Results illustrate ViiV Healthcare’s pipeline is generating multiple options for the development of new ultra long-acting HIV regimens

结果表明，ViiV Healthcare的管道正在为开发新的超长效HIV治疗方案生成多种选择。

VH4524184 (VH184), a potent, investigational third-generation integrase inhibitor (INSTI), demonstrates strong antiviral activity and positive safety results across multiple dose levels in people with HIV-1, supporting further development as a long-acting injectable antiretroviral

VH4524184（VH184）是一种强效的第三代研究性整合酶抑制剂（INSTI），在HIV-1感染者中展示了强大的抗病毒活性和良好的安全性，支持其作为长效注射抗逆转录病毒药物的进一步开发。

VH4011499 (VH499), a promising, highly potent investigational capsid inhibitor, shows positive antiviral activity and good safety findings for treatment of HIV-1, supporting further development as a long-acting antiretroviral

VH4011499（VH499）是一种前景广阔、高效力的研究性衣壳抑制剂，显示出积极的抗病毒活性和良好的安全性，支持其作为长效抗逆转录病毒药物进一步开发以治疗HIV-1。

ViiV Healthcare, the global specialist HIV company majority owned by GSK, with Pfizer and Shionogi as shareholders, today announced positive findings from two phase IIa proof-of-concept studies of investigational antiretroviral therapies VH4524184 (VH184) and VH4011499 (VH499). These findings, presented at the Conference on Retroviruses and Opportunistic Infections (CROI 2025) in San Francisco, U.S., support the continued development of these two compounds as distinct options for a new generation of long-acting injectables for HIV, with the potential for extended dosing intervals..

ViiV Healthcare是一家由GSK控股、辉瑞和盐野义制药参股的全球性HIV专业公司，今天宣布了两项IIa期概念验证研究的积极结果，涉及在研抗逆转录病毒疗法VH4524184（VH184）和VH4011499（VH499）。这些研究结果在美国旧金山举行的2025年逆转录病毒与机会性感染会议（CROI 2025）上公布，支持继续开发这两种化合物，作为新一代长效HIV注射剂的不同选择，有望实现更长的给药间隔。

Kimberly Smith, M.D., MPH, Head of Research & Development at ViiV Healthcare said

ViiV Healthcare研发部门负责人Kimberly Smith医学博士、公共卫生硕士表示

: “It’s clear long-acting injectable medicines deliver on unmet patient need and will play a critical role in achieving our ambition of ending HIV and AIDS. Our pipeline with INSTIs at the core showcases our continued leadership in long-acting injectable innovation. Data shows that the potency and tolerability of our third-generation INSTI and our capsid inhibitor will make them a major part in the development of our next generation of long-acting injectable therapies.”.

“很明显，长效注射药物满足了患者的未满足需求，并将在实现我们终结艾滋病毒和艾滋病的目标中发挥关键作用。我们以整合酶抑制剂为核心的产品线展示了我们在长效注射创新方面的持续领导地位。数据表明，我们的第三代整合酶抑制剂和衣壳抑制剂的效力和耐受性将使它们在开发下一代长效注射疗法中占据重要地位。”

VH184 demonstrated high antiviral potency

VH184表现出高效的抗病毒能力

1

1

This study aimed to explore the antiviral activity and safety of three doses of VH184 (10mg, 50mg and 300mg taken once every three days) by assessing the maximum change in plasma HIV-1 RNA levels during a 10-day monotherapy period in 22 adults who had not previously received antiretroviral therapy. People who participated in the study had HIV-1 RNA levels of at least 3000 copies/mL..

本研究旨在通过评估22名既往未接受过抗逆转录病毒治疗的成人在10天单药治疗期间血浆HIV-1 RNA水平的最大变化，来探索三种剂量（10mg、50mg和300mg，每三天服用一次）的VH184的抗病毒活性和安全性。参与研究的人群其HIV-1 RNA水平至少为3000拷贝/mL。

VH184, a third-generation INSTI, demonstrated potency at all doses leading to a marked drop in the HIV-1 viral load. After 10 days of monotherapy, the average decreases were -1.17, -2.15, and -2.31 log10 copies/mL for the 10mg, 50mg, and 300mg doses, respectively. The maximum viral load decline (-2.69 log10) was observed in the 300mg dose.

VH184是一种第三代INSTI，在所有剂量下均显示出效力，导致HIV-1病毒载量显著下降。在10天的单药治疗后，10mg、50mg和300mg剂量的平均降幅分别为-1.17、-2.15和-2.31 log10拷贝/mL。最大病毒载量下降（-2.69 log10）出现在300mg剂量组。

Additionally, no drug resistance mutations were observed at the end of the study. All side effects were mild to moderate, and no serious side effects or participant discontinuations occurred..

此外，在研究结束时未观察到任何耐药性突变。所有副作用均为轻度至中度，未出现严重副作用或参与者退出的情况。

Long-acting formulations of VH184 in adults without HIV are being evaluated in an ongoing phase 1 study (

正在进行的 1 期研究中，正在评估成人中不含 HIV 的 VH184 长效制剂 (

NCT06310551

NCT06310551

). The findings of this trial support further development of VH184 as a potential long-acting injectable antiretroviral.

）。该试验的结果支持进一步开发VH184作为一种潜在的长效注射抗逆转录病毒药物。

Higher VH499 dose correlated with greater decline in viral load

更高剂量的VH499与病毒载量的更大下降相关

2

2

This study evaluated the compound’s antiviral effect, safety, and tolerability by assessing the maximum change in plasma HIV-1 RNA levels from baseline through day 11 in 23 adults who had not previously received antiretroviral therapy. People who participated in the study also had HIV-1 RNA levels of at least 3000 copies/mL..

本研究通过评估 23 名既往未接受过抗逆转录病毒治疗的成人在第 11 天时血浆 HIV-1 RNA 水平从基线开始的最大变化，评估了该化合物的抗病毒效果、安全性和耐受性。参与研究的人群其 HIV-1 RNA 水平还至少达到 3000 拷贝/mL。

The trial of VH499, an investigational capsid inhibitor, showed that all oral doses (25mg, 100mg, and 250mg) led to a decrease in HIV-1 viral load ranging from -2.2 log 10 copies/mL in the 250mg arm, to -1.8 log10 copies/mL in the 25mg and 100mg arms. VH499 was well tolerated with all adverse events being mild to moderate in severity.

VH499（一种研究性衣壳抑制剂）的试验表明，所有口服剂量（25mg、100mg 和 250mg）均导致 HIV-1 病毒载量下降，其中 250mg 组下降了 -2.2 log10 拷贝/mL，而 25mg 和 100mg 组下降了 -1.8 log10 拷贝/mL。VH499 耐受性良好，所有不良事件的严重程度均为轻度至中度。

There were no adverse events leading to withdrawal and no serious adverse events were reported. On day 11, one individual on the 25mg dose developed a single mutation associated with reduced susceptibility to capsid inhibitors. .

没有发生导致退出的不良事件，也没有报告严重的不良事件。在第11天，一名接受25毫克剂量的个体出现了一个与衣壳抑制剂敏感性降低相关的单一突变。

In a previous phase I clinical trial of adults without HIV-1, VH499 was well- tolerated, and showed no induction or inhibition of CYP3A4.

在之前未感染HIV-1的成年人I期临床试验中，VH499耐受性良好，且未显示对CYP3A4的诱导或抑制作用。

3

3

Long-acting formulations of VH499 in adults without HIV are being evaluated in ongoing phase 1 studies (

正在持续进行的1期研究中评估VH499的长效制剂在未感染HIV的成人中的效果 (

NCT06012136

NCT06012136

;

；

NCT06724640

NCT06724640

).

）。

These findings, in combination with the potent antiviral activity in this phase IIa study, support further development of VH499 as a potential long-acting antiretroviral for HIV treatment.

这些发现，再加上这项 IIa 期研究中表现出的有效抗病毒活性，支持进一步开发 VH499 作为一种潜在的长效抗逆转录病毒药物用于 HIV 治疗。

About ViiV Healthcare

关于ViiV Healthcare

ViiV Healthcare is a global specialist HIV company established in November 2009 by GSK (LSE: GSK) and Pfizer (NYSE: PFE) dedicated to delivering advances in treatment and care for people living with HIV and for people who could benefit from HIV prevention. Shionogi became a ViiV shareholder in October 2012.

ViiV Healthcare 是一家全球专业的 HIV 公司，由葛兰素史克（GSK，伦敦证交所：GSK）和辉瑞（Pfizer，纽约证交所：PFE）于 2009 年 11 月成立，致力于为 HIV 感染者及可能受益于 HIV 预防的人群提供治疗和护理的进步。盐野义制药于 2012 年 10 月成为 ViiV 的股东。

The company’s aims are to take a deeper and broader interest in HIV and AIDS than any company has done before and take a new approach to deliver effective and innovative medicines for HIV treatment and prevention, as well as support communities affected by HIV. For more information on the company, its management, portfolio, pipeline, and commitment, please visit viivhealthcare.com. .

该公司的目标是比任何公司都更深入、更广泛地关注艾滋病和艾滋病毒，并采取新的方法，提供有效且创新的艾滋病治疗和预防药物，同时支持受艾滋病影响的社区。如需了解更多关于该公司、其管理团队、产品组合、研发进展和承诺的信息，请访问viivhealthcare.com。

About GSK

关于GSK

GSK is a global biopharma company with a purpose to unite science, technology, and talent to get ahead of disease together. Find out more at gsk.com.

GSK是一家全球生物制药公司，致力于联合科学、技术和人才，共同战胜疾病。欲了解更多信息，请访问gsk.com。

Cautionary statement regarding forward-looking statements

关于前瞻性陈述的谨慎声明

GSK cautions investors that any forward-looking statements or projections made by GSK, including those made in this announcement, are subject to risks and uncertainties that may cause actual results to differ materially from those projected. Such factors include, but are not limited to, those described under Item 3.D “Risk factors” in GSK’s Annual Report on Form 20-F for 2024..

GSK提醒投资者，GSK所做的任何前瞻性声明或预测，包括本公告中所包含的内容，均受到可能导致实际结果与预测结果存在重大差异的风险和不确定性的影响。这些因素包括但不限于GSK 2024年Form 20-F年度报告中第3.D项“风险因素”下所述的内容。

References

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等

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VH4524184（VH-184）的第三代表观遗传链转移抑制剂的概念验证试验。于2025年3月9日至12日在加利福尼亚州旧金山举行的逆转录病毒和机会性感染会议（CROI 2025）上发表。

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VH4011499（VH-499）口服新型HIV-1衣壳抑制剂的概念验证试验。于2025年3月9日至12日在美国加利福尼亚州旧金山举行的逆转录病毒和机会性感染会议（CROI 2025）上发表。

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