Clinical Trials

Several completed Phase I clinical trials sponsored by GlaxoSmithKline, with Theravance Biopharma as a co-sponsor, evaluated the therapeutic application of batefenterol for chronic obstructive pulmonary disease. These studies investigated the safety, tolerability, pharmacodynamics, and pharmacokinetics of dose-escalated batefenterol in healthy participants, alongside its pharmacokinetic profile alone and when co-administered with fluticasone furoate in an open-label, crossover setting.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02064504 Completed
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 2014-02-19 Phase 1
NCT00550225 Completed
Pulmonary Disease Chronic Obstructive
Theravance Biopharma|GlaxoSmithKline
 2007-11-29 Phase 1

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Compliance for Clinical Use

Mechanism and Biochemical Profile

Batefenterol functions as a dual-acting compound that potently antagonizes human M2 and M3 muscarinic acetylcholine receptors while selectively agonizing human β2-adrenoceptors, thereby suppressing Gq-protein-mediated signaling and stimulating intracellular cyclic adenosine monophosphate accumulation in smooth muscle cells. This dual pharmacodynamics simultaneously prevents cholinergic-mediated bronchoconstriction and induces airway relaxation, providing sustained bronchodilation to relieve airway obstruction in chronic obstructive pulmonary disease.

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>).

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Note: Technical data last updated: Sep 1, 2026.