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Hyperforin

SJW constituent

What it isSt John’s wort constituent and a potent PXR agonist.

Why this oneIt is the reason St John’s wort is a clinically important drug interaction, not the antidepressant effect.

What limits itIt strongly induces CYP3A4 and P-gp, so contraceptives, transplant drugs and anticoagulants fail.

FDA-approved for

Off-label

NO BOXED WARNINGS

Principal riskStrong CYP3A4 and P-gp induction; contraceptives fail

Classes and tags

Clinical profile

Direct muscarinic antagonism0 / 4

Mechanism of action: Hyperforin ballicule

Hyperforin ballicule: receptor binding, kinetics and half-life diagram

Open Hyperforin in the interactive console ↗