Smith Heidi L, Cheslock Peter, Leney Mark, Barton Bruce, Molrine Deborah C
a MassBiologics of the University of Massachusetts Medical School , Boston , MA , USA.
b University of Massachusetts Medical School , Worcester , MA , USA.
Virulence. 2016 Aug 17;7(6):660-8. doi: 10.1080/21505594.2016.1171436. Epub 2016 Apr 12.
Prompt administration of anti-toxin reduces mortality following Corynebacterium diphtheriae infection. Current treatment relies upon equine diphtheria anti-toxin (DAT), with a 10% risk of serum sickness and rarely anaphylaxis. The global DAT supply is extremely limited; most manufacturers have ceased production. S315 is a neutralizing human IgG1 monoclonal antibody to diphtheria toxin that may provide a safe and effective alternative to equine DAT and address critical supply issues. To guide dose selection for IND-enabling pharmacology and toxicology studies, we dose-ranged S315 and DAT in a guinea pig model of diphtheria intoxication based on the NIH Minimum Requirements potency assay. Animals received a single injection of antibody premixed with toxin, were monitored for 30 days, and assigned a numeric score for clinical signs of disease. Animals receiving ≥ 27.5 µg of S315 or ≥ 1.75 IU of DAT survived whereas animals receiving ≤ 22.5 µg of S315 or ≤ 1.25 IU of DAT died, yielding a potency estimate of 17 µg S315/IU DAT (95% CI 16-21) for an endpoint of survival. Because some surviving animals exhibited transient limb weakness, likely a systemic sign of toxicity, DAT and S315 doses required to prevent hind limb paralysis were also determined, yielding a relative potency of 48 µg/IU (95% CI 38-59) for this alternate endpoint. To support advancement of S315 into clinical trials, potency estimates will be used to evaluate the efficacy of S315 versus DAT in an animal model with antibody administration after toxin exposure, more closely modeling anti-toxin therapy in humans.
及时给予抗毒素可降低白喉棒状杆菌感染后的死亡率。目前的治疗依赖马源白喉抗毒素(DAT),有10%的血清病风险,且极少发生过敏反应。全球DAT供应极其有限;大多数生产商已停止生产。S315是一种针对白喉毒素的中和性人IgG1单克隆抗体,可能为马源DAT提供一种安全有效的替代方案,并解决关键的供应问题。为指导用于支持研究性新药(IND)的药理学和毒理学研究的剂量选择,我们基于美国国立卫生研究院(NIH)最低要求效价测定法,在豚鼠白喉中毒模型中对S315和DAT进行了剂量范围研究。动物接受单次注射与毒素预混合的抗体,监测30天,并根据疾病临床症状给予数字评分。接受≥27.5μg S315或≥1.75IU DAT的动物存活,而接受≤22.5μg S315或≤1.25IU DAT的动物死亡,得出以存活为终点的效价估计值为17μg S315/IU DAT(95%置信区间16 - 21)。由于一些存活动物表现出短暂的肢体无力,这可能是毒性的全身表现,因此还确定了预防后肢麻痹所需的DAT和S315剂量,对于这个替代终点得出相对效价为48μg/IU(95%置信区间38 - 59)。为支持S315推进到临床试验,效价估计值将用于评估在毒素暴露后给予抗体的动物模型中S315与DAT的疗效,该模型更接近模拟人类的抗毒素治疗。