Drug intelligence / Profile preview

Radix Puerariae lobatae

Development stage
Unknown
Lead developer
The Chinese University of Hong Kong
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Radix Puerariae lobatae, commonly known as Gegen or kudzu root, is a traditional Chinese herbal medicine derived from the dried root of *Pueraria lobata* (Willd.) Ohwi. It is widely used in East Asia for the treatment of cardiovascular diseases, diabetes, fever, and alcohol-related disorders. The primary bioactive components of Radix Puerariae lobatae are isoflavonoids, most notably puerarin, daidzein, and daidzin. Clinical and preclinical studies, including those led by the Chinese University of Hong Kong, have evaluated its potential for herb-drug interactions, demonstrating that it can modulate cytochrome P450 (CYP) enzymes—particularly inhibiting CYP2C19 and inducing CYP1A2—and alter anticoagulation biomarkers, which may offset the effects of co-administered drugs like warfarin. Additionally, recent research has highlighted its role in regulating intestinal fat absorption and body weight through the positive allosteric modulation of GABAA receptors containing the α1 subunit (GABRA1) in the brain-gut axis.

Other names
GegenPueraria lobata rootPuerariae Lobatae RadixYegekudzu root
02

Targets

HTR2C (5-hydroxytryptamine 2C receptor)ESR1 (ERα)ESR2 (ERβ)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)THBD (Thrombomodulin)VKORC1 (Vitamin K epoxide reductase complex subunit 1)

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