GSK4418959 Clinical Trials

Size	Price	Qty
1mg	USD 497

Clinical Trials

A clinical trial sponsored by GlaxoSmithKline is evaluating GSK4418959, an oral Werner syndrome ATP-dependent helicase inhibitor, for the treatment of advanced solid tumors, including colorectal, colon, rectal, and endometrial cancers. This ongoing Phase 1/2 first-in-human study assesses dose escalation and expansion to determine the compound's safety, tolerability, and preliminary efficacy. Currently active, not recruiting, the trial involves ongoing patient monitoring across these specified indications.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06710847	ACTIVE_NOT_RECRUITING	Neoplasms, Colorectal; Solid Tumor; Colon Cancer; Rectal Cancer; Endometrial Cancer	GlaxoSmithKline	2024-12-13	PHASE1; PHASE2

(data from https://clinicaltrials.gov, updated on 2026-02-02)

Check the GSK4418959 product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

GSK4418959 functions as a selective, reversible, ATP-competitive inhibitor of Werner syndrome ATP-dependent helicase (WRN), binding the target enzyme to potently suppress both its ATPase activity and DNA unwinding function. This biochemical inhibition disrupts critical DNA repair pathways and genomic stability, inducing synthetic lethality and selective cell death in microsatellite instability-high (MSI-H) malignancies such as colorectal, colon, rectal, and endometrial cancers.

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>).