Naporafenib (LXH254) Clinical Trials

Size	Price	Qty
2mg	USD 157
5mg	USD 247

Clinical Trials

Multiple clinical trials, sponsored predominantly by Novartis Pharmaceuticals and Erasca, Inc., are evaluating naporafenib (LXH254) across Phase 1 through Phase 3 studies. These investigations focus on advanced solid tumors, non-small cell lung cancer, ovarian cancer, BRAF V600 colorectal cancer, and metastatic NRAS-mutant cutaneous melanoma, ranging from early-phase dose-finding combinations to late-stage Phase 3 trials. Across these evaluations, recruitment statuses include active, not recruiting, and terminated.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06346067	ACTIVE_NOT_RECRUITING	Advanced or Metastatic NRAS-mutant Melanoma	Erasca, Inc.	2024-04-29	PHASE3
NCT04417621	ACTIVE_NOT_RECRUITING	Melanoma	Novartis Pharmaceuticals	2020-10-30	PHASE2
NCT03333343	ACTIVE_NOT_RECRUITING	EGFR-mutant Non-small Cell Lung Cancer	Novartis Pharmaceuticals	2018-01-29	PHASE1
NCT05907304	ACTIVE_NOT_RECRUITING	Advanced or Metastatic Solid Tumors	Erasca, Inc.	2023-08-17	PHASE1
NCT04294160	TERMINATED	BRAF V600 Colorectal Cancer	Novartis Pharmaceuticals	2020-07-22	PHASE1
NCT02974725	TERMINATED	Non-Small Cell Lung Cancer; Melanoma	Novartis Pharmaceuticals	2017-02-24	PHASE1
NCT02607813	TERMINATED	NSCLC; Ovarian Cancer; Melanoma; Other Solid Tumors	Novartis Pharmaceuticals	2016-01-18	PHASE1
NCT04417621	Active not recruiting	Melanoma	Novartis Pharmaceuticals\|Novartis	2020-10-30	Phase 2
NCT02974725	Active not recruiting	Non-Small Cell Lung Cancer\|Melanoma	Novartis Pharmaceuticals\|Novartis	2017-02-24	Phase 1
NCT02607813	Terminated	NSCLC\|Ovarian Cancer\|Melanoma\|Other Solid Tumors	Novartis Pharmaceuticals\|Novartis	2016-01-18	Phase 1

(data from https://clinicaltrials.gov, updated on 2026-02-27)

Check the Naporafenib (LXH254) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Naporafenib acts as a type II ATP-competitive inhibitor that potently binds B-RAF and C-RAF kinases at picomolar concentrations, blocking RAF dimerization and downstream MAPK signaling cascade activation within cancer cells. By suppressing intracellular MAPK pathway signaling and downstream cellular proliferation, this therapeutic action inhibits tumor growth in patients with MAPK-altered solid tumors, non-small cell lung cancer, and NRAS- or BRAF-mutant melanoma.

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>).