Ruggieri Maddalena, Avolio Carlo, Livrea Paolo, Trojano Maria
Department of Neurological and Psychiatric sciences, University of Bari, Bari, Italy.
CNS Drug Rev. 2007 Summer;13(2):178-91. doi: 10.1111/j.1527-3458.2007.00010.x.
Multiple sclerosis (MS) is considered to be primarily an inflammatory autoimmune disease. Over the last 5 years, our view of the pathogenesis of MS has evolved considerably. The axonal damage was recognized as an early event in the disease process and as an important determinant of long-term disability. Therefore, the antiinflammatory and neuroprotective strategies are thought to represent promising approach to the therapy of MS. The therapeutic potential of glatiramer acetate (GA), a synthetic amino acid polymer composed of a mixture of L-glutamic acid, L-lysine, L-alanine, and L-tyrosine in defined proportions, in MS has been apparent for many years. GA has been shown to be effective in preventing and suppressing experimental allergic encephalomyelitis (EAE), the animal model of MS. GA has been, therefore, evaluated in several clinical studies and found to alter the natural history of relapsing-remitting (RR)MS by reducing the relapse rate and affecting disability. These findings were confirmed in open-label follow-up trials covering more than 10 years of treatment. The trials demonstrated sustained efficacy for GA in slowing the progression of disability. The clinical therapeutic effect of GA is consistent with the results of magnetic resonance imaging (MRI) findings from various clinical centers. At a daily standard dose of 20 mg, s.c., GA was generally well tolerated. The induction of GA-reactive T-helper 2-like regulatory suppressor cells is thought to be the main mechanism of the therapeutic action of this drug. In addition, it was recently shown that GA-reactive T cells produce neurotrophic factors (e.g., brain-derived neurotrophic factor [BDNF]) that protect neurons and axons in the area of injury.
多发性硬化症(MS)被认为主要是一种炎症性自身免疫疾病。在过去5年中,我们对MS发病机制的认识有了很大的发展。轴突损伤被认为是疾病进程中的早期事件,也是长期残疾的重要决定因素。因此,抗炎和神经保护策略被认为是治疗MS的有前景的方法。醋酸格拉替雷(GA)是一种由L-谷氨酸、L-赖氨酸、L-丙氨酸和L-酪氨酸按特定比例混合组成的合成氨基酸聚合物,其在MS治疗中的潜力多年来一直很明显。GA已被证明在预防和抑制实验性变态反应性脑脊髓炎(EAE)——MS的动物模型方面有效。因此,GA已在多项临床研究中进行了评估,并发现其可通过降低复发率和影响残疾状况来改变复发缓解型(RR)MS的自然病程。这些发现在长达10多年治疗期的开放标签随访试验中得到了证实。试验证明GA在减缓残疾进展方面具有持续疗效。GA的临床治疗效果与各临床中心的磁共振成像(MRI)结果一致。以每天20mg的标准皮下注射剂量给药时,GA通常耐受性良好。诱导产生GA反应性辅助性T细胞2样调节性抑制细胞被认为是该药治疗作用的主要机制。此外,最近有研究表明,GA反应性T细胞可产生神经营养因子(如脑源性神经营养因子[BDNF]),从而保护损伤区域的神经元和轴突。