Drug intelligence / Profile preview

erlotinib + romidepsin

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Romidepsin plus erlotinib is a combination drug regimen studied primarily for advanced non-small cell lung cancer (NSCLC). Romidepsin is a histone deacetylase (HDAC) inhibitor that acts by inhibiting class 1 and 2 HDAC enzymes, leading to increased histone acetylation, restoration of normal gene expression, cell cycle arrest, and apoptosis in cancer cells. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR signaling pathways involved in tumor growth. The combination has shown synergistic anti-tumor effects including enhanced apoptosis and inhibition of EGFR phosphorylation. It has been investigated in clinical trials for NSCLC patients who are resistant or insensitive to erlotinib monotherapy, demonstrating disease control with manageable toxicity profiles. This combination targets both epigenetic modulation via HDAC inhibition and targeted therapy via EGFR blockade.[1][2][3][6]

02

Targets

EGFR (Epidermal growth factor receptor)HDAC1 (Histone Deacetylase 1)

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