Encenicline
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| Clinical data | |
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| ATC code | None |
| Identifiers | |
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| CAS Number | 550999-75-2 |
| PubChem (CID) | 46196517 |
| ChemSpider | 28637768 |
| ChEMBL | CHEMBL2151572 |
| Chemical and physical data | |
| Formula | C16H17ClN2OS |
| Molar mass | 320.837 g/mol |
| 3D model (Jmol) | Interactive image |
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Encenicline (INN, USAN) (code names EVP-6124, MT-4666) is a selective partial agonist of the α7 nicotinic receptor, and is in phase III clinical trials for the treatment of cognitive impairment in schizophrenia.[1][2]
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 2mg/day, with the most positive of effects having been realized in patients taking the largest dose (2mg/day). In the Phase III trial, all patients were treated with 3mg/day doses of the drug. FORUM also speculates that the increase of GI 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 regards 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 GI problems. [3]
See also
References
- ↑ Melville, Nancy A. "Novel Drug Targets 'Huge Unmet Need' in Schizophrenia". Medscape. Retrieved 13 April 2015.
- ↑ Barbier, AJ (2015-02-01). "Pharmacodynamics, Pharmacokinetics, Safety, and Tolerability of Encenicline, a Selective α7 Nicotinic Receptor Partial Agonist, in Single Ascending-dose and Bioavailability Studies". Clinical Therapeutics. 37 (2): 311–24. doi:10.1016/j.clinthera.2014.09.013. PMID 25438724.
- ↑ Rare but Severe Side Effects Sideline Some Phase 3 Encenicline Trials|http://www.alzforum.org/news/research-news/rare-severe-side-effects-sideline-some-phase-3-encenicline-trials