Drug intelligence / Profile preview

icotinib + arsenic trioxide

Development stage
Preclinical
Lead developer
Betta Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a **combination therapy** consisting of the small molecule **icotinib**, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and **arsenic trioxide**, a chemotherapeutic agent with multifactorial anti-cancer activities. The combination does not have a globally recognized brand or code name and is not approved as a fixed pharmaceutical product, but has been investigated in research and compassionate use settings, notably for **recurrent and/or metastatic head and neck squamous cell carcinoma**. In vitro studies indicate the combination increases reactive oxygen species (ROS), augments DNA damage, and impairs DNA repair mechanisms via reduction of BRCA1 and PLK1 activity, which may enhance tumor cell death. The primary therapeutic rationale is to leverage EGFR inhibition (icotinib) and the cytotoxic/DNA-damaging effects of arsenic trioxide, particularly in tumors with EGFR overexpression and TP53 mutations.

02

Targets

TRAC (T cell receptor alpha variable 17)GLI1PML-RARA (PML-retinoic acid receptor alpha fusion protein)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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