately active antagonist and therefore might have low abuse potential. At the same time, early work in man indicated analgesic
activity in doses above 20 mg.
Status:
Investigational
Source:
NCT00363454: Phase 1 Interventional Completed Cancer
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Triciribine is a purine analogue which inhibits DNA and protein synthesis, it is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. It inhibits cell growth and induces apoptosis preferentially in cells that express aberrant Akt1. In whole cells triciribine is phosphorylated by adenosine kinase which may be necessary for its activity. Triciribine is a cancer drug which was first synthesised in the 1970s and trialled clinically in the 1980s and 1990s without success. Following the discovery in the early 2000s that the drug would be effective against tumours with hyperactivated Akt, it is now again under consideration in a variety of cancers. As PTX-200, the drug is currently in two early stage clinical trials in breast cancer and ovarian cancer being conducted by the small molecule drug development company Prescient Therapeutics.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sabcomeline (SB-202026) is a potent and functionally selective M1 receptor partial agonist that originally was developed by GlaxoSmithKline. Sabcomeline had been in phase III clinical trials for the treatment of Alzheimer's disease and phase II for schizophrenia and major depressive disorder. In addition, it was studied for patients with Type 2 diabetes mellitus. However, due to poor results, the development of this drug was discontinued.
Status:
Investigational
Source:
NCT00069875: Phase 2 Interventional Completed Carcinoma, Non-Small-Cell Lung
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Etalocib (LY-293111 or VML 295) is a potent and orally active leukotriene B4 receptor antagonist of the biphenylphenol class. It efficiently blocks neutrophil activation and subsequent inflammation. Additionally, it exerts antineoplastic properties through induction of cell cycle arrest and apoptosis in tumor cells. Etalocib was being developed for the treatment of inflammatory diseases and solid tumors.
Status:
Investigational
Source:
NCT00540657: Phase 2 Interventional Completed Celiac Disease
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Vercirnon (GSK-1605786, CCX-282, nTraficet-EN) is a selective, and potent antagonist of human CCR9. Vercirnon binds to the intracellular side of the receptor, exerting allosteric antagonism and preventing G-protein coupling. CCR9 is a tissue-specific lymphocyte trafficking molecule that selectively attracts both B- and T-cells to the small gut. Inhibition of CCR9 by GSK-1605786 may inhibit B- and T-cell entry to the small gut and ameliorate inflammation while leaving immune function at other anatomical sites unaffected. Vercirnon is an orally bioavailable, anti-inflammatory agent that is being developed by ChemoCentryx for treatment of inflammatory bowel disease with an initial focus in Crohn's disease. A pivotal phase III programme of vercirnon was initiated in patients with moderate-to-severe Crohn's disease, however, the programme was suspended when the first pivotal trial failed to meet its primary endpoint. Phase II trials for ulcerative colitis and celiac disease were conducted, however investigations for ulcerative colitis were suspended while no further development has been reported for celiac disease.
Status:
Investigational
Source:
NCT00206284: Phase 2 Interventional Completed GERD Without Erosive Esophagitis
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Linaprazan is a member of a new group of acid-suppressing agents, which unlike proton pump inhibitors, act through potassium-competitive inhibition of the H+,K+-ATPase located in the apical membrane of parietal cells. It displayed rapid inhibition of acid production and had a prolonged, dose-dependent duration of effect. Linaprazan reduced porcine renal Na(+),K(+)-ATPase activity by 9+/-2%, demonstrating a high selectivity for H(+),K(+)-ATPase. It provided similar efficacy to esomeprazole in terms of esophagitis healing and heartburn control.
Status:
Investigational
Class (Stereo):
CHEMICAL (MIXED)
Naranol is an antidepressant, anxiolytic, and antipsychotic drug.