Clinical Trials

Multiple clinical trials involve tolbutamide as a sensitive probe substrate to evaluate pharmacokinetic drug-drug interaction potentials and CYP2C9 enzyme activity in phase 1 settings. These completed studies, sponsored by organizations such as Vicore Pharma AB, Pfizer, Daiichi Sankyo, and BioCryst Pharmaceuticals, evaluated conditions including hereditary angioedema, drug interactions, and healthy volunteer profiles. Together, these protocols reflect the standardized application of tolbutamide in clinical pharmacology research.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05830799 Completed
Drug Interaction
Vicore Pharma AB
 2023-03-29 Phase 1
NCT05097716 Completed
Healthy Volunteers
Pfizer
 2021-11-02 Phase 1
NCT03291288 Completed
Drug Interaction Potential
Daiichi Sankyo
 2018-02-26 Phase 1
NCT02819102 Completed
Hereditary Angioedema
BioCryst Pharmaceuticals
 2016-03 Phase 1

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

Check the Tolbutamide (HLS 831) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Tolbutamide selectively binds to and inhibits pancreatic ATP-sensitive potassium channels, thereby blocking potassium efflux and inducing membrane depolarization in beta cells. This depolarization triggers calcium-dependent insulin exocytosis to stimulate tissue glucose uptake, supporting its clinical application in phase 1 drug interaction studies assessing metabolic clearance and pharmacokinetic parameters across healthy volunteers and patient cohorts.

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.