Drug intelligence / Profile preview

isopetasin

Development stage
Preclinical
Lead developer
Johannes Gutenberg-University Mainz
Modality
Small Molecules
Administration
Oral, Subcutaneous (investigational/preclinical)
01

Overview

**Isopetasin** is a bioactive sesquiterpene found principally in Petasites species, especially *Petasites hybridus* and *Petasites formosanus*, and is part of the terpenoid family[10]. It possesses notable anti-inflammatory, analgesic, and antispasmodic actions, and has been identified as an active component responsible for anti-migraine effects in butterbur extracts[2][4][10]. Mechanistically, isopetasin acts as a selective agonist of the TRPA1 ion channel (Transient receptor potential ankyrin 1), thus desensitizing peptidergic nociceptors[2][4]. It also exhibits cytotoxic activity toward multidrug-resistant cancer cell models by directly inhibiting the P-glycoprotein (ABCB1), resulting in increased drug accumulation, mitochondrial stress, reactive oxygen species (ROS) generation, and apoptosis[7]. The compound is primarily researched for migraine prevention, but also investigated in cancer models.

Other names
Eremophila-7(11),9-dien-8-one,3alpha-hydroxy-,2-methylcrotonate,(Z)
02

Targets

TRPA1 (Transient receptor potential cation channel subfamily A member 1)

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