Drug intelligence / Profile preview

Icaritin

Development stage
Phase 4
Lead developer
Shenogen Pharma
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Icaritin is a small molecule, monoprenylated flavonol derived from the Epimedium genus, traditionally used in East Asian medicine. It acts primarily as an estrogen receptor alpha modulator and has demonstrated antitumor activity across various cancers, including hepatocellular carcinoma (HCC), breast cancer, and other solid tumors. Icaritin exerts its effects by inhibiting cell proliferation, inducing apoptosis and differentiation, suppressing migration and invasion (notably through inhibition of the Akt/mTOR signaling pathway), regulating microRNAs, targeting stem cells, reversing multidrug resistance, and modulating several signaling pathways such as PTEN/Akt, Akt/mTOR, NF-κB, MAPK/ERK. It also exhibits osteoblastic and neuroprotective activities. Icaritin is approved in China for liver cancer (HCC) treatment and is under investigation for other malignancies[1][2][3][4][5].

Brand names
Acolytin
Other names
Akelading阿可拉定Icaritine
02

Targets

ESR1 (ERα)

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