Clinical Trials

Several clinical trials have evaluated this compound in advanced solid tumors, RET-fusion non-small cell lung cancer, ovarian cancer, and malignancies harboring RET or BRAF alterations. Sponsored by academic and industrial entities, including Hoffmann-La Roche and Memorial Sloan Kettering Cancer Center, these Phase I investigations also included an expanded access protocol. Recruitment across these early-phase evaluations is currently completed or no longer available.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03784378 COMPLETED
Non Small Cell Lung Cancer; Ovarian Cancer; RET Gene Mutation; BRAF Gene Mutation
Memorial Sloan Kettering Cancer Center
 2018-12-14 PHASE1
NCT01877811 COMPLETED
Solid Tumors
Hoffmann-La Roche
 2013-06 PHASE1

(data from https://clinicaltrials.gov, updated on 2025-05-15)

Check the Agerafenib (CEP-32496) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Agerafenib selectively binds to and inhibits wild-type BRAF, mutant BRAF V600E, and c-Raf kinases, while additionally targeting related tyrosine kinases including RET, VEGFR2, and PDGFRβ. By suppressing downstream mitogen-activated protein kinase signaling and oncogenic pathways, the compound halts cellular proliferation and drives apoptosis, providing the mechanistic rationale for its clinical evaluation in solid tumors, non-small cell lung cancer, and RET- or BRAF-altered 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>).

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Note: Technical data last updated: Sep 1, 2026.