GTS-21 dihydrochloride Clinical Trials

Size	Price	Qty
5mg	USD 197
25mg	USD 497

Clinical Trials

Multiple clinical trials evaluate GTS-21 dihydrochloride across neurological, cognitive, and inflammatory conditions, including Alzheimer disease, attention deficit hyperactivity disorder, endotoxemia, sepsis, vagal activity, and tobacco use disorder. Led by industry and academic sponsors such as CoMentis, Radboud University Medical Center, and the University of Florida, these Phase 1 and Phase 2 investigations primarily comprise completed proof-of-concept crossover and dose-tolerability studies. However, a Phase 2 trial examining smoking behavior was withdrawn.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02432066	WITHDRAWN	Tobacco Use Disorder	University of Florida	2018-09-29	PHASE2
NCT00783068	COMPLETED	Endotoxemia; Sepsis; Vagal Activity	Radboud University Medical Center	2008-08
NCT00419445	COMPLETED	Attention Deficit Hyperactivity Disorder	CoMentis	2007-02	PHASE1; PHASE2
NCT00414622	COMPLETED	Alzheimer Disease	CoMentis	2006-11	PHASE2

(data from https://clinicaltrials.gov, updated on 2019-03-25)

Check the GTS-21 dihydrochloride product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

GTS-21 dihydrochloride selectively binds and activates the alpha7 nicotinic acetylcholine receptor while additionally antagonizing α4β2 nicotinic receptors and 5-HT3A receptors, thereby modulating intracellular cholinergic signaling pathways and suppressing pro-inflammatory cytokine release. This dual neuroprotective and anti-inflammatory activity underpins its cognitive-enhancing and immune-regulating effects, providing a mechanistic rationale for its clinical evaluation in neurodegenerative conditions such as Alzheimer disease as well as systemic inflammatory states like endotoxemia and sepsis.

Appendix RUO and cGMP Quality Standards

Quality Dimension	RUO (Research Use Only)	cGMP (Current Good Manufacturing Practice)
Clinical Applicability	Prohibited in human clinical trials or medical diagnostics.	Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status	Non-regulated grade; exempt from drug manufacturing laws.	Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment	Unclassified analytical or research laboratories.	Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control	Basic purity and activity testing.	Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation	Basic equipment calibration; no process validation required.	Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance	Vendor self-declared without required formal QMS.	Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact	High risk of IND rejection if used as a critical raw material.	Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).