NSI-189 - CAS 1270138-40-3
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
NSI-189
Catalog Number:
B-0084-462290
Synonyms:
NSI-189; NSI 189; NSI189
CAS Number:
1270138-40-3
Description:
NSI-189 is an experimental drug being studied by Neuralstem, Inc. Research into NSI-189 has been funded by the Defense Advanced Research Projects Agency (DARPA) and the National Institutes of Health (NIH) for the treatment of major depressive disorder. NSI-189 successfully completed a phase 1 clinical trial in 2011 where it was administered to 41 healthy volunteers. A phase 1b clinical trial for treating major depressive disorder in 24 patients started in 2012 and completed in July 2014. The study suggests that there were improvements in the patients' condition when the doses were 40/80 mg per day, but no significant improvements were seen for a higher dosage of 120 mg/day. Neuralstem intends to pursue further clinical trials for a variety of neurological conditions, including major depressive disorder, traumatic brain injury, Alzheimer's disease, post-traumatic stress disorder, stroke, and natural cognitive and memory decline in aging.
Molecular Weight:
366.5
Molecular Formula:
C22H30N4O
Quantity:
Grams-Kilos
Quality Standard:
Enterprise Standard
COA:
Certificate of Analysis-NSI-189 1270138-40-3 B15JP0412  
MSDS:
Inquire
Current Developer:
Neuralstem, Inc.
Chemical Structure
CAS 1270138-40-3 NSI-189

Reference Reading


1.A Phase 1B, randomized, double blind, placebo controlled, multiple-dose escalation study of NSI-189 phosphate, a neurogenic compound, in depressed patients.
Fava M1,2, Johe K3, Ereshefsky L4, Gertsik LG5, English BA4, Bilello JA6, Thurmond LM6, Johnstone J7, Dickerson BC8, Makris N8, Hoeppner BB1,2, Flynn M1, Mischoulon D1,2, Kinrys G1,2, Freeman MP1,2. Mol Psychiatry. 2015 Dec 8. doi: 10.1038/mp.2015.178. [Epub ahead of print]
We wanted to examine tolerability and efficacy of NSI-189, a benzylpiperizine-aminiopyridine neurogenic compound for treating major depressive disorder (MDD). This was a Phase 1B, double blind, randomized, placebo controlled, multiple-dose study with three cohorts. The first cohort received 40 mg q.d. (n=6) or placebo (n=2), the second cohort 40 mg b.i.d. (n=6) or placebo (n=2), and the third cohort 40 mg t.i.d. (n=6) or placebo (n=2). Twenty-four patients with MDD were recruited, with the diagnosis and severity confirmed through remote interviews. Eligible patients received NSI-189 or placebo for 28 days in an inpatient setting with assessments for safety, pharmacokinetics (PK) and efficacy. Outpatient follow-up visits were conducted until day 84 (±3). NSI-189 was relatively well tolerated at all doses, with no serious adverse effects. NSI-189 area under the curve increased in a dose-related and nearly proportional manner across the three cohorts, with a half-life of 17.