Chemistry:Arhalofenate
From HandWiki
Arhalofenate is a dual-acting small molecule being developed by CymaBay Therapeutics for the treatment of gout, offering both urate-lowering and anti-inflammatory effects. As a uricosuric agent, arhalofenate lowers serum urate by inhibiting its reabsorption in the proximal tubules of the kidney through blockade of transporters such as URAT1, OAT4, and OAT10.[1] Arhalofenate also suppresses gout flares by inhibiting the urate crystal–stimulated release of interleukin-1β (IL-1β), the key cytokine responsible for triggering gout attacks.[2][3][4]
References
- ↑ "The mechanism of Arhalofenate in alleviating hyperuricemia-Activating PPARγ thereby reducing caspase-1 activity". Drug Development Research 81 (7): 859–866. November 2020. doi:10.1002/ddr.21699. PMID 32506648.
- ↑ "Pipeline Therapies for Gout". Current Rheumatology Reports 26 (3): 69–80. March 2024. doi:10.1007/s11926-023-01128-3. PMID 38133712.
- ↑ "Arhalofenate acid inhibits monosodium urate crystal-induced inflammatory responses through activation of AMP-activated protein kinase (AMPK) signaling". Arthritis Research & Therapy 20 (1). September 2018. doi:10.1186/s13075-018-1699-4. PMID 30189890.
- ↑ "Role of NLRP3 in the pathogenesis and treatment of gout arthritis". Frontiers in Immunology 14. 2023. doi:10.3389/fimmu.2023.1137822. PMID 37051231.
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