U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 901 - 910 of 34988 results

Status:
Investigational
Source:
NCT02303262: Phase 2 Interventional Completed Metastatic Leiomyosarcoma
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



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:
INN:timefurone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Timefurone is a benzopyranone derivative patented by pharmaceutical company Upjohn Co. for the treatment of atherosclerosis. Timefurone mediates the hypolipidemic effect via the reduction of the intracellular synthesis of cholesterol. In preclinical studies, Timefurone significantly lowered low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and total cholesterol in cholesterol-fed male rats and monkeys. Timefurone caused small but significant changes in several clinical chemistry parameters including creatinine, total bilirubin, albumin, glucose, serum glutamic-oxalacetic transaminase, and serum glutamic-pyruvic transaminase in cynomolgus monkeys
Status:
Investigational
Source:
NCT00763022: Phase 3 Interventional Completed Diabetes Mellitus
(2003)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Imiglitazar (also known as TAK-559) is a dual peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist patented by Japanese pharmaceutical company Takeda Chemical Industries for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance, and impaired glucose tolerance. Imiglitazar shows potent hypoglycemic and hypolipidemic activity and has been studied in clinical trials in treating subjects receiving a stable dose of insulin to control type 2 diabetes mellitus. Unfortunately, Imiglitazar shows hepatotoxicity and has never been marketed.
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.
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.
Metitepine, a psychotropic agent was developed as a non-selective antagonist of serotonin, dopamine, and adrenergic receptors. Metitepine has never been marketed.
Status:
Investigational
Source:
INN:lixumistat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02795832: Phase 1/Phase 2 Interventional Completed Atopic Dermatitis
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:flavamine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

FLAVAMINE is a diterpenoid alkaloid isolated from the roots of Aconitum fiavum.
Status:
Investigational
Source:
INN:fidexaban [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

FIDEXABAN is a potent inhibitor of coagulation factor Xa with anticoagulant activity. Like other factor Xa inhibitors, it prevents thrombus formation.