Clinical Trials

Setanaxib (GKT137831) has been evaluated in multiple Phase 1 and Phase 2 clinical trials for conditions including primary biliary cholangitis, idiopathic pulmonary fibrosis, Alport syndrome, type 2 diabetes mellitus with diabetic nephropathy, and head and neck squamous cell carcinoma. Sponsored by commercial entities such as Calliditas Therapeutics and academic institutions including the University of Alabama at Birmingham, all identified studies have completed recruitment. These trials provide critical safety, pharmacokinetic, and clinical efficacy data across various fibrotic, inflammatory, metabolic, and oncologic indications.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06274489 COMPLETED
Alport Syndrome
Calliditas Therapeutics AB
 2023-11-27 PHASE1; PHASE2
NCT03865927 COMPLETED
Idiopathic Pulmonary Fibrosis
University of Alabama at Birmingham
 2020-09-07 PHASE2
NCT05014672 COMPLETED
Primary Biliary Cholangitis; Liver Stiffness
Calliditas Therapeutics Suisse SA
 2022-02-14 PHASE2
NCT05323656 COMPLETED
Squamous Cell Carcinoma of Head and Neck
Calliditas Therapeutics Suisse SA
 2022-04-06 PHASE2
NCT04327089 COMPLETED
Phase 1
Calliditas Therapeutics AB
 2020-06-24 PHASE1
NCT03226067 COMPLETED
Primary Biliary Cirrhosis
Calliditas Therapeutics AB
 2017-06-26 PHASE2
NCT03740217 COMPLETED
Phase 1
Calliditas Therapeutics AB
 2018-12-19 PHASE1
NCT02010242 COMPLETED
Type 2 Diabetes Mellitus With Diabetic Nephropathy
Calliditas Therapeutics AB
 2013-10 PHASE2

(data from https://clinicaltrials.gov, updated on 2026-04-13)

Check the Setanaxib (GKT137831) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Setanaxib functions as a potent dual inhibitor of NADPH oxidases NOX1 and NOX4, binding directly to these enzymatic targets to suppress the downstream biochemical production of reactive oxygen species (ROS). By attenuating oxidative stress and suppressing ROS-mediated pro-fibrotic signaling, this target inhibition prevents pathological extracellular matrix accumulation and cell damage, offering clinical utility in modulating tissue fibrosis in conditions such as primary biliary cholangitis, idiopathic pulmonary fibrosis, and diabetic nephropathy.

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.