GLPG0187 Clinical Trials

Size	Price	Qty
5mg	USD 197
25mg	USD 497

Clinical Trials

Several completed Phase 1 clinical trials sponsored by Lakefront Biotherapeutics NV evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of GLPG0187. In healthy volunteers, studies assessed single and multiple dosing alongside the relative bioavailability of an isopropyl malonate prodrug formulation. Furthermore, an open-label dose-escalation trial examined intravenous GLPG0187 administration in patients with solid tumors.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01313598	COMPLETED	Solid Tumors	Lakefront Biotherapeutics NV	2011-03	PHASE1
NCT01580644	COMPLETED	Healthy	Lakefront Biotherapeutics NV	2012-01	PHASE1
NCT00928343	COMPLETED	Healthy	Lakefront Biotherapeutics NV	2009-06	PHASE1

(data from https://clinicaltrials.gov, updated on 2013-06-11)

Check the GLPG0187 product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

GLPG0187 acts as a broad-spectrum integrin receptor antagonist that inhibits αvβ1-integrin with a half-maximal inhibitory concentration (IC50) of 1.3 nM, thereby disrupting cell adhesion signaling and suppressing migrasome biogenesis. By blocking integrin-mediated extracellular matrix interactions and cellular motility, this therapeutic agent exerts potent antitumor activity, supporting its clinical investigation in patients with solid tumors.

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>).