Drug intelligence / Profile preview

guggulu

Development stage
Unknown
Lead developer
Azienda ASL Brescia
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Guggulu is a natural gum resin derived from the mukul myrrh tree (*Commiphora mukul*), a plant native to India. It has been a cornerstone of Ayurvedic medicine for millennia, traditionally used to treat conditions such as arthritis, obesity, and lipid disorders. The therapeutic effects of guggulu are primarily attributed to guggulsterones (E- and Z-isomers), which are ketonic steroids that modulate nuclear receptors involved in cholesterol metabolism. Specifically, guggulsterones act as antagonists of the farnesoid X receptor (FXR) and agonists of the pregnane X receptor (PXR), thereby promoting the conversion of cholesterol into bile acids and inhibiting its biosynthesis. Guggulu is approved as an antihyperlipidemic drug in India under the brand name Gugulipid. In Western markets, it is widely available as a dietary supplement. Recent clinical research, such as a Phase 3 trial conducted by Azienda ASL Brescia in Italy, has explored its potential in combination with other Ayurvedic formulations like Triphala for managing hypercholesterolemia and weight in patients who are not candidates for statin therapy.

Brand names
Gugulipid
Other names
guggulgum guggulCommiphora mukul resinIndian bdellium
02

Targets

PXR (Pregnane X receptor)FXR (Farnesoid x-activated receptor)

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