Virology and Vaccine Discovery, Vaccines and Immune Therapies, BioPharmaceuticals R&D, AstraZeneca, Gaithersburg, MD 20878, USA.
Clinical Pharmacology and Quantitative Pharmacology, Clinical Pharmacology and Safety Sciences, BioPharmaceuticals R&D, AstraZeneca, Gaithersburg, MD 20878, USA.
Sci Transl Med. 2022 Mar 9;14(635):eabl8124. doi: 10.1126/scitranslmed.abl8124.
Despite the success of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) vaccines, there remains a need for more prevention and treatment options for individuals remaining at risk of coronavirus disease 2019 (COVID-19). Monoclonal antibodies (mAbs) against the viral spike protein have potential to both prevent and treat COVID-19 and reduce the risk of severe disease and death. Here, we describe AZD7442, a combination of two mAbs, AZD8895 (tixagevimab) and AZD1061 (cilgavimab), that simultaneously bind to distinct, nonoverlapping epitopes on the spike protein receptor binding domain to neutralize SARS-CoV-2. Initially isolated from individuals with prior SARS-CoV-2 infection, the two mAbs were designed to extend their half-lives and reduce effector functions. The AZD7442 mAbs individually prevent the spike protein from binding to angiotensin-converting enzyme 2 receptor, blocking virus cell entry, and neutralize all tested SARS-CoV-2 variants of concern. In a nonhuman primate model of SARS-CoV-2 infection, prophylactic AZD7442 administration prevented infection, whereas therapeutic administration accelerated virus clearance from the lung. In an ongoing phase 1 study in healthy participants (NCT04507256), a 300-mg intramuscular injection of AZD7442 provided SARS-CoV-2 serum geometric mean neutralizing titers greater than 10-fold above those of convalescent serum for at least 3 months, which remained threefold above those of convalescent serum at 9 months after AZD7442 administration. About 1 to 2% of serum AZD7442 was detected in nasal mucosa, a site of SARS-CoV-2 infection. Extrapolation of the time course of serum AZD7442 concentration suggests AZD7442 may provide up to 12 months of protection and benefit individuals at high-risk of COVID-19.
尽管严重急性呼吸综合征冠状病毒 2(SARS-CoV-2)疫苗取得了成功,但仍需要更多针对有患 2019 冠状病毒病(COVID-19)风险的个体的预防和治疗选择。针对病毒刺突蛋白的单克隆抗体(mAbs)具有预防和治疗 COVID-19 的潜力,并可降低重症疾病和死亡的风险。在这里,我们描述了 AZD7442,这是一种由两种 mAbs,AZD8895(替沙吉韦单抗)和 AZD1061(西加韦单抗)组成的组合,它们同时结合到刺突蛋白受体结合域上的不同、不重叠的表位,从而中和 SARS-CoV-2。这两种 mAbs最初是从先前感染过 SARS-CoV-2 的个体中分离出来的,它们的设计目的是延长半衰期并降低效应功能。AZD7442 mAbs 可单独阻止刺突蛋白与血管紧张素转换酶 2 受体结合,阻断病毒进入细胞,并中和所有测试的 SARS-CoV-2 关切变异株。在 SARS-CoV-2 感染的非人类灵长类动物模型中,预防性给予 AZD7442 可预防感染,而治疗性给予可加速肺部病毒清除。在一项正在进行的健康参与者的 1 期研究(NCT04507256)中,肌肉注射 300mg 的 AZD7442 可使 SARS-CoV-2 血清几何平均中和滴度比恢复期血清高 10 倍以上,且在 AZD7442 给药后 9 个月仍比恢复期血清高 3 倍以上。大约 1%至 2%的血清 AZD7442 可在鼻黏膜中检测到,这是 SARS-CoV-2 感染的部位。血清 AZD7442 浓度的时间过程外推表明,AZD7442 可能提供长达 12 个月的保护,并使 COVID-19 高危个体受益。