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

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Showing 1061 - 1070 of 34988 results

Status:
Investigational
Source:
NCT04469023: Phase 2 Interventional Completed Patients with Insomnia
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:batelapine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Batelapine (or CGS 13429), an antipsychotic drug, that was undergoing preclinical development, but the further studied were discontinued
Status:
Investigational
Source:
NCT00689221: Phase 3 Interventional Completed Glioblastoma
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Cilengitide is a cyclized Arg-Gly-Glu (RGD)-containing pentapeptide that selectively blocks activation of the αvβ3 and αvβ5 integrins. Its precursor was first synthesized in 1995 as c(RGDfV), and later modified by the incorporation of N-methyl Val c(RGDfMetV), generating the current form of the drug. Cilengitide displays subnanomolar antagonistic activity for αvβ3 and αvβ5, and is the first integrin antagonist evaluated in clinical phase I and II trials for treatment of glioblastoma and several other tumor types. Cilengitide-induced glioma cell death and inhibition of blood vessel formation may use different molecular mechanisms, including regulation of tumor hypoxia and activation of apoptotic pathways. Cilengitide inhibits cell signaling through FAK-Src-Akt and Erk mediated pathways in endothelial and tumor cells and attenuates the effect of VEGF stimulation on growth factor signaling. Cilengitide has shown encouraging activity in patients with glioblastoma as single agent, and in association with standard RT and temozolomide.
Status:
Investigational
Source:
NCT01871428: Phase 3 Interventional Completed Diabetes Mellitus Type 2
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Aleglitazar is a dual agonist of PPARalpha/PPARgamma which was developed by Hoffmann-La Roche for the treatment of type 2 diabetes. Aleglitazar activates PPAR receptors with EC50 in nanomolar range and exerts a cardioprotective effect in vitro. The drug is currently in phase III of clinical trials.
Status:
Investigational
Source:
INN:vebufloxacin
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Vebufloxacin (OPC-7241) is a nalidixic acid analog. It exhibited potent antibacterial activity against gram-positive and -negative bacteria, including Staphylococcus aureus and Pseudomonas aeruginosa.
Status:
Investigational
Source:
NCT02391480: Phase 1 Interventional Completed Cancer
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Mivebresib (ABBV-075) is a small molecule Bromodomain and Extra-Terminal motif (BET) inhibitor being studied in a Phase 1 clinical trial in patients with advanced hematologic malignancies and solid tumors. Mivebresib binds to BRD4 with a Ki of 1.5 nM. Comprehensive preclinical characterization of ABBV-075 demonstrated broad activity across cell lines and tumor models, representing a variety of hematologic malignancies and solid tumor indications. In most cancer cell lines derived from solid tumors, ABBV-075 triggers prominent G1 cell-cycle arrest without extensive apoptosis. Consistent with its broad spectrum of activities in vitro, ABBV-075 has comparable or superior efficacies to standard of care agents in flank xenograft mouse models of non-small-cell and small cell lung cancers, pancreatic, breast, prostate, head & neck cancers, multiple myeloma, diffuse large B cell lymphoma and leukemia.
Alvameline is a partial agonist of the M1 mAChR that also displays M2/M3 antagonist effects. It readily crosses the blood-brain barrier. It has an effect profile that makes it of interest to test its ability to counteract bladder overactivity in humans. Behaviorally, alvameline has been shown to significantly improve Morris water maze (MWM) performance in both young and ageimpaired rats. It failed to improve cognition in patients with mild to moderate Alzheimer's disease.
Status:
Investigational
Source:
INN:carbofenotion
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Carbophenothion is a highly toxic organophosphate insecticide used as a citrus pesticide called Trithion. Carbophenothion is a potent inhibitor of acetylcholinesterase, a neuromuscular enzyme that is widely needed for the normal function of insects, as well as people and many other animals. The Environmental Protection Agency (EPA) classifies it as a Restricted Pesticide (RUP). Carbophenothion is used in various brands, such as Trithion. This pesticide contains 80% Carbophenothion as its only active ingredient. Due to the widespread use of these organophosphates in the United States in the nineties, this was the most common cause of agricultural poisoning. Carbophenothion is used as an insecticide and acaricide, the main purpose of which is to protect citrus fruits, but also to protect the cotton from aphids (lice) and spider mites. In addition, it is used in combination with oil, and also as a pesticide against many other pests on fruits, nuts, vegetables, sorghum, corn, and others. In addition, it is used to combat animal parasites.
Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research. In humans, ritanserin increases deep slow-wave sleep, improved liveliness in a variety of psychiatric disorders and facilitated participation in behaviour therapy. During clinical trials, unexpected observations indicated that ritanserin may be of value in treating obsessive-compulsive disorder, acute mania, negative symptoms of schizophrenia, drug addicts, etc. Clinical observations confirmed the efficacy of ritanserin in the chronic withdrawal phase after detoxification from ethanol. Ritanserin had been in phase III clinical trials by Janssen L.P. for the treatment of anxiety disorder and major depressive disorder. However, the clinical development of ritanserin was discontinued.
Status:
Investigational
Source:
NCT01487551: Phase 2 Interventional Completed Systemic Sclerosis
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Paquinimod is an immunomodulatory compound preventing S100A9 binding to TLR-4. It was studied in experimental osteoarthritis, in patients with mild active systemic lupus erythematosus and in systemic sclerosis patients. In January 2014, the US FDA granted orphan drug designation to paquinimod for the treatment of systemic scleroderma. The Orphan designation is implemented to promote the development of drugs that may provide significant benefit to patients suffering from rare diseases identified as life threatening or chronically debilitating. The further development of paquinimod for systemic lupus erythematosus and rheumatoid arthritis was discontinued.

Showing 1061 - 1070 of 34988 results