E7130 Usage And Synthesis

Description

E7130, also known as C52-halichondrin-B amine, is a novel microtubule inhibitor and a promising tumor microenvironment ameliorator. It is a novel microtubule dynamics inhibitor and can also increase intratumoural CD31-positive endothelial cells and reduce alpha-SMA-positive cancer-associated fibroblasts at pharmacologically relevant compound concentrations.

Biological Activity

E7130 is believed to improve tumor microenvironment by unique action for potential effect on immune activation by releasing hypoxia and suppressing interaction between cancer cells and stroma.

Clinical Use

E7130 is a microtubule inhibitor and a promising ameliorator of the tumor microenvironment. It has demonstrated significant antitumor activity and tumor microenvironment (TME) -related biomarker changes in preclinical models and is currently in phase I clinical trial[1]. It is under development for the treatment of solid tumors including HER2 negative breast cancer, oropharyngeal cancer, gastric cancer, head and neck cancer squamous cell carcinoma, laryngeal cancer, hypopharyngeal cancer, gastro-esophageal cancer rectal cancer and colon cancer. The drug candidate is administered through intravenous route. The drug candidate is a halichondrin analogue.

References

[1] Ryu S, et al. Development of an analytical method to determine E7130 concentration in mouse plasma by micro-sampling using ultra-performance liquid chromatography–high resolution mass spectrometry. Journal of Chromatography B, 2022; 1207: 123366.