Etanercept is a competitive tumor necrosis factor (TNF) inhibitor that prevents TNF-α and TNF-β from binding to cell surface receptors[1]. Etanercept is effective for rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis[2].
In vitro, Etanercept (1 μg/mL) significantly reduces TNF-α secretion levels in THP-1 cells after 3 hours of treatment following lipopolysaccharide (LPS) stimulation[3].
In vivo, Etanercept (10mg/kg) administered subcutaneously in rats with adjuvant-induced arthritis (AIA) significantly reduces arthritis scores, improves endothelial function and the NOS/BH4/arginase balance, and inhibits the cyclooxygenase-2 (COX-2) pathway[4]. Etanercept (5mg/kg) administered subcutaneously in rats with periodontitis significantly reduces periodontitis inflammation and tissue damage, decreases neutrophil infiltration, and downregulates the expression of apoptotic regulatory factors Bax and Bcl-2[5]. Etanercept (5 mg/kg) administered intraperitoneally in rats with traumatic brain injury (TBI) significantly improves TBI-induced cerebral ischemia, motor and cognitive deficits, inhibits neuronal and glial apoptosis, and reduces levels of inflammatory factors[6].
References:
[1] Alldred A. Etanercept in rheumatoid arthritis[J]. Expert opinion on pharmacotherapy, 2001, 2(7): 1137-1148.
[2] Culy C R, Keating G M. Etanercept: an updated review of its use in rheumatoid arthritis, psoriatic arthritis and juvenile rheumatoid arthritis[J]. Drugs, 2002, 62(17): 2493-2537.
[3] Grattendick K J, Nakashima J M, Feng L, et al. Effects of three anti-TNF-α drugs: etanercept, infliximab and pirfenidone on release of TNF-α in medium and TNF-α associated with the cell in vitro[J]. International immunopharmacology, 2008, 8(5): 679-687.
[4] Totoson P, Maguin-Gaté K, Prigent-Tessier A, et al. Etanercept improves endothelial function via pleiotropic effects in rat adjuvant-induced arthritis[J]. Rheumatology, 2016, 55(7): 1308-1317.
[5] Di Paola R, Mazzon E, Muià C, et al. Effects of etanercept, a tumour necrosis factor‐α antagonist, in an experimental model of periodontitis in rats[J]. British journal of pharmacology, 2007, 150(3): 286-297.
[6] Chio C C, Lin J W, Chang M W, et al. Therapeutic evaluation of etanercept in a model of traumatic brain injury[J]. Journal of neurochemistry, 2010, 115(4): 921-929.
Etanercept是一种竞争性肿瘤坏死因子（TNF）抑制剂，抑制TNF-α和TNF-β与细胞表面受体的结合[1]。Etanercept对风湿性关节炎、幼年特发性关节炎和斑块性银屑病有效[2]。
在体外，Etanercept（1μg/mL）处理THP-1细胞3 h，显著降低了细胞在脂多糖（LPS）刺激后TNF-α的分泌水平[3]。
在体内，Etanercept（10mg/kg）通过皮下注射治疗辅助诱导关节炎（AIA）大鼠，显著降低了关节炎评分，改善了内皮功能和NOS/BH4/精氨酸酶平衡，抑制了环氧合酶2（COX-2）通路[4]。Etanercept（5mg/kg）通过皮下注射治疗牙周炎大鼠，显著降低牙周炎炎症和组织损伤，减少了中性粒细胞浸润，下调了细胞调亡调节因子Bax和Bcl-2的表达[5]。Etanercept（5mg/kg）通过腹膜注射治疗创伤性脑损伤（TBI）大鼠，显著改善了TBI诱导的脑缺血、运动和认知功能缺陷，抑制了神经元胶质细胞凋亡，降低了炎症因子水平[6]。