Constantinescu Simona E, Constantinescu Cris S
a School of Medicine , University of Newcastle , Newcastle , UK.
Expert Rev Clin Pharmacol. 2016;9(1):49-57. doi: 10.1586/17512433.2016.1108189. Epub 2015 Nov 4.
Laquinimod (ABR-215062) is an oral immunomodulatory agent developed for the treatment of relapsing multiple sclerosis (MS). Laquinimod is a derivative of the drug roquinimex, but lacks the unacceptable side effect profile of this drug which was documented in previous MS trials. Preclinical studies in experimental models of MS, both of autoimmune neuroinflammation and of toxin induced demyelination show a multitude of immunomodulatory and anti-inflammatory effects, including some that are effective directly in the central nervous system. Phase I study results confirmed the safety and tolerability of laquinimod, and phase II and III studies provide a picture of a consistent albeit moderate effect on relapse rate and new lesion development on magnetic resonance imaging combined with a stronger effect on sustained progression and brain atrophy. These findings make laquinimod a potentially useful future treatment of MS.
拉喹莫德（ABR - 215062）是一种口服免疫调节剂，用于治疗复发型多发性硬化症（MS）。拉喹莫德是药物罗喹美克的衍生物，但没有该药物在先前MS试验中所记录的不可接受的副作用。在MS的实验模型中进行的临床前研究，无论是自身免疫性神经炎症模型还是毒素诱导的脱髓鞘模型，都显示出多种免疫调节和抗炎作用，包括一些直接作用于中枢神经系统的有效作用。I期研究结果证实了拉喹莫德的安全性和耐受性，II期和III期研究表明，拉喹莫德对复发率和磁共振成像上新病灶的形成有一致但适度的影响，对持续进展和脑萎缩有更强的影响。这些发现使拉喹莫德成为未来治疗MS的一种潜在有用药物。
