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Restrict the search for
vitamin a
to a specific field?
Status:
Investigational
Source:
NCT02303262: Phase 2 Interventional Completed Metastatic Leiomyosarcoma
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Mocetinostat is an rationally designed, orally available, Class 1-selective, small molecule, 2-aminobenzamide HDAC inhibitor with potential antineoplastic activity. Mocetinostat binds to and inhibits Class 1 isoforms of HDAC, specifically HDAC 1, 2 and 3, which may result in epigenetic changes in tumor cells and so tumor cell death; although the exact mechanism has yet to be defined, tumor cell death may occur through the induction of apoptosis, differentiation, cell cycle arrest, inhibition of DNA repair, upregulation of tumor suppressors, down regulation of growth factors, oxidative stress, and autophagy, among others. It is undergoing clinical trials for treatment of various cancers including bladder cancer, diffuse large B cell lymphoma, follicular lymphoma, myelodysplastic syndromes, non-small cell lung cancer. Fatigue, weight loss or anorexia were most common treatment-related adverse events.
Status:
Investigational
Source:
NCT00163085: Phase 2 Interventional Completed Parkinson's Disease
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Traxoprodil (CP-101,606) is a potent, selective N-Methyl-D-aspartate (NMDA) receptor (NR2B subunit) antagonist under development by Pfizer for its potential as a neuroprotectant in head injury and neurodegenerative disease. It is in phase II trials in the US and in phase I in Japan for the potential treatment of head injury, such as, Depressive Disorder, Major and Parkinson's Disease. CP-101,606 does not protect against glutamate-induced neurotoxicity in cultured cerebellar neurons, up to a dose of 10 uM. These results are consistent with CP-101,606 being a potent NMDA antagonist, selective for the type of NMDA receptor associated with the hippocampus. Some further investigation revealed that CP-101,606 was associated with a dose-related dissociation and amnesia. These results support the hypothesis that glutamate antagonists may be useful antidyskinetic agents. However, future studies will have to determine if the benefits of dyskinesia suppression can be achieved without adverse cognitive effects.
Status:
Investigational
Source:
NCT00405054: Phase 2 Interventional Terminated Leukemia
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Tozasertib, originally developed as VX-680 by Vertex (Cambridge, MA) and later renamed MK-0457 by Merck (Whitehouse Station, NY), was the first aurora kinase inhibitor to be tested in clinical trials. The drug, a pyrimidine derivative, has affinity for all aurora family members at nanomolar concentrations with inhibitory constant values (Ki(app)) of 0.6, 18, and 4.6 nM for aurora A, aurora B, and aurora C, respectively. Preclinical studies confirmed that tozasertib inhibited both aurora A and aurora B kinase activity, and activity has been reported against prostate, thyroid, ovarian, and oral squamous cancer cell lines. Upon treatment with tozasertib, cells accumulate with a 4N DNA content due to a failure of cytokinesis. This ultimately leads to apoptosis, preferentially in cells with a compromised p53 function. Tozasertib is an anticancer chemotherapeutic pan-aurora kinase (AurK) inhibitor that also inhibits FMS-like tyrosine kinase 3 (FLT3) and Abl. Tozasertib is currently in clinical trials as a potential treatment for acute lymphoblastic leukemia (ALL). In cellular models of cancer, tozasertib activates caspase-3 and PARP and decreases expression of HDAC, increasing apoptosis and inhibiting cell growth. In other cellular models, tozasertib inhibits cell proliferation and metastasis by blocking downstream ERK signaling and downregulating cdc25c and cyclin B. This compound also decreases tumor growth in an in vivo model of prostate cancer.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Aranotin, a metabolite of Arachniotus aureus, possesses the antiviral and antibiotic properties. It inhibits viral RNA synthesis against strains of rhino-, coxsackie, polio- and parainfluenza viruses.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT04711252: Phase 3 Interventional Active, not recruiting ER-Positive HER2-Negative Breast Cancer
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Class (Stereo):
CHEMICAL (RACEMIC)
Taziprinone was studied as an antitussive agent. Information about the current use of this compound is not available.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Sunepitron (CP-93,393) is an anxiolytic drug with highly selective serotonin 5-hydroxytryptamine 1A autoreceptor agonist, alpha2-adrenergic antagonist, and dopamine D2 agonist properties. Sunepitron hydrochloride had been in Phase III clinical trials by Pfizer for the treatment of anxiety disorder and depression. However, this research has been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Sulazuril (also known as Hoe 092 V) is a phenyltriazolone derivative patented by Hoechst A.-G. as agrochemical protozoacide. Sulazuril is effective against a broad spectrum of fish and crustacean parasites.
Status:
Investigational
Source:
INN:lutetium (<sup>177</sup>Lu) zadavotide guraxetan [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
