Clinical Trials

Numerous clinical trials sponsored by Takeda evaluated the safety, pharmacokinetics, and therapeutic potential of fasiglifam (TAK-875) across Phase I, Phase II, and Phase III studies targeting type 2 diabetes mellitus, impaired glycemic control, chronic kidney disease, and cardiovascular disease. Although early-phase pharmacokinetic evaluations successfully reached completed status, several advanced Phase II and Phase III trials were ultimately terminated or withdrawn during development.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02015780 WITHDRAWN
Type 2 Diabetes Mellitus; Chronic Kidney Disease
Takeda
 2013-12 PHASE3
NCT01609582 TERMINATED
Type 2 Diabetes; Cardiovascular Disease
Takeda
 2012-06 PHASE3
NCT01834274 TERMINATED
Diabetes Mellitus, Type 2
Takeda
 2013-06 PHASE3
NCT01549964 TERMINATED
Glycemic Control
Takeda
 2012-04 PHASE3
NCT01481116 TERMINATED
Diabetes Mellitus, Type 2
Takeda
 2012-01 PHASE3
NCT01829464 TERMINATED
Diabetes
Takeda
 2013-05 PHASE3
NCT01829477 TERMINATED
Diabetes Mellitus, Type 2
Takeda
 2013-04 PHASE3
NCT01647542 TERMINATED
Type 2 Diabetes Mellitus
Takeda
 2012-10 PHASE3
NCT01982253 TERMINATED
Type 2 Diabetes Mellitus
Takeda
 2013-10 PHASE2
NCT01433406 COMPLETED
Diabetes Mellitus
Takeda
 2011-10 PHASE3
NCT01456195 COMPLETED
Diabetes Mellitus, Type 2
Takeda
 2011-11 PHASE3
NCT01433419 COMPLETED
Diabetes Mellitus
Takeda
 2012-01 PHASE3
NCT01585792 COMPLETED
Diabetic Patients
Takeda
 2012-05 PHASE3
NCT01433393 COMPLETED
Diabetes Mellitus
Takeda
 PHASE3
NCT01414920 COMPLETED
Diabetes Mellitus, Type 2
Takeda
 2011-08 PHASE2
NCT01496443 COMPLETED
Pharmacokinetics
Takeda
 2012-01 PHASE1
NCT01496443 Completed
Pharmacokinetics
Takeda
 2012-01 Phase 1
NCT01007097 COMPLETED
Diabetes Mellitus, Type 2
Takeda
 2009-12 PHASE2
NCT00949091 COMPLETED
Diabetes Mellitus, Type 2
Takeda
 2009-01 PHASE1
NCT00949091 Completed
Diabetes Mellitus Type 2
Takeda
 2009-01 Phase 1

(data from https://clinicaltrials.gov, updated on 2014-01-27)

Check the Fasiglifam(TAK-875) Hemihydrate product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Fasiglifam selectively binds to and activates G-protein-coupled receptor 40 (GPR40), triggering intracellular inositol monophosphate accumulation and calcium elevation within pancreatic beta cells. This receptor activation enhances glucose-dependent insulin secretion, promoting systemic glycemic control in clinical settings evaluated for type 2 diabetes mellitus.

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.