Gilead Sciences announced a significant milestone: the U.S. FDA accepted their New Drug Applications (NDAs) for lenacapavir (LEN), a groundbreaking twice-yearly injectable HIV-1 capsid inhibitor for pre-exposure prophylaxis (PrEP). The FDA granted priority review, with a decision expected by June 19, 2025.

吉利德科学宣布了一项重要里程碑：美国食品药品监督管理局（FDA）接受了他们关于lenacapavir（LEN）的新药申请（NDAs），这是一种用于暴露前预防（PrEP）的突破性每半年注射一次的HIV-1衣壳抑制剂。FDA授予其优先审查，预计将于2025年6月19日作出决定。

LEN represents a novel class of HIV therapies by targeting the viral capsid, a multifunctional protein essential for HIV replication. Unlike traditional antiretrovirals that target enzymes such as reverse transcriptase or protease, LEN binds directly to the capsid protein, disrupting several critical steps in the virus’s life cycle..

LEN 代表了一类通过靶向病毒衣壳的新型 HIV 治疗方法，病毒衣壳是一种对 HIV 复制至关重要的多功能蛋白。与传统抗逆转录病毒药物靶向逆转录酶或蛋白酶不同，LEN 直接结合衣壳蛋白，破坏病毒生命周期中的多个关键步骤。

At Sino Biological, we are proud to support this era of progress with our industry-leading recombinant HIV antigen products. As the fight against HIV evolves, our high-quality antigens empower researchers, vaccine developers, and diagnostic innovators to stay ahead of the curve.

在义翘神州，我们很自豪能够通过我们行业领先的重组 HIV 抗原产品来支持这个进步的时代。随着对抗 HIV 的斗争不断发展，我们的高质量抗原使研究人员、疫苗开发人员和诊断创新者能够保持领先。

Mechanism of Action

作用机制

LEN is a first-in-class, long-acting HIV-1 capsid inhibitor that disrupts multiple stages of the viral replication cycle. By binding to the capsid protein, it blocks the nuclear import of HIV-1 proviral DNA, preventing its integration into the host genome. Additionally, it disrupts capsid core formation, resulting in structurally defective virions, and interferes with Gag/Gag-Pol function, reducing proper virus assembly and release.

LEN 是一种首创的长效 HIV-1 衣壳抑制剂，能够破坏病毒复制周期的多个阶段。通过与衣壳蛋白结合，它阻止 HIV-1 前病毒 DNA 的核输入，防止其整合到宿主基因组中。此外，它还破坏衣壳核心的形成，导致结构缺陷的病毒颗粒，并干扰 Gag/Gag-Pol 功能，减少病毒的正确组装和释放。

This multistage inhibition gives LEN potent antiviral activity, even against drug-resistant HIV-1 strains. Administered subcutaneously every six months after an oral lead-in phase, its extended half-life (8–12 weeks) ensures sustained viral suppression, offering a promising option for individuals with multidrug-resistant HIV or those seeking alternatives to daily therapy (Figure 1)..

这种多阶段抑制作用赋予了LEN强大的抗病毒活性，即使是对抗耐药性HIV-1毒株也同样有效。在口服引导期后，每六个月通过皮下注射给药，其延长的半衰期（8-12周）确保了持续的病毒抑制，为具有多重耐药性的HIV患者或寻求每日治疗替代方案的人群提供了有前景的选择（图1）。

Figure 1. Mechanism of Action of LEN

图1. LEN的作用机制

Why Choose Sino Biological HIV Antigens?

为什么选择义翘神州的HIV抗原？

Featured Product: HIV-1 Envelope Glycoprotein

特色产品：HIV-1 包膜糖蛋白

Research Application

研究应用

Sino Biological products are frequently cited in well-reputed journals. For instance, Yang, C., Liu, D., and colleagues used recombinant HIV capsid protein p24 (Sino Biological) and an HIV-1 p24 ELISA Pair Set to develop a gold nanorod (AuNR)-based microfluidic-integrated multicolor immunosensor for HIV-1 p24 detection with patients’ serum samples.

义翘神州的产品频繁被知名期刊引用。例如，Yang, C.、Liu, D.及其同事使用了重组HIV衣壳蛋白p24（义翘神州）和HIV-1 p24 ELISA配对抗体对，开发了一种基于金纳米棒（AuNR）的微流控集成多色免疫传感器，用于通过患者血清样本检测HIV-1 p24。

Their study demonstrated that increased levels of HIV-1 p24 are detectable within 1-2 weeks after infection (Figure 2).

他们的研究表明，在感染后1-2周内可检测到HIV-1 p24水平的升高（图2）。

In another study, McKendry, R., and collaborators developed novel nanobodies to detect HIV-1 p24. They assessed these nanobodies' ability to detect multiple p24 subtypes using an indirect enzyme-linked immunosorbent assay (ELISA) with purified recombinant HIV-1 p24 proteins, including Group M subtype D, as well as Groups N and O (Sino Biological) (Figure 3) 2..

在另一项研究中，McKendry, R.及其合作者开发了新型纳米抗体来检测HIV-1 p24。他们使用间接酶联免疫吸附测定（ELISA）评估了这些纳米抗体检测多种p24亚型的能力，使用了纯化的重组HIV-1 p24蛋白，包括M组亚型D以及N组和O组（义翘神州）（图3）2。

Additionally, Li, L., and coworkers discovered that a glycosylated dihydrochalcone, trilobatin, inhibits HIV-1 entry by blocking the gp41 pocket-forming site. They further evaluated the possible mechanisms of action in gp120-mediated HIV-1 entry and found that trilobatin did not bind to the gp120 envelope.

此外，李莉及其同事发现一种糖基化的二氢查尔酮——三叶苷，通过阻断gp41口袋形成位点来抑制HIV-1的进入。他们进一步评估了在gp120介导的HIV-1进入过程中可能的作用机制，发现三叶苷并未与gp120包膜结合。

In contrast, the positive control, HP-OVA, bound to HIV gp120 (Sino Biological) in an ELISA assay (Figure 4)3..

相比之下，阳性对照 HP-OVA 在 ELISA 检测中与 HIV gp120（义翘神州）结合（图 4）。

Figure 2.

图2。

(B) UV-visible spectra of etched AuNRs for detecting 0-16 ng/mL HIV-1 p24. (C) Linear relationship between ∆λ and HIV-1 p24 concentration (R²=0.967). (D) Analytical results of HIV-1 p24 in serum samples.

(B) 用于检测0-16 ng/mL HIV-1 p24的蚀刻AuNRs的紫外可见光谱。 (C) ∆λ与HIV-1 p24浓度之间的线性关系（R²=0.967）。 (D) 血清样品中HIV-1 p24的分析结果。

DOI: 10.1021/acs.analchem.0c02091

数字对象标识符：10.1021/acs.analchem.0c02091

Figure 3

图3

. Comparison of binding of different p24 subtypes by four nanobodies and two p24-binding mAbs. Results from an indirect ELISA for Group M subtype D, Group N, and O (NDK, 06CM-U14296, BCF06; Sino Biological) with nanobodies 59H10, 37E7, 59H4, LAB5, and mAbs NIH-3537, Capricorn HIV-1/2 (CP-HIV-1/2).

. 四种纳米抗体和两种p24结合单克隆抗体对不同p24亚型结合的比较。通过间接ELISA检测M组D亚型、N组和O组（NDK、06CM-U14296、BCF06；义翘神州）与纳米抗体59H10、37E7、59H4、LAB5及单克隆抗体NIH-3537、Capricorn HIV-1/2（CP-HIV-1/2）的结果。

DOI: 10.1021/acsinfecdis.6b00189

数字对象标识符：10.1021/acsinfecdis.6b00189

Figure 4.

图4。

Inhibitory activities of trilobatin against HIV-1 gp120 (Sino Biological). HP-OVA served as a positive control.

三叶苷对HIV-1 gp120的抑制活性（Sino Biological）。HP-OVA作为阳性对照。

DOI: 10.1002/1873-3468.13113

DOI：10.1002/1873-3468.13113

Sino Biological is dedicated to fostering collaborations that drive impactful breakthroughs in HIV and other viral research. Leveraging our high-quality reagents and cutting-edge technologies, we are committed to supporting your scientific endeavors. For more information on our virus-related solutions, please visit our website: https://www.sinobiological.com..

义翘神州致力于推动在艾滋病和其他病毒研究领域产生重大突破的合作。利用我们高质量的试剂和前沿技术，我们全力支持您的科学研究。欲了解我们与病毒相关的解决方案的更多信息，请访问我们的网站：https://www.sinobiological.com。

References

参考文献

1. Liu, D. et al. Microfluidic-Integrated Multicolor Immunosensor for Visual Detection of HIV-1 p24 Antigen with the Naked Eye. Anal Chem 92, 11826–11833 (2020).

1. 刘, D. 等. 用于肉眼可视化检测 HIV-1 p24 抗原的微流控多色免疫传感器. 分析化学 92, 11826–11833 (2020).

2. Gray, E. R. et al. Unravelling the Molecular Basis of High Affinity Nanobodies against HIV p24: In Vitro Functional, Structural, and in Silico Insights. ACS Infect Dis 3, 479–491 (2017).

2. Gray, E. R. 等。揭示针对 HIV p24 的高亲和力纳米抗体的分子基础：体外功能、结构和计算机模拟洞察。ACS Infect Dis 3，479–491（2017）。

3. Yin, S. et al. Trilobatin as an HIV ‐1 entry inhibitor targeting the HIV ‐1 Gp41 envelope. FEBS Lett 592, 2361–2377 (2018)

3. 尹，S. 等。Trilobatin 作为 HIV-1 入侵抑制剂靶向 HIV-1 Gp41 包膜。《FEBS通讯》592卷，2361–2377页（2018年）