| Hazard Information | Back Directory | [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. |
|
|