Drug intelligence / Profile preview

erlotinib + vorinostat

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Erlotinib + vorinostat is a combination of two small molecule drugs used primarily in investigational settings for the treatment of advanced cancers, particularly non-small cell lung cancer (NSCLC) with EGFR mutations. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR signaling, thereby inhibiting tumor cell proliferation and survival. Vorinostat (also known as suberoylanilide hydroxamic acid or SAHA) is a histone deacetylase (HDAC) inhibitor that induces accumulation of acetylated proteins, leading to altered gene expression and increased apoptosis in cancer cells. The rationale for combining these agents is to overcome resistance to EGFR inhibitors by modulating epigenetic mechanisms and enhancing apoptotic pathways. Clinical studies have shown that this combination can be safely administered but has limited efficacy in patients with NSCLC who have progressed on prior EGFR TKI therapy[1][2][7].

Brand names
ZolinzaTarceva
Other names
erlotinib plus vorinostatERL plus SAHA
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)HDAC (HDAC family)

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