Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C16H17ClN2OS.ClH.H2O |
| Molecular Weight | 375.313 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.Cl.ClC1=CC=CC2=C1SC(=C2)C(=O)N[C@H]3CN4CCC3CC4
InChI
InChIKey=OYFJBYJMAHEUQV-GXKRWWSZSA-N
InChI=1S/C16H17ClN2OS.ClH.H2O/c17-12-3-1-2-11-8-14(21-15(11)12)16(20)18-13-9-19-6-4-10(13)5-7-19;;/h1-3,8,10,13H,4-7,9H2,(H,18,20);1H;1H2/t13-;;/m0../s1
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C16H17ClN2OS |
| Molecular Weight | 320.837 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | H2O |
| Molecular Weight | 18.0153 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/22085888 | https://www.ecnp.eu/~/media/Files/ecnp/Projects%20and%20initiatives/Medicines%20Chest/EVP%206124.pdf
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/22085888 | https://www.ecnp.eu/~/media/Files/ecnp/Projects%20and%20initiatives/Medicines%20Chest/EVP%206124.pdf
Encenicline (EVP-6124; MT-4666) acts as a potent partial and selective agonist at alpha-7 nicotinic acetylcholine receptor. Encenicline significantly improved memory function in animal models. FORUM Pharmaceuticals (formerly EnVivo Pharmaceuticals) is developing encenicline for the treatment of cognition disorders such as schizophrenia and for Alzheimer's disease.
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
35.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
4.66 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
0.588 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
100 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2800 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
358 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
45.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
8890 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
63 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
60.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
52.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
60.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25438724 |
180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered: |
ENCENICLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Natalizumab: AN 100226, anti-4alpha integrin monoclonal antibody. | 2004 |
|
| Discovery and development of α7 nicotinic acetylcholine receptor modulators. | 2011 Dec 8 |
|
| Randomized, Double-Blind, Placebo-Controlled Study of Encenicline, an α7 Nicotinic Acetylcholine Receptor Agonist, as a Treatment for Cognitive Impairment in Schizophrenia. | 2015 Dec |
Patents
Sample Use Guides
Encenicline was well tolerated at single doses up to 180 mg, and doses as low as 1 mg had dose- and time-dependent pharmacodynamic effects on the central nervous system.
Results from a phase IIb trial showed that encenicline (2.0mg once daily) significantly improved cognition and clinical function in patients with mild-to-moderate Alzheimer's disease.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
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9201D24ZB5
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Validated (UNII)
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1350343-61-1
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ANHYDROUS->SOLVATE |
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ACTIVE MOIETY |
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