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erlotinib + nicotinamide
- Development stage
- Unknown
- Lead developer
- Astellas Pharma
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Erlotinib + nicotinamide is a combination therapy investigated for the treatment of advanced or metastatic non-small cell lung cancer (NSCLC) harboring EGFR mutations. Erlotinib is a small molecule tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR), specifically effective against mutations in exons 19 and 21. Nicotinamide, a form of vitamin B3, acts as a sirtuin inhibitor (HDAC III) and is added to the regimen to re-activate the epigenetically silenced tumor suppressor gene RUNX3. The rationale for this combination is that RUNX3 inactivation by promoter hypermethylation occurs in a significant portion of lung adenocarcinomas and correlates with poor clinical outcomes; re-activating this gene may enhance the efficacy of EGFR-targeted therapies. Clinical evaluation of this combination has been conducted in randomized trials, such as NCT02416739, to assess improvements in progression-free survival (PFS) and overall survival (OS).
- Other names
- nicotinamide + erlotinibnicotinamide and erlotinib
02
Targets
EGFR T790M (Epidermal growth factor receptor T790M mutant)
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