JNJ-678 (JNJ-53718678) is a respiratory syncytial virus (RSV) fusion protein inhibitor[1-2]. JNJ-678 inhibits the fusion of the virus with the host cell membrane by binding to and stabilizing the prefusion conformation of the RSV fusion protein, thereby preventing viral entry into host cells. JNJ-678 is suitable for research related to RSV infection[3-4].
In vitro, human bronchial epithelial cells (HBECs) were infected with RSV. After 6–24 hours, JNJ-678 (100nM) was added, and the incubation continued for 3 days. JNJ-678 significantly inhibited viral replication[5].
In vivo, cotton rats were orally administered a single dose of JNJ-678 (1–100mg/kg) 1 hour prior to intranasal RSV challenge. JNJ-678 significantly reduced infectious virus titers in the lungs[5].
References:
[1] Huntjens DRH, Ouwerkerk-Mahadevan S, Brochot A, et al. Population Pharmacokinetic Modeling of JNJ-53718678, a Novel Fusion Inhibitor for the Treatment of Respiratory Syncytial Virus: Results from a Phase I, Double-Blind, Randomized, Placebo-Controlled First-in-Human Study in Healthy Adult Subjects. Clin Pharmacokinet. 2017 Nov;56(11):1331-1342.
[2] Stevens M, Rusch S, DeVincenzo J, et al. Antiviral Activity of Oral JNJ-53718678 in Healthy Adult Volunteers Challenged With Respiratory Syncytial Virus: A Placebo-Controlled Study. J Infect Dis. 2018 Jul 24;218(5):748-756.
[3] Cockerill GS. JNJ-5371678, Defining a Role for Fusion Inhibitors in the Treatment of Respiratory Syncytial Virus. J Med Chem. 2020 Aug 13;63(15):8043-8045.
[4] Cichero E, Calautti A, Francesconi V, et al. Probing In Silico the Benzimidazole Privileged Scaffold for the Development of Drug-like Anti-RSV Agents. Pharmaceuticals (Basel). 2021 Dec 15;14(12):1307.
[5] Roymans D, Alnajjar SS, Battles MB, et al. Therapeutic efficacy of a respiratory syncytial virus fusion inhibitor. Nat Commun. 2017 Aug 1;8(1):167.
JNJ-678 (JNJ-53718678)是一种呼吸道合胞病毒（RSV）融合蛋白抑制剂[1-2]。JNJ-678通过结合并稳定RSV融合蛋白的预融合构象来抑制病毒与宿主细胞膜的融合，从而阻止病毒进入宿主细胞。JNJ-678可用于呼吸道合胞病毒感染的相关研究[3-4]。
在体外，对支气管上皮细胞（HBECs）感染呼吸道合胞病毒（RSV）6-24小时后，加入JNJ-678（100nM）继续孵育3天。JNJ-678能显著抑制病毒复制[5]。
在体内，JNJ-678（1-100mg/kg；口服）用于处理在RSV感染前1小时接受给药的棉鼠。JNJ-678显著降低了肺中的感染性病毒滴度[5]。