NSI-189

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NSI-189 structure.svg
Systematic (IUPAC) name
(4-Benzylpiperazin-1-yl)-[2-(3-methylbutylamino)pyridin-3-yl]methanone
Clinical data
Pregnancy
category
  • US: N (Not classified yet)
Legal status
  • Unscheduled
Routes of
administration		 Oral[1]
Pharmacokinetic data
Biological half-life 17.4–20.5 hours[1]
Identifiers
CAS Number 1270138-40-3
PubChem CID: 50922681
ChemSpider 32701740
Chemical data
Formula C22H30N4O
Molecular mass 366.4998 g/mol
  • CC(C)CCNC1=C(C=CC=N1)C(=O)N2CCN(CC2)CC3=CC=CC=C3
  • InChI=1S/C22H30N4O/c1-18(2)10-12-24-21-20(9-6-11-23-21)22(27)26-15-13-25(14-16-26)17-19-7-4-3-5-8-19/h3-9,11,18H,10,12-17H2,1-2H3,(H,23,24)
  • Key:DYTOQURYRYYNOR-UHFFFAOYSA-N N

NSI-189 is an experimental, novel potential antidepressant that is under investigation by Neuralstem, Inc. for the treatment for major depressive disorder (MDD), as well as for cognitive impairment and neurodegeneration.[2][1][3] Research into NSI-189 has been funded by the Defense Advanced Research Projects Agency (DARPA) and the National Institutes of Health (NIH).[4] The mechanism of action of NSI-189 appears to be activation of neurogenesis in and possible enlargement of the hippocampus,[2] but how the drug mediates these effects is unknown, and binding studies have so far failed to identify any certain molecular targets for the drug.[3] As stated by Neuralstem, NSI-189 is a "new chemical entity with [a] novel mechanism of action, molecular target yet unknown, but not mediated by SSRI or SNRI or by BDNF release or via any known GPCRs, kinases, or channels." The drug was discovered via high-throughput screening of a library of 10,269 compounds for neurogenic effects in vitro.[3]

NSI-189 successfully completed a phase I clinical trial for MDD in 2011, where it was administered to 41 healthy volunteers.[5] A phase Ib clinical trial for treating MDD in 24 patients started in 2012 and completed in July 2014, with results published in December 2015.[6][1] Neuralstem is now preparing to initiate phase II clinical studies for MDD in the first quarter of 2016, with results expected in the second half of 2017.[3][1] In the two clinical studies conducted thus far, NSI-189 has shown statistically significant effectiveness in reducing depressive symptoms, has been found to be safe and well-tolerated (with no major adverse effects observed), and has been found to improve cognitive deficits in depressed patients.[2][3] In addition to MDD, Neuralstem intends to pursue clinical development of NSI-189 for a variety of other neurological conditions, including traumatic brain injury, Alzheimer's disease, post-traumatic stress disorder, stroke, and natural cognitive and memory decline in aging.[4][2]

See also

References

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  1. ↑ 1.0 1.1 1.2 1.3 1.4 Lua error in package.lua at line 80: module 'strict' not found.
  2. ↑ 2.0 2.1 2.2 2.3 Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ 3.0 3.1 3.2 3.3 3.4 Lua error in package.lua at line 80: module 'strict' not found.
  4. ↑ 4.0 4.1 FDA Approves Neuralstem To Treat Final Cohort In NSI-189 Phase Ib Trial In Major Depressive Disorder
  5. ↑ Single-Dose Pharmacokinetics (PK) Study of Novel Neurogenic Compound NSI-189
  6. ↑ Multiple-Dose Pharmacokinetics (PK), and Pharmacodynamic (PD) Effect of NSI-189 Phosphate in Depression Patient Subjects
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