Ziritaxestat (GLPG1690) Clinical Trials

Size	Price	Qty
5mg	USD 147
25mg	USD 370

Clinical Trials

Multiple clinical trials sponsored primarily by Galapagos NV and Lakefront Biotherapeutics NV have evaluated the small-molecule autotaxin inhibitor ziritaxestat across healthy subjects, idiopathic pulmonary fibrosis, and systemic sclerosis. Spanning Phase 1 through Phase 3, completed early-phase studies in healthy volunteers focused on safety, tolerability, bioavailability, and drug-drug interactions. Subsequent Phase 2 trials explored therapeutic efficacy in idiopathic pulmonary fibrosis, though pivotal Phase 3 evaluations were ultimately terminated.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03976648	TERMINATED	Systemic Sclerosis	Lakefront Biotherapeutics NV	2019-07-18	PHASE2
NCT03711162	TERMINATED	Idiopathic Pulmonary Fibrosis	Lakefront Biotherapeutics NV	2018-11-28	PHASE3
NCT03733444	TERMINATED	Idiopathic Pulmonary Fibrosis	Lakefront Biotherapeutics NV	2018-11-05	PHASE3
NCT03798366	COMPLETED	Systemic Sclerosis	Lakefront Biotherapeutics NV	2019-01-14	PHASE2
NCT03787186	COMPLETED	Healthy	Lakefront Biotherapeutics NV	2018-11-09	PHASE1
NCT03515382	COMPLETED	Healthy	Lakefront Biotherapeutics NV	2018-03-16	PHASE1
NCT03515382	Completed	Healthy	Galapagos NV	2018-03-16	Phase 1
NCT03143712	COMPLETED	Healthy	Lakefront Biotherapeutics NV	2017-04-18	PHASE1
NCT02738801	COMPLETED	Idiopathic Pulmonary Fibrosis	Lakefront Biotherapeutics NV	2016-03	PHASE2
NCT03143712	Completed	Healthy	Galapagos NV	2017-04-18	Phase 1
NCT02738801	Completed	Idiopathic Pulmonary Fibrosis	Galapagos NV	2016-03	Phase 2
NCT02179502	COMPLETED	Healthy	Lakefront Biotherapeutics NV	2014-06	PHASE1

(data from https://clinicaltrials.gov, updated on 2022-03-29)

Check the Ziritaxestat (GLPG1690) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Ziritaxestat selectively binds to and inhibits autotaxin with an IC50 of 131 nM and Ki of 15 nM, blocking the enzymatic conversion of lysophosphatidylcholine into lysophosphatidic acid. This reduction in lysophosphatidic acid levels suppresses pro-fibrotic cellular signaling, fibroblast activation, and extracellular matrix deposition, thereby attenuating pathological tissue remodeling in fibrotic conditions such as idiopathic pulmonary fibrosis and systemic sclerosis.

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>).