Drug intelligence / Profile preview

belinostat + erlotinib

Development stage
Preclinical
Lead developer
Valerio Therapeutics
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Belinostat + erlotinib is a combination of two small molecule anticancer agents with distinct mechanisms of action. Belinostat is a histone deacetylase (HDAC) inhibitor that induces cell cycle arrest, apoptosis, and inhibition of angiogenesis by preventing the removal of acetyl groups from lysine residues on histones and non-histone proteins, leading to increased expression of tumor suppressor genes[1][4][6]. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that blocks EGFR signaling pathways involved in cancer cell proliferation and survival[2][3][5]. Both drugs are approved individually for various cancers; belinostat for relapsed or refractory peripheral T-cell lymphoma, and erlotinib for metastatic non-small cell lung cancer with specific EGFR mutations as well as advanced pancreatic cancer. The combination may be explored in research settings to target multiple oncogenic pathways.

02

Targets

ABCG2 (Breast cancer resistance protein)HDAC (HDAC family)UGT1A1 (UDP-glucuronosyltransferase 1A1)EGFR (Epidermal growth factor receptor)

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