Encenicline (
INN
Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...
,
USAN
280px, "Samguk Sagi" Book 04. Silla's Records. In 512, Usan-guk（于山國）was Ulleungdo（鬱陵島）
Usan-guk, or the State of Usan, occupied Ulleung-do and the adjacent islands during the Korean Three Kingdoms period. According to th ...
, code names EVP-6124, MT-4666) is a selective
partial agonist
In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonis ...
of the
α7 nicotinic receptor. It was in
phase III clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, diet ...
s for the treatment of
cognitive impairment
Cognitive deficit is an inclusive term to describe any characteristic that acts as a barrier to the cognition process.
The term may describe
* deficits in overall intelligence (as with intellectual disabilities),
* specific and restricted defici ...
in
schizophrenia
Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social wit ...
, but failed to meet the study endpoints in 2016.
FORUM Pharmaceuticals, who currently is subjecting the drug to the FDA approval process, had all studies suspended until further notice in fall of 2015 due to rare, but serious gastrointestinal problems occurring in patients participating in the drug trial, potentially being a consequence of taking the drug. The trials were scheduled to be run until January 2017, but as of December 2016, they appear to still be on hold. There is speculation by FORUM Pharmaceuticals that this may be due to either the increased daily dose given in the phase III trial compared to earlier trials that showed promise. In previous trials, the highest dose given was 2 mg/day, with the most positive of effects having been realized in patients taking the largest dose (2 mg/day). In the phase III trial, all patients were treated with 3 mg/day doses of the drug. FORUM also speculates that the increase of gastrointestinal problems occurring in the phase III trial could be due to the increased demographic risk that elderly (the average age in the study was 75) and those with Alzheimer's disease have in regard to gastrointestinal issues, citing another study they conducted with a younger demographic (in which the average age was 35–40) for the treatment of schizophrenia of 1,500 individuals in which there were zero complains of gastrointestinal problems.
See also
*
AR-R17779
*
Bradanicline
*
GTS-21
GTS-21 (DMXBA) is a derivative of the natural product anabaseine that acts as a partial agonist at neural nicotinic acetylcholine receptors. It binds to both the α4β2 and α7 subtypes, but activates only the α7 to any significant extent.
...
*
PHA-543,613
PHA-543,613 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors, with a high level of brain penetration and good oral bioavailability. It is under development as a possible treatm ...
*
PNU-282,987
*
SSR-180,711
*
TC-1698
TC-1698 is a drug developed by Targacept which acts as a partial agonist for the α7 subtype of neural nicotinic acetylcholine receptors. It has neuroprotective effects in animal studies, and has been used as a lead compound to find further pot ...
*
WAY-317,538
References
External links
*
Benzothiophenes
Carboxamides
Chloroarenes
Experimental drugs
Nicotinic agonists
Nootropics
Stimulants
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