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Resatorvid is a small molecule inhibitor of Toll-like receptor 4 (TLR4) signaling, developed primarily for the treatment of severe sepsis. It acts by binding selectively to the intracellular domain of TLR4, specifically at cysteine residue 747, thereby disrupting interactions between TLR4 and its adaptor molecules such as TIRAP and TRAM. This inhibition suppresses downstream signal transduction and reduces the production of inflammatory cytokines. Although phase III clinical trials in sepsis were halted early due to lack of efficacy, resatorvid has demonstrated anti-inflammatory and neuroprotective effects in preclinical models. It has also been explored for potential use in ulcerative colitis, various cancers (including multiple myeloma, breast cancer, ovarian cancer), traumatic brain injury, and skin tumorigenesis[1][3][4][5][6][7].
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