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