Drug intelligence / Profile preview

yuanhuadine

Development stage
Preclinical
Lead developer
Seoul National University
Modality
Small Molecules
Administration
Oral, Intratumoral
01

Overview

Yuanhuadine is a natural daphnane-type diterpene orthoester isolated from the flower buds of *Daphne genkwa*. It has demonstrated potent anti-proliferative and anti-tumor activities, particularly in non-small cell lung cancer (NSCLC). The compound's mechanism of action involves the up-regulation of SerpinB2 (plasminogen activator inhibitor-2), which leads to the suppression of invadopodia-like structure protrusions and reduced invasiveness in cancer cells. Yuanhuadine has shown potential in overcoming acquired resistance to EGFR tyrosine kinase inhibitors (TKIs) like gefitinib by modulating the urokinase plasminogen activator (uPA) system and elevating SerpinB2 levels, which are typically down-regulated in resistant cell lines.

02

Targets

AXL (AXL receptor tyrosine kinase)mTOR (Mammalian target of rapamycin kinase)EGFR (Epidermal growth factor receptor)AKT (RAC-alpha serine/threonine-protein kinase)MET (Mesenchymal-epithelial transition factor receptor)NNMT (Nicotinamide N-methyltransferase)PAI-2 (Plasminogen activator inhibitor-2)

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