News - Liminal BioSciences will be presenting at EASL Congress 2026 (27–30 May) in Barcelona
Selective GPR84 Antagonist
Selective G-protein coupled receptor 84 (GPR84) Antagonist
GPR84 is a pro-inflammatory target primarily expressed on cells associated with the immune system and its expression levels increase significantly during periods of inflammatory stress. Inhibition of GPR84 can inhibit neutrophil and macrophage migration and reduce cytokine release.
We believe that the GPR84 receptor could be an important biological target in metabolic disease. Our clinical and preclinical research, combined with published work from other groups, indicates a potential role for antagonism of GPR84 in metabolic diseases, including MASH.
Our GPR84 Antagonist Program – Focused on developing a best-in-class, oral GPR84 antagonist for MASH/MAFLD
Our lead compound is CBI-6511 is a selective, high-potency, small molecule antagonist of the medium-chain fatty acid receptor GPR84. CBI-6511 has a differentiated but complimentary mechanism of action compared to standard of care therapies.
In pre-clinical experiments, GPR84 antagonists are active in high fat diet models of MASH/MAFLD with significant reductions in LDL-c and liver steatosis.
CBI-6511 has completed a Phase 1 SAD/MAD clinical study in healthy volunteers and was found to be generally safe and well-tolerated with pharmacokinetics suitable for once or twice daily oral dosing.
We have also completed a 28-day dose-range finding Phase 1b/2a clinical trial in healthy volunteers with high Body Mass Index (“BMI”) to evaluate the effect of CBI-6511 on serum lipids and to evaluate the effect of CBI-6511 taken in combination with a statin.
We are now planning to commence a 12-week Phase IIa study in MASH in early 2027.
Further Reading:
*These links will take you to an independent third party website site.
- Adiponectin, a Therapeutic Target for Obesity, Diabetes, and Endothelial Dysfunction
- GLPG1205, a GPR84 Modulator: Safety, Pharmacokinetics, and Pharmacodynamics in Healthy Subjects
- Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84
- An expressed sequence tag (EST) data mining strategy succeeding in the discovery of new G-protein coupled receptors
- Inflammatory changes in adipose tissue enhance expression of GPR84, a medium-chain fatty acid receptor: TNFα enhances GPR84 expression in adipocytes
- Medium-chain Fatty Acids as Ligands for Orphan G Protein-coupled Receptor GPR84
- Activation of the Immune-Metabolic Receptor GPR84 Enhances Inflammation and Phagocytosis in Macrophages
- Pharmacology of Free Fatty Acid Receptors and Their Allosteric Modulators
