Delving into the Latest Updates on Nelonicline with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CHRNA7

Mechanism

α7 receptor agonists(Neuronal acetylcholine receptor protein alpha-7 subunit agonists)

Therapeutic Areas

Nervous System DiseasesCongenital DisordersEndocrinology and Metabolic Disease+ [2]

Active Indication-

Inactive Indication

Alzheimer DiseaseChanarin-Dorfman SyndromeCognitive Dysfunction+ [1]

Originator Organization

AbbVie, Inc.

Active Organization-

Inactive Organization

AbbVie, Inc.

Abbott Laboratories

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

Login to view timeline

Structure

Molecular FormulaC17H19N3OS

InChIKeyQZDCYUCETTWCMO-FOOLLQQTSA-N

CAS Registry1026134-63-3

Schizophrenia is a chronic neuropsychiatric disorder that affects nearly 1% of the global population. There are various anti-psychotic drugs available for the treatment of schizophrenia, but they have certain side effects; therefore, there is a need to explore and develop novel potential lead compounds against schizophrenia. The currently available drugs e.g. typical and atypical antipsychotics act on different dopamine and serotonin receptors and as per literature reports, various piperidine and piperazine derivatives have shown promising activity against these receptors. When different heterocyclic groups are attached to basic piperidine and piperazine rings, the antipsychotic activity is greatly potentiated. In this direction, various antipsychotic drugs have been synthesized at the laboratory level, and few are under clinical trial studies, such as Lu AE58054, PF-04802540, ORG25935, DMXB-A, Bitopertin, and ABT-126. In the present review, we include the studies related to the effect of different substituents on piperidine/piperazine derivatives and their anti-psychotic activity. Various series of synthesized compounds by other researchers with piperidine/piperazine nucleus have been reviewed and diagrammatically represented in the form of SAR (structure-activity relationships), which will help the scientists for the development of potential lead compounds.

01 Sep 2018·Drug Metabolism and Disposition

Correction to “Metabolism and Disposition of a Novel Selective α7 Neuronal Acetylcholine Receptor Agonist ABT-126 in Humans: Characterization of the Major Roles for Flavin-Containing Monooxygenases and UDP-Glucuronosyl Transferase 1A4 and 2B10 in Catalysis”

Article

Author: Stresser, Liu H. ; Michmerhuizen, M. J.

27 Jun 2018·The Journal of Clinical PsychiatryQ2 · MEDICINE

Efficacy and Safety of the α7-Nicotinic Acetylcholine Receptor Agonist ABT-126 in the Treatment of Cognitive Impairment Associated With Schizophrenia

Q2 · MEDICINE

Article

Author: Wang, Deli ; Othman, Ahmed A ; Zhao, Jun ; Haig, George M ; Bain, Earle E

OBJECTIVETo evaluate the efficacy and safety of the α₇-nicotinic receptor agonist ABT-126 for treatment of cognitive impairment in stable subjects with schizophrenia who smoke.METHODSA 12-week double-blind, placebo-controlled, parallel-group study was conducted from August 2012 to March 2014. Subjects with a diagnosis of schizophrenia based on DSM-IV-TR criteria (confirmed by the Mini-International Neuropsychiatric Interview version 6.0.0) were randomized 1:1:1 to ABT-126 25 mg, ABT-126 75 mg, or placebo once daily while maintained on their background antipsychotic medication. The primary endpoint was the change from baseline on the Measurement and Treatment Research to Improve Cognition in Schizophrenia (MATRICS) Consensus Cognitive Battery (MCCB) neurocognitive composite score; the primary analysis compared ABT-126 with placebo at week 12 using a mixed-effects model for repeated measures. Secondary endpoints included the change from baseline on the University of California San Diego Performance-based Skills Assessment-2 Extended-Range, the 16-item Negative Symptom Assessment scale (NSA-16), and safety assessments.RESULTSOf the 157 randomized subjects, 82% completed the study. The mean baseline MCCB neurocognitive composite score for the entire study sample was 28.8; scores were similar across groups. No statistical difference in the change from baseline score between any of the ABT-126 dose groups and placebo was observed on the MCCB neurocognitive composite score (ABT-126 25 mg, +0.28; ABT-126 75 mg, +0.41; placebo, +1.42). Differences in the NSA-16 total score were seen with ABT-126 75 mg versus placebo at week 6 (-2.79; P = .011) and week 12 (-1.94; P = .053). Adverse events with ABT-126 were similar to placebo, except for constipation (5.8% for ABT-126 vs 0% for placebo).CONCLUSIONSABT-126 did not demonstrate a procognitive effect in subjects with stable schizophrenia who smoke. A trend for improvement in negative symptoms was observed with the high dose. The safety profile of ABT-126 was similar to placebo.TRIAL REGISTRATIONClinicalTrials.gov identifier: NCT01678755.

100 Deals associated with Nelonicline

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 2	GB	AbbVie, Inc.	01 Oct 2009
Alzheimer Disease	Phase 2	SK	AbbVie, Inc.	01 Oct 2009
Alzheimer Disease	Phase 2	US	AbbVie, Inc.	01 Oct 2009
Alzheimer Disease	Phase 2	ZA	AbbVie, Inc.	01 Oct 2009
Alzheimer Disease	Phase 2	CZ	AbbVie, Inc.	01 Oct 2009
Alzheimer Disease	Phase 2	GB	AbbVie, Inc.	01 Oct 2009
Alzheimer Disease	Phase 2	US	AbbVie, Inc.	01 Oct 2009
Alzheimer Disease	Phase 2	ZA	AbbVie, Inc.	01 Oct 2009
Alzheimer Disease	Phase 2	CZ	AbbVie, Inc.	01 Oct 2009
Alzheimer Disease	Phase 2	SK	AbbVie, Inc.	01 Oct 2009

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01655680 (Pubmed \| Neuropsychopharmacology) Manual	Phase 2	Cognitive Dysfunction \| Schizophrenia	432	ABT-126	(oslymzxvzs) = ncxpqrujhq aredpebjwu (gnhhqrxxzl, 0.54) View more	Negative	01 Nov 2016
				Placebo	(oslymzxvzs) = asfzisucrh aredpebjwu (gnhhqrxxzl, 0.56) View more