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Showing 721 - 730 of 4227 results

Status:
Investigational
Source:
NCT00838890: Phase 1/Phase 2 Interventional Terminated Refractory Hematologic Cancer
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



BMS-863233, also known as XL413, is a potent and selective cell division cycle 7 (CDC7) kinase inhibitor with potential antineoplastic activity. BMS-863233 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induction of tumor cell apoptosis, and the inhibition of tumor cell proliferation in CDC7-overexpressing tumor cells. CDC7, a serine-threonine kinase overexpressed in a variety of tumor cell types, plays an essential role in the initiation of DNA replication by activating origins of replication.
Status:
Investigational
Source:
NCT00832546: Phase 1 Interventional Completed Healthy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tezampanel, also known as LY 293558 and NGX-424, is a drug originally developed by Eli Lilly, which is a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family. Tezampanel was in phase II clinical trial for treatment migraine, but this study was discontinued. Also this drug has several others potential pharmacological actions, one of them is anxiety disorders
Status:
Investigational
Source:
NCT00057213: Phase 2 Interventional Completed Depressive Disorder, Major
(2003)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Radafaxine (GW353162, ( )-(2S,3S)-2-(3-chlorophenyl-3,5,5-trimethyl-2-morphinol) or S,S-hydroxybupropion) is an active metabolite of bupropion. It acts as an inhibitor of the dopamine transporter. Radafaxine was investigated for the treatment of depression however, development was discontinued.
Aplindore (DAB-452) is a small molecule that displays potent dopamine D2 receptor partial agonist activity in in vitro and in vivo assays and is predicted to have antipsychotic efficacy without motor side effects. Aplindore had been in phase II clinical trials for the treatment of Parkinson's disease and restless legs syndrome. Aplindore was generally well tolerated and there were no withdrawals due to adverse events and no serious adverse events.
Millennium Pharmaceuticals Inc's tandutinib (MLN-518), a piperazinyl derivative of quinazoline, is an orally active inhibitor of FLT3 kinase and family members PDGFR beta and c-Kit. Tandutinib inhibited FLT3 phosphorylation, downstream signaling and malignant growth in vitro and in animal models. The drug exhibited limited activity as a single agent in phase I and II clinical trials in patients with AML and myelodysplastic syndrome, but displayed promising antileukemic activity (90% complete remissions) in a phase I/II trial in patients with newly diagnosed AML when administered in combination with cytarabine and daunorubicin. Phase II clinical trials for tandutinib in patients with Glioblastoma have being discontinued. The use of tandutinib to treat AML has been granted fast-track status by the U.S. Food and Drug Administration. Phase II trials were underway., but later withwrawn.
Status:
Investigational
Source:
NCT00300963: Phase 2 Interventional Completed Schizophrenia
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Talnetant (SB-223412) is a selective, orally active neurokinin 3 receptor antagonist and is under development for the potential treatment of several disorders, including irritable bowel syndrome, schizophrenia, chronic obstructive pulmonary disease, cough, overactive bladder and urinary incontinence. The most common adverse effects were headache, fatigue, and nausea.
Status:
Investigational
Source:
INN:atocalcitol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Atocalcitol is a vitamin D analogue. A hallmark of vitamin D3 analogues in psoriasis amelioration is the ability to inhibit the proliferation of keratinocytes. Atocalcitol had been in phase II clinical trials for the treatment of psoriasis. However, this research has been discontinued.
Status:
Investigational
Source:
NCT01357395: Phase 2 Interventional Completed Small Cell Lung Carcinoma
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Amuvatinib (formerly known as MP470) is an oral multi-targeted tyrosine kinase inhibitor, which play critical roles in transducing growth signals to cancer cells. It suppresses c-MET, c-RET and the mutant forms of cKIT, PDGFR and FLT3. It also disrupts DNA repair likely through suppression of homologous recombination protein Rad51, an important survival pathway in many human cancers. In vitro and in vivo data have demonstrated amuvatinib synergy with DNA damaging agents including etoposide and doxorubicin. Overall, in the amuvatinib clinical development program, over 200 subjects were exposed to at least one dose of amuvatinib. In the Phase 1b clinical study in combination with carboplatin and etoposide, responses in small cell lung cancer (SCLC), neuroendocrine as well as other tumor types were observed. Human pharmacokinetic data suggest that co-administration of amuvatinib did not alter exposures of standard of care agents including carboplatin, etoposide, doxorubicin, paclitaxel, topotecan or erlotinib as measured by overall exposure. In the first-in-human study, durable clinical benefit was observed in the gastrointestinal stromal tumors (GIST) with modulation of Rad51 observed in skin punch biopsies. In clinical trials, amuvatinib has demonstrated a wide therapeutic window and shows minimal toxicity in the expected therapeutic dose range, despite suppressing several signaling pathways within cells. However, in spite of this, this drug was discontinued, because it was not pre-specified primary endpoints in the clinical proof of concept (cPOC) stage. But the combination of MP470 and Erlotinib, which target the HER family/PI3K/Akt pathway may represent a novel therapeutic strategy for prostate cancer.
Status:
Investigational
Source:
INN:cetaben [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Cetaben has been identified as an anti-atherosclerotic hypolipidaemic substance. Cetaben is a unique, PPARα-independent peroxisome proliferator with hypolipidemic activity that inhibits cholesterol synthesis in the human hepatoma Hep-G2 cells resulting in reversible changes in Golgi morphology. Cetaben represents an exceptional type of peroxisome proliferator, specifically affecting peroxisomes, without having a negative influence on the processes of peroxisome biogenesis. Cetaben raised only the peroxisomal enzymes, acyl-CoA oxidase, glycerone-phosphate acyltransferase, D-amino-acid oxidase, catalase, and urate oxidase. Cetaben sodium has being shown to be an antiatherosclerotic agent.
Status:
Investigational
Source:
NCT01214603: Phase 2 Interventional Completed Leukemia
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



LY-2090314 is a GSK-3alpha and GSK-3beta inhibitor developed by Eli Lilly. Phase 2 clinical trials of LY-2090314 as a signle agenst against acute leukemia did not show clinical benefit. LY-2090314 was studied in combination pemetrexed and carboplatin against solid tumors, and in combination with FOLFOX, gemcitabine, and nab-paclitaxel against pancreatic cancer.