Chemistry:GLPG1205
From HandWiki
GLPG1205 is an experimental drug which acts as a selective antagonist (or perhaps negative allosteric modulator) at the free fatty acid receptor GPR84.[1] It has antiinflammatory and anti-fibrotic effects and reached Phase II human clinical trials for treatment of both ulcerative colitis and idiopathic pulmonary fibrosis, although development for both indications was ultimately dropped due to poor efficacy.[2] However, it continues to be researched for potential applications in the treatment of other conditions such as asthma and acute immune-mediated liver injury.[3][4]
References
- ↑ "Discovery of 9-Cyclopropylethynyl-2-((S)-1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial". Journal of Medicinal Chemistry 63 (22): 13526–13545. November 2020. doi:10.1021/acs.jmedchem.0c00272. PMID 32902984.
- ↑ "GLPG1205 for idiopathic pulmonary fibrosis: a phase 2 randomised placebo-controlled trial". The European Respiratory Journal 61 (3). March 2023. doi:10.1183/13993003.01794-2022. PMID 36328358.
- ↑ "The GPR84 Antagonist GLPG1205 Reduces Features of Disease in Experimental Severe Asthma". American Journal of Respiratory Cell and Molecular Biology 70 (5): 424–427. May 2024. doi:10.1165/rcmb.2023-0221LE. PMID 38690993.
- ↑ "Targeting GPR84 to alleviate acute immune-mediated liver injury". Molecular Medicine (Cambridge, Mass.) 31 (1): 187. May 2025. doi:10.1186/s10020-025-01248-9. PMID 40369402.
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