Drug intelligence / Profile preview

FFAR4 agonist + GPR84 agonist

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Rectal
01

Overview

This is a combination of two pharmacological agents, one acting as an agonist at the Free Fatty Acid Receptor 4 (FFAR4, also known as GPR120) and the other as an agonist at G protein-coupled receptor 84 (GPR84). Both are G protein-coupled receptors involved in metabolic and inflammatory signaling. FFAR4 activation is associated with anti-inflammatory effects, improved insulin sensitivity, gut hormone release (such as GLP-1 and PYY), and energy homeostasis. GPR84 activation is linked to proinflammatory responses in immune cells but also modulates gut hormone secretion when coactivated with FFAR4. In a proof-of-concept study in obese adults, combined colonic delivery of natural FFAR4 and GPR84 agonists reduced caloric intake and increased postprandial peptide YY (PYY) levels without adverse effects[1]. The combination targets enteroendocrine cells that coexpress both receptors; their simultaneous activation leads to superadditive release of appetite-regulating hormones such as GLP-1 and PYY[1]. This approach is being explored for obesity management.

02

Targets

FFAR4 (Free fatty acid receptor 4)GPR84

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