Drug intelligence / Profile preview

bigelovin

Development stage
Preclinical
Modality
Small Molecules
Administration
Intravenous
01

Overview

Bigelovin is a **sesquiterpene lactone** isolated from the plant *Inula helianthus-aquatica*. It functions as a **selective retinoid X receptor α agonist**, demonstrating potent anti-tumor, anti-inflammatory, and anti-angiogenic properties. Bigelovin induces apoptosis and autophagy in various cancer cell lines, including liver and colorectal cancers, by inhibiting the mTOR pathway and generating reactive oxygen species (ROS)[1][3][5][6]. It selectively inhibits the JAK2/STAT3 signaling pathway by inactivating JAK2, reduces NF-κB signaling via IKK-β degradation, upregulates death receptor 5 (DR5), and causes cell cycle G2/M arrest and DNA damage, contributing to its cytotoxic and anti-proliferative effects[2][3][4]. The compound shows efficacy in animal xenograft models and is mainly used in preclinical research.

Other names
bigelovinBigVsesquiterpene lactone from Inula helianthus-aquatica
02

Targets

STAT3 (Signal Transducer and Activator of Transcription 3)mTOR (Mammalian target of rapamycin kinase)JAK2 (Janus kinase 2)RXRA (Retinoid X receptor alpha)

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