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

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Artenimol (dihydroartemisinin) is a derivate of antimalarial compound artemisinin. Artenimol (dihydroartemisinin) is able to reach high concentrations within the parasitized erythrocytes. Its endoperoxide bridge is thought to be essential for its antimalarial activity, causing free-radical damage to parasite membrane systems including: • Inhibition of falciparum sarcoplasmic-endoplasmic reticulum calcium ATPase, • Interference with mitochondrial electron transport • Interference with parasite transport proteins • Disruption of parasite mitochondrial function. Dihydroartemisinin in combination with piperaquine tetraphosphate (Eurartesim, EMA-approved in 2011) is indicated for the treatment of uncomplicated Plasmodium falciparum malaria. The formulation meets WHO recommendations, which advise combination treatment for Plasmodium falciparum malaria to reduce the risk of resistance development, with artemisinin-based preparations regarded as the ‘policy standard’. However, experimental testing demonstrates that, due to its intrinsic chemical instability, dihydroartemisinin is not suitable to be used in pharmaceutical formulations. In addition, data show that the currently available dihydroartemisinin preparations fail to meet the internationally accepted stability requirements.
Status:
Investigational
Source:
INN:isatoribine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

ISATORIBINE, a guanosine analog, is an immunopotentiating agent. It is a selective agonist of toll‐like receptor 7, a pattern-recognition receptor that activates the innate immune response.
Status:
Investigational
Source:
NCT00454870: Phase 2 Interventional Completed Alzheimer's Disease
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Facinicline (MEM-63908 or R-4996) is a selective nicotinic alpha-7 receptor (α7nAChR) partial agonist. It also has properties of a serotonin 3 receptor antagonist. It has hydrochloride form: RG3487 (formerly MEM3454). Facinicline enhances DA efflux by nAChR stimulation, whereas ACh efflux is primarily mediated via 5-HT3 receptor antagonism. It improves cognition and sensorimotor gating in rodents. It has been tested in Alzheimer's disease and cognitive symptoms of schizophrenia.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

Concept
Status:
Other

Class:
CONCEPT