Drug intelligence / Profile preview

Epimedium Prenylflavonoids Extract

Development stage
Unknown
Lead developer
National University Hospital
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Epimedium Prenylflavonoids Extract is a standardized botanical extract derived from the *Epimedium* plant (Berberidaceae), developed by researchers at the National University Hospital, Singapore. It is being investigated as a pharmaceutical-quality intervention for postmenopausal osteoporosis and cardiovascular disease. The extract contains a complex of prenylflavonoid compounds, including icariin, icariside I, icariside II, icaritin, and desmethylicaritin. It functions as a selective estrogen receptor modulator (SERM), influencing bone remodeling by targeting estrogen receptors and markers such as bone-specific alkaline phosphatase (BSAP) and the osteoclast adaptor protein TRAF6. Additionally, the extract has demonstrated cardiovascular benefits through nitric oxide-dependent vasorelaxation and improvements in endothelial function. Clinical development has included Phase 1 trials in healthy men to establish safety and pharmacokinetics, as well as studies in postmenopausal women to evaluate bone health markers.

Other names
Standardized Epimedium Prenylflavonoids Extract
02

Targets

TRAF6ALPL (Tissue-nonspecific alkaline phosphatase)ESR1 (ERα)

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