Zajączkowska Renata, Mika Joanna, Leppert Wojciech, Kocot-Kępska Magdalena, Malec-Milewska Małgorzata, Wordliczek Jerzy
Department of Interdisciplinary Intensive Care, Jagiellonian University Medical College, 31-008 Krakow, Poland.
Department of Pain Pharmacology, Maj Institute of Pharmacology, Polish Academy of Sciences, 31-343 Krakow, Poland.
Pharmaceuticals (Basel). 2021 Jan 31;14(2):112. doi: 10.3390/ph14020112.
The efficacy of neuropathic pain control remains unsatisfactory. Despite the availability of a variety of therapies, a significant proportion of patients suffer from poorly controlled pain of this kind. Consequently, new drugs and treatments are still being sought to remedy the situation. One such new drug is mirogabalin, a selective ligand for the α2δ subunits of voltage-gated calcium channels (VGCC) developed by Sankyo group for the management of neuropathic pain. In 2019 in Japan, mirogabalin was approved for peripheral neuropathic pain following the encouraging results of clinical trials conducted with diabetic peripheral neuropathic pain (DPNP) and postherpetic neuralgia (PHN) patients. The ligand selectivity of mirogabalin for α2δ-1 and α2δ-2 and its slower dissociation rate for α2δ-1 than for α2δ-2 subunits of VGCC may contribute to its strong analgesic effects, wide safety margin, and relatively lower incidence of adverse effects compared to pregabalin and gabapentin. This article discusses the mechanism of action of mirogabalin, presents data on its pharmacodynamics and pharmacokinetics, and reviews the available experimental and clinical studies that have assessed the efficacy and safety of the drug in the treatment of selected neuropathic pain syndromes.
神经性疼痛的控制效果仍不尽人意。尽管有多种治疗方法，但仍有相当一部分患者的此类疼痛控制不佳。因此，人们仍在寻求新的药物和治疗方法来改善这种情况。一种这样的新药是米罗加巴林，它是三共集团开发的用于治疗神经性疼痛的电压门控钙通道（VGCC）α2δ亚基的选择性配体。2019年在日本，米罗加巴林在对糖尿病性周围神经病变性疼痛（DPNP）和带状疱疹后神经痛（PHN）患者进行的临床试验取得令人鼓舞的结果后，被批准用于治疗周围神经性疼痛。米罗加巴林对α2δ-1和α2δ-2的配体选择性以及其对α2δ-1的解离速率比对VGCC的α2δ-2亚基慢，这可能导致其具有强大的镇痛作用、较宽的安全范围，并且与普瑞巴林和加巴喷丁相比不良反应发生率相对较低。本文讨论了米罗加巴林的作用机制，介绍了其药效学和药代动力学数据，并综述了评估该药物治疗特定神经性疼痛综合征的疗效和安全性的现有实验和临床研究。
