LGK974 (WNT974) Clinical Trials

Size	Price	Qty
5mg	USD 247
50mg	USD 970

Clinical Trials

Multiple Phase I clinical trials sponsored by Novartis Pharmaceuticals evaluate the safety, tolerability, and preliminary efficacy of oral LGK974 (WNT974) in patients with Wnt ligand-dependent malignancies. Evaluated indications include pancreatic cancer, BRAF-mutant colorectal cancer, melanoma, triple-negative breast cancer, and squamous cell carcinomas of head and neck, cervical, esophageal, and lung origins. Documented recruitment statuses across these studies include active, not recruiting, and completed.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01351103	COMPLETED	Pancreatic Cancer; BRAF Mutant Colorectal Cancer; Melanoma; Triple Negative Breast Cancer; Head and Neck Squamous Cell Cancer; Cervical Squamous Cell Cancer; Esophageal Squamous Cell Cancer; Lung Squamous Cell Cancer	Novartis Pharmaceuticals	2011-12-01	PHASE1
NCT01351103	Active not recruiting	Pancreatic Cancer\|BRAF Mutant Colorectal Cancer\|Melanoma\|Triple Negative Breast Cancer\|Head and Neck Squamous Cell Cancer\|Cervical Squamous Cell Cancer\|Esophageal Squamous Cell Cancer\|Lung Squamous Cell Cancer	Novartis Pharmaceuticals\|Novartis	2011-12-01	Phase 1

(data from https://clinicaltrials.gov, updated on 2025-06-13)

Check the LGK974 (WNT974) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

LGK974 potently and specifically binds to Porcupine (PORCN), an acyltransferase required for Wnt ligand palmitoylation, thereby blocking Wnt secretion and downstream signal transduction to suppress oncogenic cell proliferation. By inhibiting PORCN-dependent signaling, LGK974 impairs tumor cell growth and survival, demonstrating therapeutic relevance in Wnt-driven malignancies such as pancreatic cancer, BRAF-mutant colorectal cancer, and head and neck squamous cell carcinoma.

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>).