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

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Showing 1331 - 1340 of 24423 results

Status:
Investigational
Source:
INN:dizocilpine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dizocilpine (MK-801) is an antagonist of the N-methyl-D-aspartate (NMDA) receptor in the glutamate category involved with the central nervous system (CNS). The drug displays a variety of physiological actions, many of which involve the CNS, such as anesthetic and anticonvulsant properties. It penetrates readily into CNS and was described as the agent with central sympathomimetic properties. Co-administration of dizocilpine with psychostimulants, such as cocaine, amphetamine and nicotine, has been reported to prevent the development of behavioural sensitization to these drugs as well as associated neuroadaptations in rodents. However, studies with bromocriptine have suggested that co-administration of dizocilpine might merely cause sensitization to become state-dependent. A single injection of MK-801 to rats models both positive and negative symptoms of schizophrenia. Treatment of mice with dizocilpine induced learning impairment.
Status:
Investigational
Source:
INN:phencyclidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Phencyclidine is an illegal, hallucinogenic drug that was initially used as an anesthetic agent in the 1950s and early 1960s, but was then withdrawn in 1965 because of dissociative hallucinogenic effects that were often disturbing and sometimes severe and prolonged. Phencyclidine is a noncompetitive NMDA (N-methyl-D-aspartate) receptor antagonist and glutamate receptor antagonist, but also interacts with other receptor sites, and may have effects with dopamine, opioid and nicotinic receptors. Phencyclidine disrupts the functioning of receptors for the neurotransmitter glutamate, which plays a major role in the perception of pain as well as in learning, memory, and emotion. It also influences the actions of the neurotransmitter dopamine, which causes the euphoria associated with drug use. Phencyclidine overdose deaths may occur after taking a large dose, though many phencyclidine related deaths result from delusions and other psychological consequences of the drug’s use. There have been reports of death due to accidental drowning, leaping from high places, and motor vehicle accidents in addition to violent episodes of self-mutilation, suicides, and homicides.
Status:
Investigational
Source:
NCT03920982: Not Applicable Interventional Unknown status Acute Kidney Injury
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT04263337: Phase 1 Interventional Enrolling by invitation Concussion, Brain
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02332720: Phase 2 Interventional Completed Hepatitis C
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ruzasvir (previously known as MK-8408) was developed as a nonstructural protein 5A (NS5A) inhibitor for the treatment of hepatitis C and hepatitis C infection. Ruzasvir successfully completed phase II clinical trial for combination therapy. The obtained results have shown that ruzasvir in combination with uprifosbuvir was highly effective and well-tolerated in participants infected with hepatitis C virus genotypes GT1, GT2, GT4, GT5, and GT6, with a lower efficacy in GT3-infected persons.
Status:
Investigational
Source:
NCT01724320: Phase 1 Interventional Unknown status Solid Tumors
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Conditions:

PTX-008 (OTX008) is a calixarene-based compound and galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities. Upon subcutaneous administration, galectin-1 inhibitor OTX008 binds Gal-1 which leads to Gal-1 oxidation and proteosomal degradation through a not yet fully elucidated mechanism, and eventually downregulates Gal-1. This decreases tumor cell growth and inhibits angiogenesis. Gal-1, a multifunctional carbohydrate-binding protein, is often overexpressed on tumor cells and plays a key role in cancer cell proliferation, apoptosis, tumor angiogenesis and evasion of immune responses. PTX-008 had been in phase I clinical trials for the treatment of solid tumours. This compound was originally discovered by University of Minnesota and PepTx, then licensed to OncoEthix (acquired by Merck Sharp & Dohme in 2014). However, no recent developments has been reported.
Status:
Investigational
Source:
NCT03747497: Phase 2 Interventional Completed Skin Diseases, Bacterial
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

MRX-I is a potent oxazolidinone antibiotic against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, penicillin-intermediate S. pneumoniae, and vancomycin-resistant enterococci. MRX-I demonstrated comparable or slightly higher activity than linezolid and was active against enterococci resistant to both vancomycin and teicoplanin. In addition, MRX-I exhibited bactericidal activities against staphylococci and streptococci but was bacteriostatic against enterococci. MRX-I inhibits formation of functional 70S initiation complex essential for bacterial protein synthesis, leading to the cessation of bacterial growth. Oral MRX-I was associated with a greater bioavailability and exposure when administered with food, and minimal accumulation of MRX-I occurred after multiple-dose administration. Oral MRX-I was well tolerated at single doses of up to 1,200 and 800 mg q12h for up to 28 days; all adverse events were mild to moderate in severity, and there was no drug discontinuation due to adverse events.
Status:
Investigational
Source:
NCT03216902: Phase 2 Interventional Completed Open-angle Glaucoma, Ocular Hypertension
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sepetoprost (also known as ONO-9054), prostaglandin analog was developed as a dual agonist of prostaglandin E3 (EP3) and prostaglandin F (FP) receptors. It is known, that the use of a dual prostaglandin EP3 and prostaglandin F receptor agonists is a novel approach for the reduction of intraocular pressure (IOP) in open-angle glaucoma and ocular hypertension. Sepetoprost was successfully studied in clinical trials phase II for the treatment of open-angle glaucoma, ocular hypertension, and mild open angle-glaucoma.
Status:
Investigational
Source:
NCT04379869: Phase 1 Interventional Completed Healthy Volunteers
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Showing 1331 - 1340 of 24423 results