Drug intelligence / Profile preview

arglabin

Development stage
Unknown
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Arglabin is a sesquiterpene lactone of the guaianolide subclass, originally isolated from Artemisia glabella. It is characterized by a 5,7,5-tricyclic ring system with an epoxide and an exocyclic methylene group conjugated to the carbonyl of the lactone. Arglabin acts as an inhibitor of farnesyl transferase, thereby interfering with RAS proto-oncogene activation—a key pathway in many human tumors[4]. It also inhibits the NLRP3 inflammasome, reducing production of pro-inflammatory cytokines IL-1β and IL-18[5]. Preclinical studies show that arglabin reduces inflammation and plasma lipids, increases autophagy, and shifts macrophages toward an anti-inflammatory phenotype. These effects result in reduced atherosclerotic lesions in animal models[3][5]. Clinically, arglabin has been studied as an anticancer agent for breast cancer (notably in Kazakhstan), colon cancer, ovarian cancer, lung cancer[3][4][6], and has shown activity against acute myelogenous leukemia cell lines comparable to parthenolide[4]. Its immunomodulatory properties include regulation of cytokine production such as IL-1β, IL-2, and TNF-alpha.

Brand names
Arglabin
Other names
ArglabinSesquiterpene lactone guaianolide (class descriptor)84692-91-1 (CAS number)
02

Targets

FTase (Protein Farnesyltransferase)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)

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