Drug intelligence / Profile preview

cafestol

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

Overview

Cafestol is a natural diterpenoid molecule found in coffee beans, particularly in unfiltered coffee such as French press and Turkish coffee[1][3]. It is known for its diverse biological activities, including raising serum cholesterol levels by inhibiting bile acid synthesis through downregulation of cholesterol 7α-hydroxylase and sterol 27-hydroxylase[5][6]. Cafestol acts as an agonist ligand for nuclear receptors such as farnesoid X receptor (FXR) and pregnane X receptor (PXR), affecting cholesterol homeostasis[1][4]. Beyond its impact on lipid metabolism, cafestol exhibits anti-inflammatory, anticarcinogenic, hepatoprotective, antidiabetic, and neuroprotective properties. Mechanistically, it can increase glucose-stimulated insulin secretion and glucose uptake in muscle cells; it also modulates inflammatory mediators via pathways like Nrf2/HO-1 and Sirt1 activation[2][3]. Cafestol has shown potential benefits in models of cancer prevention and neuroprotection (e.g., Parkinson’s disease models)[2].

Other names
cafesterolcoffeol
02

Targets

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

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