Drug intelligence / Profile preview

Triphendiol

Development stage
Preclinical
Lead developer
MEI Pharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Triphendiol is an investigational small molecule anticancer agent developed as an orally delivered chemosensitizing drug. It is primarily being studied for use in conjunction with standard chemotherapeutic agents for the treatment of late-stage pancreatic cancer, cholangiocarcinoma (bile duct cancer), and melanoma. Triphendiol exhibits broad cytostatic and cytotoxic activity against various human cancer cell lines in vitro, causing cell cycle arrest at the G2/M phase and inducing apoptosis through activation of the intrinsic (mitochondrial) apoptotic pathway. Its mechanism involves downregulation of X-linked inhibitor of apoptosis protein (XIAP), activation of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) death receptors, caspase 9-mediated apoptosis, inhibition of topoisomerase II, disruption of ATP production via degradation of the electron transport chain, and activation of autophagy through AMP-activated protein kinase (AMPK)-mTOR signaling. Triphendiol has shown high selectivity for tumor cells with minimal effects on non-tumor cells and no observable toxicity in animal studies at therapeutic doses[6][8].

02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)TNFRSF10D (TRAIL receptor 4)CASP9 (Caspase-9)TOP2A (DNA topoisomerase II)XIAP

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