【 文献重点摘要 】
 

Botulinum neurotoxin type-A (BoNT-A) blocks the release of acetylcholine from peripheral cholinergic nerve terminals and is an important option for the treatment of disorders characterised by excessive cholinergic neuronal activity . Several BoNT-A products are currently marketed, each with unique manufacturing processes, excipients, formulation, and non-interchangeable potency units. Nevertheless, the effects of all the products are mediated by the 150 kDa BoNT-A neurotoxin. We assessed the quantity and light chain (LC) activity of BoNT-A in three commercial BoNT-A products (Dysport®; Botox®; Xeomin®). We quantified 150 kDa BoNT-A by sandwich ELISA and assessed LC activity by EndoPep assay . In both assays, we assessed the results for the commercial products against recombinant 150 kDa BoNT-A. The mean 150 kDa BoNT-A content per vial measured by ELISA was 2.69 ng/500 U vial Dysport®, 0.90 ng/100 U vial Botox®, and 0.40 ng/100 U vial Xeomin®. To present clinically relevant results, we calculated the 150 kDa BoNT-A/US Food and Drug Administration (FDA)-approved dose in adult upper limb spasticity: 5.38 ng Dysport®(1000 U; 2 × 500 U vials), 3.60 ng Botox®(400 U; 4 × 100 U vials), and 1.61 ng Xeomin®(400 U; 4 × 100 U vials). EndoPep assay showed similar LC activity among BoNT-A products. Thus, greater amounts of active neurotoxin are injected with Dysport®, at FDA-approved doses, than with other products. This fact might explain the long duration of action reported across multiple indications, which benefits patients, caregivers, clinicians, and healthcare systems.

Keywords

botulinum toxin; BoNT; spasticity; Dysport®, abobotulinumtoxinA; glabellar lines

A型肉毒神经毒素(BoNT-A)可阻断外周胆碱能神经末梢的乙酰胆碱释放，是治疗以胆碱能神经元过度活动为特征的疾病的重要选择。目前市场上有几种BoNT-A产品，每种产品都有独特的制造工艺、辅料、配方和不可互换的效价单位。然而，所有这些产物的作用都是由150 kDa的BoNT-A神经毒素介导的。我们评估了三种商用BoNT-A产品(Dysport®、Botox®和Xeomin®)中BoNT-A的数量和轻链(LC)活性。用夹心ELISA法定量150 kDa BoNT-A，用EndoPep法测定LC活性。在这两种检测中，我们评估了商业化产品对重组150 kDa BoNT-A的抑制效果。ELISA测定的平均150 kDa BoNT-A含量为2.69 ng/500U小瓶Dysport®、0.90 ng/100U小瓶肉毒杆菌®和0.40 ng/100U小瓶Xeomin®。为了展示临床相关结果，我们计算了美国食品和药物管理局(FDA)批准的150 kDa BoNT-A治疗成人上肢痉挛的剂量：5.38 ng Dysport®(1000 U；2×500 U瓶装)、3.60 ng Botox®(400 U；4×100 U瓶装)和1.61 ng Xeomin®(400 U；4×100 U瓶装)。EndoPep分析表明，不同的BoNT-A产物具有相似的LC活性。因此，与其他产品相比，Dysport®按FDA批准的剂量注射的活性神经毒素更多。这一事实可能解释了多个适应症报告的长期作用，这使患者、护理者、临床医生和医疗保健系统受益。

关键词

肉毒杆菌毒素；BoNT；痉挛；Dysport®，A型肉毒毒素；眉间纹