Drug intelligence / Profile preview

petasites

Development stage
Unknown
Lead developer
Max Zeller Söhne
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Petasites, commonly known as butterbur, is a botanical extract derived from the roots or leaves of the *Petasites hybridus* plant. It is primarily utilized for the preventive treatment of migraine and the management of allergic rhinitis. The active constituents, petasin and isopetasin, are believed to exert therapeutic effects through the inhibition of leukotriene synthesis (via 5-lipoxygenase inhibition) and by acting as L-type calcium channel blockers, which provide anti-inflammatory and antispasmodic properties. Clinical studies, including randomized controlled trials, have demonstrated that standardized, pyrrolizidine alkaloid-free extracts (such as Petadolex) significantly reduce the frequency of migraine attacks. Due to the presence of hepatotoxic and carcinogenic pyrrolizidine alkaloids in the raw plant, commercial preparations must be processed to remove these compounds to ensure safety.

Brand names
PetadolexTesalinPetaforce
Other names
butterburPetasites hybridusPetasites extractPetasites hybridus root extract
02

Targets

PLA2 (Phospholipase A2 group IID)ALOX5 (Arachidonate 5-lipoxygenase)PDE3PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PLC (Phospholipase C family)PDE4 (Phosphodiesterase 4A1)OCT3 (Organic cation transporter 3)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)

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