Omipalisib (GSK2126458) Clinical Trials

Size	Price	Qty
2mg	USD 170
5mg	USD 270

Clinical Trials

Sponsored by GlaxoSmithKline, several Phase 1 clinical trials evaluated the safety, tolerability, pharmacokinetics, and dose escalation of omipalisib (GSK2126458). Comprising completed and terminated studies, these investigations established the compound's pharmacodynamics and therapeutic potential. The research encompassed patients across both malignant and non-malignant conditions, specifically solid tumors, advanced malignancies, and idiopathic pulmonary fibrosis.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01725139	COMPLETED	Idiopathic Pulmonary Fibrosis	GlaxoSmithKline	2013-03-08	PHASE1
NCT01248858	TERMINATED	Cancer	GlaxoSmithKline	2010-12-03	PHASE1
NCT01725139	Completed	Idiopathic Pulmonary Fibrosis	GlaxoSmithKline	2013-03-08	Phase 1
NCT00972686	COMPLETED	Solid Tumours	GlaxoSmithKline	2009-08-31	PHASE1
NCT01248858	Terminated	Cancer	GlaxoSmithKline	2010-12-03	Phase 1
NCT00972686	Completed	Solid Tumours	GlaxoSmithKline	2009-08-31	Phase 1

(data from https://clinicaltrials.gov, updated on 2019-11-21)

Check the Omipalisib (GSK2126458) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Omipalisib (GSK2126458) is a potent dual inhibitor that selectively binds to Class I PI3K isoforms (p110α/β/δ/γ) and mTORC1/2 complexes, thereby suppressing downstream phosphorylation of AKT and p70S6K to induce G1-phase cell cycle arrest and autophagy. By blocking key pro-survival signaling cascades, this target inhibition suppresses cell growth and proliferation, providing the mechanistic basis for its clinical evaluation in solid tumors and idiopathic pulmonary fibrosis.

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>).