Drug intelligence / Profile preview

icariin

Development stage
Phase 3
Lead developer
DoubleRainbow Biosciences
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Icariin is a naturally occurring flavonoid glycoside isolated primarily from plants of the Epimedium genus, commonly known as Horny Goat Weed. It is a major bioactive constituent in traditional Chinese medicine, used for centuries as an aphrodisiac and for treating erectile dysfunction[1][5]. Icariin acts as a weak phosphodiesterase type 5 (PDE5) inhibitor, enhancing nitric oxide production and cGMP accumulation in smooth muscle cells, which underlies its effects on sexual function[5]. Beyond its use for sexual health, icariin exhibits multiple pharmacological activities including anti-atherosclerotic effects through anti-oxidative, anti-inflammatory, lipid-modulatory actions[3], and has shown potential anticancer properties by inducing apoptosis and inhibiting cell proliferation in various cancer models[6]. Icariin has also been investigated in clinical trials for bipolar disorder and substance abuse disorders. It is widely available over-the-counter globally as a dietary supplement marketed for sexual performance enhancement, athletic performance improvement, memory support, osteoporosis prevention, and other health benefits[2][4][5].

Other names
icarinepimedium extract (when referring to the standardized active component)horny goat weed extract (when referring to the standardized active component)
02

Targets

PDE5 (Phosphodiesterase 5A)UGT1A3 (UDP-glucuronosyltransferase family 1 member A3)

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