Drug intelligence / Profile preview

petasites hybridus extract

Development stage
Phase 4
Lead developer
Weber & Weber
Administration
Oral
01

Overview

**Petasites hybridus extract** is a standardized herbal extract derived from the rhizome and/or leaves of the plant Petasites hybridus, commonly known as butterbur. Its primary active constituents are petasins, a group of sesquiterpene esters (such as petasin, isopetasin, neopetasin) that exert multiple anti-inflammatory effects. The mechanisms involve inhibition of cyclooxygenase-2 (COX-2) activity and expression, blockade of 5-lipoxygenase, suppression of phospholipase C activity, and inhibition of leukotriene and prostaglandin biosynthesis. Petasins also demonstrate calcium channel antagonism, inhibiting L-type voltage-dependent calcium channels (VDCCs), and reduce calcium influx in neutrophils and eosinophils. These activities are relevant to migraine prophylaxis, tension headache reduction, and potentially allergy and asthma management. Commercial extracts (notably Petadolex, Ze339) are produced using CO2 extraction to minimize hepatotoxic pyrrolizidine alkaloids (PAs). The primary indication is migraine prevention, with clinical studies demonstrating efficacy and good tolerability.

Brand names
PetadolexZe 339Ze339Ze-339
Other names
butterbur extractbutterbur root extractbutterbur leaf extractPetasites hybridus rhizome extract
02

Targets

ALOX12 (Arachidonate 12-lipoxygenase, 12S type)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)LTCC (Voltage-gated calcium channel (L-type))

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