Emapunil (AC-5216) Clinical Trials

Size	Price	Qty
5mg	USD 147
25mg	USD 370

Clinical Trials

Multiple clinical trials have evaluated the synthetic translocator protein ligand emapunil (AC-5216/XBD173) across Phase 1 and Phase 2, with all studies now completed. Novartis Pharmaceuticals sponsored a Phase 2 trial assessing the drug's efficacy, safety, and tolerability in patients with anxiety disorders, including generalized anxiety disorder. Additionally, the National Institute of Mental Health conducted a Phase 1 study to evaluate baseline molecular imaging parameters and target receptor binding blockade using specific translocator protein radioligands.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02181582	COMPLETED	Baseline; Blocking Receptor Binding	National Institute of Mental Health (NIMH)	2014-06-24	PHASE1
NCT00108836	Completed	Anxiety Disorders	Novartis Pharmaceuticals\|Novartis	2005-03	Phase 2

(data from https://clinicaltrials.gov, updated on 2018-09-27)

Check the Emapunil (AC-5216) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Emapunil functions as a high-affinity ligand for the 18 kDa translocator protein, which promotes mitochondrial neurosteroid synthesis and enhances downstream GABA-A receptor-mediated inhibitory neurotransmission. This potentiation of central inhibitory signaling dampens neuronal hyperexcitability, providing the mechanistic basis for achieving target receptor binding blockade and therapeutic efficacy in anxiety disorders.

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>).