Drug intelligence / Profile preview

hypericum perforatum

Development stage
Phase 4
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

Hypericum perforatum is a medicinal plant commonly known as St. John’s wort. It has been used for centuries to treat various conditions, most notably mild to moderate depression[1][2][4]. The primary active constituents are hypericin and hyperforin (phloroglucinols), along with flavonoids such as quercetin and rutin[4]. Its mechanism of action is multifactorial and includes inhibition of the reuptake of serotonin, dopamine, and norepinephrine; inhibition of monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT); modulation of GABA-A and GABA-B receptors; activation of pregnane-X-receptor; and possible antioxidant effects[6][8]. Standardization is typically based on the content of hypericin or hyperforin[4]. While widely available as an over-the-counter supplement for mood disorders in many countries, it interacts with numerous medications due to its induction of cytochrome P450 enzymes.

Brand names
St. John's WortPerforate St John's-wortTipton's weedKlamath weed
Other names
Saint John's wortSJWHyperici herba
02

Targets

PXR (Pregnane X receptor)MAOA (Monoamine oxidase A)MAOB (Monoamine oxidase B)NET (Norepinephrine Transporter)DAT (Dopamine plasma membrane transport protein)SERT (Sodium-dependent serotonin transporter)

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