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

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Showing 1601 - 1610 of 34144 results

Status:
Investigational
Source:
USAN:SCOPAFUNGIN [USAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Scopafungin (also known as GE4800) is an inhibitor of oxidative phosphorylation in mitochondria. Scopafungin also inhibits, in vitro, a variety of pathogenic fungi, yeasts, and gram-positive bacteria.
Status:
Investigational
Source:
INN:metindizate
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Metindizate was developed as a spasmolytic agent. Information about the current use of this compound is not available.
Status:
Investigational
Source:
JAN:TERALLETHRIN [JAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Terallethrin is an insecticide that controls flying insects including houseflies, wasps and mosquitoes.
Status:
Investigational
Source:
NCT04321343: Phase 2 Interventional Completed NASH - Nonalcoholic Steatohepatitis
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:cefoselis
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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:
NCT03084952: Phase 2 Interventional Unknown status Leishmaniasis; American, Cutaneous
(2021)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

18-Methoxycoronaridine (18-MC) is a derivative of ibogaine invented in 1996 by the research team around the pharmacologist Stanley D. Glick from the Albany Medical College and the chemist Martin E. Kuehne from the University of Vermont. In animal studies it has proved to be effective at reducing self-administration of morphine, cocaine, methamphetamine, nicotine and sucrose. 18-MC is a α3β4 nicotinic antagonist and, in contrast to ibogaine, has no affinity at the α4β2 subtype nor at NMDA-channels nor at the serotonin transporter, and has significantly reduced affinity for sodium channels and for the σ receptor, but retains modest affinity for μ-opioid receptors where it acts as an antagonist, and κ-opioid receptors. The sites of action in the brain include the medial habenula, interpeduncular nucleus, dorsolateral tegmentum and basolateral amygdala. Unlike ibogaine and its principal metabolite noribogaine, 18-MC does not increase expression of glial cell line-derived neurotrophic factor (GDNF) in a dopaminergic–like cell line. 18-Methoxycoronaridine is a potent leishmanicide effect against Leishmania amazonensis, a causative agent of cutaneous and diffuse cutaneous leishmaniasis in the New World.
Status:
Investigational
Source:
NCT01732237: Phase 1 Interventional Completed Healthy
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

JNJ-42396302 was under investigation in clinical trial NCT01732237 (A Study to Investigate the Pharmacokinetics of JNJ-42396302, JNJ-53773187, and JNJ-42692507 in Healthy Male Participants).
Status:
Investigational
Source:
NCT01496495: Phase 1 Interventional Completed Myelodysplastic Syndromes
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with potential antineoplastic, anti-inflammatory and antiangiogenic activities. Pexmetinib inhibited leukemic proliferation, prevented activation of downstream effector kinases and abrogated the effects of TNF-alpha on healthy hematopoietic stem cells. In ex vivo stimulated human whole blood, LPS-induced cytokines was inhibited by Pexmetinib with an IC50 value ranging from 50-120 nM. ARRY-614 inhibited the release of IL-6 from SEA- or LPS-challenged mice with an ED50 value less than 10 mg/kg. Combining Pexmetinib with lenalidomide inhibited both pro-inflammatory cytokines and tumor growth in vivo with higher potency, compared with either agent alone. In dose escalation or expansion cohorts, treatment with Pexmetinib either once daily or twice daily was applied to forty-five patients. Pexmetinib reduced the levels of circulating biomarkers and the p38 MAPK activation of bone marrow.

Showing 1601 - 1610 of 34144 results