Joanna Zikos, Gabriela M Webb, Helen L Wu, Jason S Reed, Jennifer Watanabe, Jodie L Usachenko, Ala M Shaqra, Celia A Schiffer, Koen K A Van Rompay, Jonah B Sacha, Diogo M Magnani
{"title":"FcRn增强突变导致怀孕猕猴的胎儿和新生儿体内艾滋病毒CCR5阻断单克隆抗体eronlimab的水平升高且持续时间延长。","authors":"Joanna Zikos, Gabriela M Webb, Helen L Wu, Jason S Reed, Jennifer Watanabe, Jodie L Usachenko, Ala M Shaqra, Celia A Schiffer, Koen K A Van Rompay, Jonah B Sacha, Diogo M Magnani","doi":"10.1080/19420862.2024.2406788","DOIUrl":null,"url":null,"abstract":"<p><p>Prenatal administration of monoclonal antibodies (mAbs) is a strategy that could be exploited to prevent viral infections during pregnancy and early life. To reach protective levels in fetuses, mAbs must be transported across the placenta, a selective barrier that actively and specifically promotes the transfer of antibodies (Abs) into the fetus through the neonatal Fc receptor (FcRn). Because FcRn also regulates Ab half-life, Fc mutations like the M428L/N434S, commonly known as LS mutations, and others have been developed to enhance binding affinity to FcRn and improve drug pharmacokinetics. We hypothesized that these FcRn-enhancing mutations could similarly affect the delivery of therapeutic Abs to the fetus. To test this hypothesis, we measured the transplacental transfer of leronlimab, an anti-CCR5 mAb, in clinical development for preventing HIV infections, using pregnant rhesus macaques to model <i>in utero</i> mAb transfer. We also generated a stabilized and FcRn-enhanced form of leronlimab, termed leronlimab-PLS. Leronlimab-PLS maintained higher levels within the maternal compartment while also reaching higher mAb levels in the fetus and newborn circulation. Further, a single dose of leronlimab-PLS led to complete CCR5 receptor occupancy in mothers and newborns for almost a month after birth. These findings support the optimization of FcRn interactions in mAb therapies designed for administration during pregnancy.</p>","PeriodicalId":18206,"journal":{"name":"mAbs","volume":"16 1","pages":"2406788"},"PeriodicalIF":5.6000,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11441024/pdf/","citationCount":"0","resultStr":"{\"title\":\"FcRn-enhancing mutations lead to increased and prolonged levels of the HIV CCR5-blocking monoclonal antibody leronlimab in the fetuses and newborns of pregnant rhesus macaques.\",\"authors\":\"Joanna Zikos, Gabriela M Webb, Helen L Wu, Jason S Reed, Jennifer Watanabe, Jodie L Usachenko, Ala M Shaqra, Celia A Schiffer, Koen K A Van Rompay, Jonah B Sacha, Diogo M Magnani\",\"doi\":\"10.1080/19420862.2024.2406788\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Prenatal administration of monoclonal antibodies (mAbs) is a strategy that could be exploited to prevent viral infections during pregnancy and early life. To reach protective levels in fetuses, mAbs must be transported across the placenta, a selective barrier that actively and specifically promotes the transfer of antibodies (Abs) into the fetus through the neonatal Fc receptor (FcRn). Because FcRn also regulates Ab half-life, Fc mutations like the M428L/N434S, commonly known as LS mutations, and others have been developed to enhance binding affinity to FcRn and improve drug pharmacokinetics. We hypothesized that these FcRn-enhancing mutations could similarly affect the delivery of therapeutic Abs to the fetus. To test this hypothesis, we measured the transplacental transfer of leronlimab, an anti-CCR5 mAb, in clinical development for preventing HIV infections, using pregnant rhesus macaques to model <i>in utero</i> mAb transfer. We also generated a stabilized and FcRn-enhanced form of leronlimab, termed leronlimab-PLS. Leronlimab-PLS maintained higher levels within the maternal compartment while also reaching higher mAb levels in the fetus and newborn circulation. Further, a single dose of leronlimab-PLS led to complete CCR5 receptor occupancy in mothers and newborns for almost a month after birth. These findings support the optimization of FcRn interactions in mAb therapies designed for administration during pregnancy.</p>\",\"PeriodicalId\":18206,\"journal\":{\"name\":\"mAbs\",\"volume\":\"16 1\",\"pages\":\"2406788\"},\"PeriodicalIF\":5.6000,\"publicationDate\":\"2024-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11441024/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"mAbs\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/19420862.2024.2406788\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/9/26 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q1\",\"JCRName\":\"MEDICINE, RESEARCH & EXPERIMENTAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"mAbs","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/19420862.2024.2406788","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/9/26 0:00:00","PubModel":"Epub","JCR":"Q1","JCRName":"MEDICINE, RESEARCH & EXPERIMENTAL","Score":null,"Total":0}
引用次数: 0
摘要
产前服用单克隆抗体(mAbs)是一种可用于预防孕期和生命早期病毒感染的策略。胎盘是一道选择性屏障,可通过新生儿 Fc 受体(FcRn)主动、特异地促进抗体(Abs)转移到胎儿体内,从而使胎儿体内的 mAbs 达到保护水平。由于 FcRn 还能调节抗体的半衰期,因此人们开发了 M428L/N434S 等 Fc 突变(通常称为 LS 突变),以增强与 FcRn 的结合亲和力,改善药物的药代动力学。我们假设,这些增强 FcRn 的突变同样会影响治疗药物 Abs 向胎儿的输送。为了验证这一假设,我们使用怀孕的恒河猴来模拟 mAb 在子宫内的转移,测量了用于预防 HIV 感染的临床开发中的抗 CCR5 mAb leronlimab 的胎盘转移情况。我们还生成了一种稳定的 FcRn 增强型来龙利单抗,称为来龙利单抗-PLS。Leronlimab-PLS在母体内保持了较高的水平,同时在胎儿和新生儿循环中也达到了较高的mAb水平。此外,单剂量的leronlimab-PLS可使母体和新生儿在出生后近一个月内完全占据CCR5受体。这些发现为优化孕期用药 mAb 疗法中的 FcRn 相互作用提供了支持。
FcRn-enhancing mutations lead to increased and prolonged levels of the HIV CCR5-blocking monoclonal antibody leronlimab in the fetuses and newborns of pregnant rhesus macaques.
Prenatal administration of monoclonal antibodies (mAbs) is a strategy that could be exploited to prevent viral infections during pregnancy and early life. To reach protective levels in fetuses, mAbs must be transported across the placenta, a selective barrier that actively and specifically promotes the transfer of antibodies (Abs) into the fetus through the neonatal Fc receptor (FcRn). Because FcRn also regulates Ab half-life, Fc mutations like the M428L/N434S, commonly known as LS mutations, and others have been developed to enhance binding affinity to FcRn and improve drug pharmacokinetics. We hypothesized that these FcRn-enhancing mutations could similarly affect the delivery of therapeutic Abs to the fetus. To test this hypothesis, we measured the transplacental transfer of leronlimab, an anti-CCR5 mAb, in clinical development for preventing HIV infections, using pregnant rhesus macaques to model in utero mAb transfer. We also generated a stabilized and FcRn-enhanced form of leronlimab, termed leronlimab-PLS. Leronlimab-PLS maintained higher levels within the maternal compartment while also reaching higher mAb levels in the fetus and newborn circulation. Further, a single dose of leronlimab-PLS led to complete CCR5 receptor occupancy in mothers and newborns for almost a month after birth. These findings support the optimization of FcRn interactions in mAb therapies designed for administration during pregnancy.
期刊介绍:
mAbs is a multi-disciplinary journal dedicated to the art and science of antibody research and development. The journal has a strong scientific and medical focus, but also strives to serve a broader readership. The articles are thus of interest to scientists, clinical researchers, and physicians, as well as the wider mAb community, including our readers involved in technology transfer, legal issues, investment, strategic planning and the regulation of therapeutics.