预约演示
更新于：2026-09-07
Doravirine/Islatravir
多拉韦林/伊拉曲韦
更新于：2026-09-07
概要
基本信息
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2026-03-06), |
最高研发阶段(中国)申请上市 |
特殊审评优先审评 (中国) |
登录后查看时间轴
结构/序列
分子式C12H12FN5O3 |
InChIKeyIKKXOSBHLYMWAE-QRPMWFLTSA-N |
CAS号865363-93-5 |
查看全部结构式(2)
关联
11
项与 多拉韦林/伊拉曲韦 相关的临床试验NCT07086079
A Clinical Study to Evaluate the Breast Milk and Plasma Pharmacokinetics of MK-8591A in Healthy Lactating Female Participants
The goal of this study is to learn what happens to doravirine (DOR) and islatravir (ISL) in a healthy lactating female's body over time. Researchers want to learn if DOR and ISL are in breast milk.
开始日期2025-09-26 |
申办/合作机构 |
NCT06719570
An Open-Label Study to Evaluate the Effect of a High-Fat Meal on the Pharmacokinetics of Doravirine/Islatravir (100 mg/0.25 mg) Fixed-dose Combination Tablet and to Compare the Pharmacokinetics of Doravirine/Islatravir to Doravirine and Islatravir Single Entities in Healthy Adult Participants
The purpose of this study is to learn what happens to MK-8591A in a person's body over time. Researchers will compare what happens to MK-8591A in the body when it is given with and without food.
开始日期2024-01-23 |
申办/合作机构 |
NCT05766501
A Phase 3 Open-label Clinical Study of Doravirine/Islatravir (DOR/ISL [100 mg/0.25 mg]) Once Daily for the Treatment of HIV-1 Infection in Participants Who Previously Received DOR/ISL (100 mg/0.75 mg) QD in a Phase 3 Clinical Study
The purpose of this study is to evaluate the safety and tolerability of DOR/ISL in adult participants with HIV-1 who had been previously treated with DOR/ISL in earlier clinical studies. There are no formal hypotheses to be tested in this study.
开始日期2023-03-17 |
申办/合作机构 |
100 项与 多拉韦林/伊拉曲韦 相关的临床结果
登录后查看更多信息
100 项与 多拉韦林/伊拉曲韦 相关的转化医学
登录后查看更多信息
100 项与 多拉韦林/伊拉曲韦 相关的专利（医药）
登录后查看更多信息
5
项与 多拉韦林/伊拉曲韦 相关的文献（医药）2026-07-01·Lancet HIV
Fixed-dose daily doravirine (100 mg) with islatravir (0·25 mg) versus bictegravir, emtricitabine, and tenofovir alafenamide for initial HIV-1 therapy: 48-week results of a phase 3, randomised, controlled, double-blind, non-inferiority trial
Article
作者: Diamond, Tracy L ; Fox, Michelle C ; Avihingsanon, Anchalee ; Vesnesky, Mary ; Sinclair, Gary ; Paredes, Roger ; Klopfer, Stephanie O ; Gatanaga, Hiroyuki ; Pisculli, Mary L ; Rockstroh, Jürgen K ; Bettacchi, Christopher ; Kassim, Sheetal ; Crabtree Ramírez, Brenda ; Molina, Jean-Michel ; Stamm, Luisa M ; Mugo, Nelly ; Xu, Yayun
BACKGROUND:
Doravirine and islatravir is a two-drug regimen being investigated for the treatment of HIV-1. This study evaluated efficacy and safety of once daily doravirine and islatravir versus bictegravir, emtricitabine, and tenofovir alafenamide in adults with HIV-1 who were treatment-naive.
METHODS:
MK-8591A-053 is a phase 3, randomised, double-blind, active-controlled, non-inferiority study being done at 116 research, community, and hospital-based clinics across 20 countries. Adults aged at least 18 years with HIV-1 RNA of 500 copies per mL or more never previously treated for HIV-1 were randomly assigned (1:1), stratified by screening HIV-1 RNA viral load and CD4-cell count, to received either doravirine (100 mg) and islatravir (0·25 mg) or bictegravir (50 mg), emtricitabine (200 mg), and tenofovir alafenamide (25 mg) orally once daily. The primary endpoint was percentage of participants with HIV-1 RNA less than 50 copies per mL at week 48 (FDA snapshot; prespecified non-inferiority margin -10%). Participants who received at least one dose of study intervention were analysed for safety. This trial is ongoing and is registered with ClinicalTrials.govNCT05705349.
FINDINGS:
We screened 756 participants for eligibility between March 8, 2023, and Oct 11, 2024. 269 participants were treated with doravirine-islatravir and 267 with bictegravir-emtricitabine-tenofovir. The last study visit for this analysis occurred on Oct 13, 2025. Median age was 32 years (IQR 26-40), 134 (25%) participants were assigned female at birth, 225 (42%) were White, 92 (17%) had CD4 counts less than 200 cells per μL, 197 (37%) had an HIV-1 RNA greater than 100 000 copies per mL, and 314 (59%) had pre-existing resistance-associated mutations. At week 48, doravirine-islatravir was non-inferior to bictegravir-emtricitabine-tenofovir: 247 (91·8%) of 269 versus 242 (90·6%) of 267 had HIV-1 RNA less than 50 copies per mL (estimated difference 1·2%, 95% CI -3·7 to 6·2). Mean increase in CD4 count was 218 cells per μL in the doravirine-islatravir group and 226 cells per μL in the bictegravir-emtricitabine-tenofovir group (estimated difference -6·8, 95% CI -35·8 to 22·2). Two participants in the doravirine-islatravir group and one in the bictegravir-emtricitabine-tenofovir group with pretreatment HIV-1 RNA greater than 1 million copies per mL and CD4 counts less than 200 cells per μL acquired treatment-emergent mutations. Phenotypic analysis revealed resistance to doravirine in two participants treated with doravirine-islatravir. 38 (14%) of 269 participants in the doravirine-islatravir group and 48 (18%) of 267 in the bictegravir-emtricitabine-tenofovir group had treatment-related adverse events: the most common were increased weight (7, 3%), headache (6, 2%), and dizziness (5, 2%) in the doravirine-islatravir group and increased weight (9, 3%), headache (9, 3%), and decreased estimated glomerular filtration rate (8, 3%) in the bictegravir-emtricitabine-tenofovir group.
INTERPRETATION:
Doravirine (100 mg) and islatravir (0·25 mg) is a two-drug, once daily regimen with efficacy and safety similar to bictegravir (50 mg), emtricitabine (200 mg), and tenofovir alafenamide (25 mg) for initial treatment of HIV-1, which could provide an option for treatment without an integrase strand transfer inhibitor.
FUNDING:
Merck Sharp & Dohme, a subsidiary of Merck & Co.
2026-02-01·LANCET
Switch to fixed-dose doravirine (100 mg) and islatravir (0·25 mg) once daily in virologically suppressed adults with HIV-1 on bictegravir, emtricitabine, and tenofovir alafenamide: 48-week results of a phase 3, multicentre, randomised, controlled, double-blind, non-inferiority trial
Article
作者: Su, Feng-Hsiu ; Colson, Amy E ; Ramgopal, Moti N ; Mills, Anthony M ; Johnson, Margaret ; Katner, Harold P ; Crofoot, Gordon ; Diamond, Tracy L ; Lahoulou, Rima ; Barninger, Erika ; Fox, Michelle C ; Bettacchi, Christopher ; Osiyemi, Olayemi O ; Klopfer, Stephanie O ; Eves, Karen ; Xu, Yayun ; Stamm, Luisa M ; Gatanaga, Hiroyuki ; Hinestrosa, Federico
BACKGROUND:
The combination of doravirine and islatravir is under investigation as a fixed-dose, single-tablet regimen for the treatment of HIV-1. We aimed to assess the efficacy and safety of switching to doravirine (100 mg) and islatravir (0·25 mg) from bictegravir, emtricitabine, and tenofovir alafenamide in virologically suppressed adults with HIV-1.
METHODS:
This phase 3, randomised, controlled, double-blind, non-inferiority trial was conducted at 49 research, community, and hospital-based clinics in six countries: Australia, Chile, Israel, Japan, the UK, and the USA. Adults aged 18 years or older with HIV-1, who were virologically suppressed (with a viral load of HIV-1 RNA <50 copies per mL) for at least 3 consecutive months on bictegravir, emtricitabine, and tenofovir alafenamide and had no history of treatment failure or known resistance to doravirine, were eligible for the study. Participants were randomly assigned, in a 2:1 ratio according to a computer-generated randomisation schedule with a block size of three, to switch to oral doravirine (100 mg) and islatravir (0·25 mg) or to continue bictegravir, emtricitabine, and tenofovir alafenamide, once daily. Participants, investigators, study staff, and sponsor personnel were masked to study treatment; sponsor personnel directly involved in this analysis were unmasked at week 48. The primary endpoint, which was assessed in all randomly assigned participants who received at least one dose of study treatment, was the percentage of participants with a viral load of 50 copies per mL or higher at week 48 according to the US Food and Drug Administration snapshot approach; non-inferiority would be concluded if the upper bound of the multiplicity-adjusted 95% CI for the treatment difference was less than 4%. The trial is registered at ClinicalTrials.gov, NCT05630755, and is ongoing but closed to enrolment.
FINDINGS:
Between Feb 17 and Nov 17, 2023, 585 individuals were screened, of whom 514 were randomly assigned and 513 treated: 342 participants were switched to doravirine (100 mg) and islatravir (0·25 mg) and 171 continued bictegravir, emtricitabine, and tenofovir alafenamide. The median age of the 513 participants was 47 years (IQR 37-58), 403 (79%) were assigned male and 110 (21%) were assigned female at birth, 158 (31%) were Black or African American, and 117 (23%) were Hispanic, Latino, or Latina. At week 48, doravirine and islatravir showed non-inferiority to bictegravir, emtricitabine, and tenofovir alafenamide (viral load ≥50 copies per mL in five [1·5%] of 342 vs one [0·6%] of 171 participants) with a treatment difference of 0·9% (multiplicity-adjusted 95% CI -1·9 to 2·9). The rates of adverse events (74·6% [255 of 342 participants] vs 71·3% [122 of 171 participants]; difference 3·2 [95% CI -4·7 to 11·6]), treatment-related adverse events (10·2% [35] vs 9·4% [16]; 0·9 [-5·1 to 6·0]), serious adverse events (4·4% [15] vs 6·4% [11]; -2·0 [-7·1 to 1·9]), and discontinuations due to adverse events (2·9% [ten] vs 1·8% [three]; 1·2 [-2·3 to 3·9]) were similar in the doravirine and islatravir group and the bictegravir, emtricitabine, and tenofovir alafenamide group, and no deaths were reported.
INTERPRETATION:
The combination of doravirine (100 mg) and islatravir (0·25 mg) has similar efficacy and safety profiles to bictegravir, emtricitabine, and tenofovir alafenamide, and could provide a two-drug, once daily, oral single-tablet option without an integrase strand-transfer inhibitor for adults who are virologically suppressed and want to switch to a different ART regimen.
FUNDING:
Merck Sharp & Dohme, a subsidiary of Merck & Co.
2026-02-01·LANCET
Switch to fixed-dose doravirine (100 mg) and islatravir (0·25 mg) once daily in virologically suppressed adults with HIV-1 on oral antiretroviral therapy: 48-week results of a phase 3, multicentre, randomised, open-label, non-inferiority trial
Article
作者: Grandhi, Anjana ; Jackson, Beth ; Mngqibisa, Rosie ; Kim, Jason ; Bloch, Mark ; Diamond, Tracy L ; Tebas, Pablo ; Braun, Dominique L ; Fuszard, Monica ; Orkin, Chloe ; Fox, Michelle C ; Kumar, Princy ; Eves, Karen ; Walmsley, Sharon ; Klopfer, Stephanie O ; Carr, Andrew ; Stamm, Luisa M ; Velez, Juan Diego ; Yokomaku, Yoshiyuki
BACKGROUND:
Doravirine and islatravir is an investigational, once-daily, single-tablet regimen containing two potent antiretrovirals with complementary mechanisms of action and resistance profiles. We aimed to evaluate the efficacy and safety of switching from stable, oral antiretroviral therapy (ART) to the fixed combination of doravirine (100 mg) and islatravir (0·25 mg) in virologically suppressed adults living with HIV-1.
METHODS:
This phase 3, randomised, active-controlled, open-label, non-inferiority trial was conducted at 53 research, community, and hospital-based clinics in eight countries: Australia, Canada, Colombia, Japan, South Africa, Switzerland, the UK, and the USA. Adults (aged ≥18 years) with a viral load of fewer than 50 copies of HIV-1 RNA per mL on any oral, two-drug or three-drug ART regimen for at least 3 months, with no history of treatment failure, known resistance to doravirine, or active hepatitis B infection, were randomly assigned (2:1) according to a computer-generated randomisation schedule (block size three) to receive oral doravirine (100 mg) and islatravir (0·25 mg) once daily or to continue baseline ART for 48 weeks. Randomisation was stratified by the anchor antiretroviral drug class (integrase strand-transfer inhibitor [INSTI], non-nucleoside reverse transcriptase inhibitor, or protease inhibitor) in the baseline regimen. The primary endpoint (assessed in all treated participants) was the percentage of participants with a viral load of 50 copies per mL or higher at week 48 (analysed according to the US Food and Drug Administration snapshot approach); non-inferiority would be concluded if the upper bound of the multiplicity-adjusted 95% CI for the treatment difference was less than 4%. The safety analysis population included all randomly assigned participants who received at least one dose of study treatment. The trial is registered at ClinicalTrials.gov, NCT05631093, and is ongoing but closed to enrolment.
FINDINGS:
Between Feb 20 and Oct 24, 2023, 614 individuals were screened for eligibility, of whom 553 were randomly assigned to receive doravirine and islatravir (n=368) or baseline ART (n=185). 551 participants received at least one dose of allocated medication: 366 in the doravirine and islatravir group and 185 in the baseline ART group. Of these 551 participants, 332 (60%) were assigned male and 219 (40%) were assigned female at birth, and the median age was 51 years (IQR 41-59); 250 (45%) identified as Black or African American and 80 (15%) identified as Hispanic, Latino, or Latina. Doravirine and islatravir showed non-inferiority at week 48, with viral loads of 50 copies per mL or higher in five (1·4%) of 366 participants versus nine (4·9%) of 185 participants on baseline ART (difference -3·6% [multiplicity-adjusted 95% CI -7·8 to -0·8]). Treatment-related adverse events were more common with doravirine and islatravir (44 [12·0%] of 366 participants) than with baseline ART (nine [4·9%] of 185 participants; difference 7·2 [95% CI 2·2 to 11·6]). Rates were similar in the doravirine and islatravir group and the baseline ART group for any adverse event (79·5% [291 of 366 participants] vs 83·8% [155 of 185 participants]; difference -4·3 [-10·7 to 2·8]), serious adverse events (6·3% [23] vs 4·9% [nine]; 1·4 [-3·2 to 5·2]), and discontinuation due to adverse events (0·5% [two] vs 2·2% [four]; -1·6 [-4·9 to 0·2]). One death occurred (in the baseline ART group) and was not considered treatment-related. No participants discontinued treatment as a result of protocol-specified declines in CD4 cell or total lymphocyte counts.
INTERPRETATION:
Doravirine and islatravir is efficacious and well tolerated and would represent the first non-INSTI-based, two-drug regimen for HIV-1 treatment. With increasing concern over the potential development of widespread INSTI resistance, this once-daily, oral, single-tablet regimen could be a potential option for people living with HIV-1 requiring a change to their antiretroviral regimen. The safety and efficacy findings support the ongoing development of islatravir, a drug with long-acting potential.
FUNDING:
Merck Sharp & Dohme, a subsidiary of Merck & Co.
162
项与 多拉韦林/伊拉曲韦 相关的新闻（医药）2026-09-07
·微信
注：本文不构成任何投资意见和建议，以官方/公司公告为准；本文仅作医疗健康相关药物介绍，非治疗方案推荐（若涉及），不代表平台立场。任何文章转载需得到授权。
8月27日，吉利德宣布美国FDA批准了其口服复方单片制剂Bixlenvo，用于治疗病毒学抑制的成人HIV感染者。这是目前HIV治疗领域体积最小的每日一次单片方案，也是首个专门面向那些正在接受复杂多片方案治疗、病毒抑制良好却无法使用现有单片制剂的患者群体所设计的单片方案。
这款产品的获批，瞄准的是那些被主流产品覆盖不到、却又真实存在的患者需求。
下面从几个角度来聊聊这款产品和它背后的行业逻辑。一、产品本身
Bixlenvo把两种抗HIV药物装在了一片药里，一个是比克替拉韦，这是Biktarvy的核心成分之一，属于整合酶链转移抑制剂，耐药屏障高，国内外指南都把它放在推荐列表的前列。另一个是来那帕韦，这是全球首个获批的衣壳抑制剂，作用机制跟现有的抗逆转录病毒药物都不一样，不存在已知的交叉耐药。
把这两个药放在一起做成单片，意味着那些因为既往耐药、不耐受或者药物相互作用而无法使用现有单片方案的患者，现在多了一个选择。吉利德估算，这类患者约占美国HIV感染者总数的5%或以上。这个比例看起来不大，但考虑到美国HIV感染者的基数，这依然是一个不容忽视的群体。
支撑Bixlenvo获批的两项III期临床试验，ARTISTRY-1和ARTISTRY-2。
ARTISTRY-1入组的患者是迄今为止III期注册试验中年龄最大的HIV治疗人群，中位年龄60岁。这些患者的中位治疗史长达28年。28年是什么概念？差不多是上世纪90年代末就开始接受抗病毒治疗了。那时候的HIV治疗方案远没有现在这么方便，很多人经历过早期单药或双药治疗的时代，体内已经累积了不少耐药突变。基线时，这些患者每天要服用2到11片药，约40%的人每天需要服药超过一次。67%的受试者存在核苷逆转录酶抑制剂耐药史，81%因为抗病毒药物耐药而不得不采用复杂的多片方案。
48周的结果显示，Bixlenvo组有0.8%的受试者病毒载量≥50拷贝/mL，继续使用复杂多片方案的对照组是1.1%，这个数据达到了预设的非劣效标准。让这些每天要吃一把药的老患者换成每天一片Bixlenvo，疗效并不比原来差。
ARTISTRY-2的设计思路则不同，它入组的是已经使用Biktarvy治疗至少6个月且病毒抑制良好的患者，一组换成Bixlenvo，另一组继续用Biktarvy。48周时，Bixlenvo组383人中有1.3%达到病毒载量标准，Biktarvy组191人中有1.0%。同样满足非劣效判定。
除了维持病毒抑制，ARTISTRY-1还观察，从复杂多片方案转换到Bixlenvo的患者，总胆固醇中位数降低了15.1 mg/dL，而继续使用复杂方案的对照组反而增加了2.8 mg/dL，患者报告的治疗满意度评分平均提高了7分，ARTISTRY-2则显示，换用Bixlenvo对体重没有显著影响。
安全性方面，Bixlenvo组药物相关不良事件发生率10%，对照组12%。最常见的不良反应是头痛、恶心和腹泻，发生率都不高。整体来看，Bixlenvo的耐受性良好，没有发现新的安全性信号。二、市场定位
Bixlenvo的目标人群，是那些病毒已经抑制、但因为种种原因无法使用现有单片方案的患者。不是让Biktarvy的患者换药，而是去服务那些Biktarvy服务不了的人。
定价方面，Bixlenvo每30天用量的批发价为4595美元，这个价格跟市面上其他每日一次的单片HIV药物基本持平，吉利德还配套了患者援助计划，符合条件的无保险患者可以免费获得药品，有商业保险或私人医保的患者可以获得自付费用补助。
4595美元的价格并不低，但也没有因为是新产品就定得比现有产品高出一截。吉利德的做法更像是把Bixlenvo放进现有的价格体系里，让医生和患者在考虑换药时少一个价格上的顾虑，毕竟对于已经在使用其他单片方案的患者来说，如果价格差不多、疗效相当、副作用可控，多一个选择总是好事。三、从三药到两药
Bixlenvo的获批也反映了HIV治疗领域正在发生的一个趋势性变化，从三药方案向两药方案的迁移。
过去很多年，三药联合治疗是HIV管理的金标准，Biktarvy就是三药方案的代表，把比克替拉韦、恩曲他滨和替诺福韦艾拉酚胺装在了一片药里，三药方案的优势在于疗效确切、耐药屏障高，积累了大量的长期数据。
但HIV感染需要终身治疗。随着患者年龄增长、合并症增多，长期用药的安全性变得越来越重要，少一个药，意味着减少一种药物的长期暴露，降低潜在的药物相互作用风险，对于一些年纪较大、已经在吃多种慢性病药物的患者来说，这个优势是实实在在的。
2025年，三药方案仍占全球HIV市场销售额的52%，但两药方案的份额已经从2021年的22%增长到了29%，少一个药正在成为越来越多人的选择。
GSK旗下的ViiV在两药方案上布局很早，Dovato已经在初治患者中证明非劣效于三药方案，2025年销售额达到45亿美元。Juluca也是两药方案，卖了10亿美元。默沙东的多拉韦林/伊斯拉曲韦组合在2026年3月和4月分别在日本和美国获批。
ARTISTRY-1和ARTISTRY-2证明了，即便是那些治疗史很长、耐药背景复杂的患者，换成两药方案同样能把病毒控制住。这为两药方案的适用范围提供了一个新的证据。四、Biktarvy之后怎么办
Biktarvy是吉利德HIV业务的核心，2025年全年销售额143亿美元，同比增长7%，在美国治疗市场保持着超过52%的份额。但任何产品都有生命周期，Biktarvy的专利预计在2030年代中期到期。专利悬崖是每一个制药公司都要面对的问题，吉利德也不例外。
吉利德公司的目标是为HIV治疗和预防提供多种选择，Bixlenvo就是这种思路下的产物。
吉利德还规划到2033年推出7款新的HIV治疗和预防产品。围绕来那帕韦，吉利德正在开发多种给药方式，包括每日口服药、每周口服方案和长效注射剂。用不同的产品覆盖不同的患者需求，延长整个HIV franchise的生命周期。
Bixlenvo在这个战略中不跟Biktarvy争初治患者，也不抢Biktarvy的存量市场，去服务那些Biktarvy覆盖不到的人。这种差异化定位既避免了自家产品之间的内耗，又扩大了整体的市场覆盖。五、口服STR、长效注射与PrEP的三线交锋
HIV治疗领域的竞争正在变得越来越多元。
口服端，Bixlenvo要面对的是Biktarvy和ViiV的Dovato这些已经站稳脚跟的产品，Bixlenvo的优势在于它是首个针对复杂用药人群的单片方案，在这个细分市场有先发优势。但默沙东的Idvynso同样是一款每日一次的两药单片，2026年4月在美国获批，口服STR赛道的玩家越来越多，竞争只会更加激烈。
长效注射端，ViiV的Cabenuva是每月一次或每两个月一次的注射方案。在III期试验中，Cabenuva已经证明优于每日口服方案，对于那些不愿意每天吃药的患者来说，长效注射是一个很有吸引力的选择，GSK还在开发每年两次给药的在研药物。
预防端，来那帕韦作为半年一次的PrEP注射剂在2025年6月获批，吉利德的PrEP业务整体在2026年第二季度首次突破单季10亿美元。FDA已经受理了Yeztugo每周一次口服PrEP方案的补充新药申请，PDUFA日期定在2027年2月。
HIV市场正在从一个以口服每日一次方案为主的市场，变成一个口服、长效注射、PrEP多种形态并存的市场。Bixlenvo在口服端站稳脚跟，来那帕韦在预防端攻城略地，吉利德的产品组合正在变得越来越立体。
Bixlenvo不是那种颠覆性创新的产品，来那帕韦之前已经获批用于多重耐药患者的治疗，比克替拉韦更是用了很多年的老面孔。但把这两个药做成单片、专门面向复杂用药人群，这个思路本身是有价值的。
HIV治疗走到今天，大的技术突破越来越难，更多的时候是在做精细化的工作，把已有的工具组合得更好用、覆盖更多的人群、解决更具体的问题。
参考来源：
[1]Gilead Sciences. U.S. FDA Approves Gilead's Bixlenvo™, a New Once-Daily Single Tablet Option for Virologically Suppressed Adults With HIV, Including Those on Complex Regimens. Business Wire.
[2]FDA Approves Bixlenvo for HIV-1 Switch Therapy in Virologically Suppressed Adults. Patient Care Online.
[3]吉利德HIV双药单片复方Bixlenvo获FDA批准上市. 摩熵医药 .
[4]ARTISTRY-1: Phase 3 Trial of Bictegravir/Lenacapavir in Virologically Suppressed Adults with HIV-1.
[5]ARTISTRY-2: Phase 3 Trial of Bictegravir/Lenacapavir versus Biktarvy in Virologically Suppressed Adults with HIV-1..
[6]Gilead data show investigational HIV combination maintains viral suppression. PharmaTimes.
[7]吉利德科学2025年净利润同比增长近17倍 HIV预防需求强劲增长. 证券时报.
[8]Gilead Sciences Fourth Quarter 2025 Prepared Remarks.
[9]2026 HIV治疗两药方案与依从性研究：2DR份额升至29%，简化治疗成主流.
[10]FDA approves daily HIV pill from Gilead designed to simplify treatment for some patients.
[11]FDA Approves Once-Daily Idvynso Tablet for Treating HIV. Drugs.com.
临床3期
2026-08-28
The US FDA has approved Bixlenvo (bictegravir 75 mg/lenacapavir 50 mg), a once-daily single-tablet regimen (STR) for HIV-1 treatment in virologically suppressed adults — including, for the first time, those on complex multi-tablet regimens who could not previously use an STR. Gilead Sciences (Nasdaq: GILD) said the combination is the smallest oral STR and the first approved STR option for virologically suppressed patients on complex regimens who are unable to use existing STRs because of factors including historical resistance or tolerability.
Bixlenvo is indicated as a complete regimen for adults with HIV-1 RNA below 50 copies per mL on a stable antiretroviral regimen, with no known or suspected resistance to either component. Initiation requires a two-day loading period with Sunlenca (lenacapavir) co-administered alongside Bixlenvo, after which Bixlenvo is taken alone once daily. Contraindications include co-administration with dofetilide and strong CYP3A inducers.
Approval rested on two Phase III trials — ARTISTRY-1 (NCT05502341) and ARTISTRY-2 (NCT06333808) — both evaluating virologic suppression maintenance at Week 48 after switching to Bixlenvo. ARTISTRY-1 enrolled a notably treatment-experienced population: median age 60 years, median 28 years on antiretroviral therapy, 67% with nucleoside reverse transcriptase inhibitor (NRTI) resistance, and 81% on complex regimens due to resistance. Both trials reported comparable efficacy to prior regimens and no new safety signals; the most common adverse reactions were headache (4%), nausea (3%), and diarrhea (2%). ARTISTRY-1 results were published in The Lancet and ARTISTRY-2 in Lancet HIV.
Bictegravir is an integrase strand transfer inhibitor (INSTI) that blocks insertion of viral cDNA into the host genome. Lenacapavir, a first-in-class capsid inhibitor also marketed as Sunlenca, disrupts capsid-dependent processes across multiple stages of the HIV lifecycle — nuclear import, uncoating, and virion assembly — with no cross-resistance to other approved antiretroviral classes.
The approval adds another option to an increasingly competitive HIV switch market that includes ViiV Healthcare's Dovato (dolutegravir/lamivudine), long-acting injectable Cabenuva (cabotegravir/rilpivirine), and Merck's recently approved Idvynso (doravirine/islatravir). Bixlenvo is differentiated by its ability to simplify treatment for some heavily treatment-experienced patients currently requiring complex multi-tablet regimens.
Spot something wrong? Report an issue with this article
临床3期上市批准临床结果临床研究寡核苷酸
2026-08-10
·珐成浩鑫
NEWS（8.3-8.7）
////
【P村情报】是珐成浩鑫诚意推出的资讯板块。我们汇总生物医药行业一周的重要新闻，帮助各位看官梳理热点、把握趋势，了解行业最新动向。
8/3
■ 全球首个，罗氏眼科IL-6单抗拟纳入优先审评
CDE网站显示，罗氏的伐米奇拜单抗（vamikibart）拟纳入优先审评，用于治疗葡萄膜炎性黄斑水肿（UME）。伐米奇拜单抗是罗氏自Sesen Bio（已被Carisma Therapeutics收购）引进的一款IL-6单抗，具有较长的玻璃体内滞留时间和较快的系统性清除速度。该药物结合、阻断IL-6信号的活性是托珠单抗的1000倍。
■ 诺华重磅核药再获批准
诺华宣布Pluvicto（镥[177Lu]特昔维匹肽）的新适应症获得FDA批准，用于前列腺特异性膜抗原阳性（PSMA+）转移性雄激素途径调节-未敏感型（mAPMN/S）前列腺癌（以前称为激素敏感性前列腺癌）患者。至此，Pluvicto目前可用于所有阶段的PSMA+转移性前列腺癌患者，适用人群几乎翻倍。
■ 中国生物制药BCL-2抑制剂申报上市CDE网站显示，中国生物制药旗下公司正大天晴的TQB3909地基上市申请，用于治疗既往经过至少包含BTK抑制剂在内的一种系统治疗的成人慢性淋巴细胞白血病/小淋巴细胞性淋巴瘤（CLL/SLL）。TQB3909是正大天晴自主研发的一款高效、口服生物利用度高的选择性BCL-2抑制剂，于2021年进入临床阶段。BCL-2家族蛋白可以通过阻止线粒体外膜通透化（MOMP）从而抑制肿瘤细胞凋亡，其过表达与癌症的耐药性的形成密切相关。通过抑制BCL-2与促凋亡蛋白（如BAK）的结合，抑制BCL-2依赖性肿瘤的生长，从而发挥抗肿瘤的作用。
8/4
■ 20.93亿美元，康宁杰瑞FIC新药授权出海康宁杰瑞宣布其全资子公司江苏康宁杰瑞与Pathos AI就康宁杰瑞自主研发的同类首创（First-in-class, FIC）新药TROP2/HER3双特异性抗体偶联药物（ADC）JSKN016达成授权许可协议。JSKN016是康宁杰瑞利用单域抗体、双抗及糖基定点偶联平台自主研发的靶向TROP2/HER3双抗ADC。该药物通过糖基定点偶联获得DAR4的均一结构，实现高稳定性与低脱靶毒性。在作用机制上一方面可以精准结合肿瘤细胞表面受体，阻断致癌信号通路；另一方面定点释放拓扑异构酶Ⅰ抑制剂，高效杀伤肿瘤。JSKN016已在多种实体瘤中展现出良好的抗肿瘤活性和安全性，目前已开展JSKN016单药和联合疗法治疗肺癌、乳腺癌等的多项Ⅱ期临床研究，治疗三阴性乳腺癌的Ⅲ期临床研究正在进行中。■ 14mg口服司美格鲁肽在华获批新适应症诺和诺德在发布上半年业绩时披露了司美格鲁肽口服片剂的三项重要进展。基于ESSENCE研究，已在美国递交25mg司美格鲁肽口服片剂（Wegovy pill）用于治疗代谢障碍相关脂肪性肝炎（MASH）的上市申请，预计在2027年一季度迎来审批决定。此前，2.4mg司美格鲁肽注射液（Wegovy）于2025年8月基于ESSENCE研究获得FDA批准MASH适应症。在ESSENCE研究中，2.4mg司美格鲁肽注射液组和安慰剂组实现肝纤维化改善且脂肪性肝炎没有恶化的患者比例分别为36.8%和22.4%（P<0.001），实现脂肪性肝炎得到缓解且肝纤维化没有恶化的患者比例分别为62.9%和34.3%（P<0.001）。该注射液已在中国申报MASH适应症。已向FDA递交25mg司美格鲁肽口服片剂（Ozempic pill）用于治疗2型糖尿病的上市申请，预计在今年四季度迎来审批决定。
■ 全球首个埃博拉病毒mRNA疫苗启动临床试验
Moderna宣布其针对布本迪布焦埃博拉病毒（Bundibugyo ebolavirus，BDBV）的mRNA疫苗mRNA-1469已在加拿大启动I期临床试验，首批受试者已完成接种。目前，已有疫苗主要针对扎伊尔埃博拉病毒（Zaire ebolavirus），但尚无获批疫苗可预防BDBV引起的埃博拉病毒病。mRNA-1469是全球首个进入临床阶段的埃博拉mRNA疫苗。
8/5
■ 武田FIC新药在美国获批上市
武田宣布奥普雷顿（oveporexton，英文商品名：Orzeyful，中文商品名：奥泽悦）获得FDA批准用于治疗1型发作性睡病。该药物已于今年7月在国内获批上市，是全球首个获批的食欲素2型受体（OX2R）激动剂。奥普雷顿可选择性地刺激OX2R以恢复其信号传导，并改善因食欲素缺乏而导致的1型发作性睡病。
■ 默沙东HIV-1新药在华申报上市
CDE网站显示，默沙东的多拉韦林伊拉曲韦片（doravirine/islatravir，英文商品名：Idvynso）在华申报上市。根据优先审评进度，本次申报的适应症为：作为治疗成人HIV-1感染的完整双药治疗方案，适用于正接受稳定抗逆转录病毒治疗方案达到病毒学抑制（HIV-1 RNA<50拷贝/ml）、无抗病毒治疗失败史且无已知与多拉韦林耐药相关突变的患者，替代其当前的抗逆转录病毒治疗方案。
■ 石药与阿斯利康成立合资公司石药集团发布公告，已与阿斯利康签署协议，双方共同设立合资公司，于石家庄高新区建设新一代生物制剂生产基地，标志双方合作从管线授权研发延伸至全球化生产制造领域。根据股权安排，石药集团持股51%，阿斯利康持股49%，双方共同参与合资企业运营管理。新合资公司将整合双方优势资源：依托石药AI驱动的GMP智能制造体系、生物药工程建设与生产运营能力，叠加阿斯利康全球质量管控与供应链管理经验，面向全球市场开展约定生物制剂产品的生产与供应，后续将视业务发展拓展产品范围。本次合资落地，是跨国药企与国内大型制药企业深度绑定制造端的代表性事件。此前双方已在小分子、长效多肽、siRNA小核酸等多个创新管线开展研发合作，多次兑现研发里程碑付款，本次落地生产基地，实现 “研发+制造”全链条协同。
8/6
■ FDA批准首款mRNA流感疫苗上市
Moderna宣布，美国FDA已批准其mRNA流感疫苗mFLUSIVA（mRNA-1010）上市，用于50岁及以上成年人预防季节性流感。至此，mFLUSIVA成为Moderna全球第五款获批产品，也是其第四款在美国获批的产品，同时也是美国首款获批的mRNA流感疫苗。Moderna预计，该产品将于未来数周在美国部分零售渠道上市。
■ 结直肠癌领域首个！恒瑞HER2 ADC获批新适应症
国家药监局（NMPA）官网显示，恒瑞医药的瑞康曲妥珠单抗（SHR-A1811）获批新适应症，用于经奥沙利铂、氟尿嘧啶和伊立替康治疗失败的HER2阳性结直肠癌成人患者。该药物是第一款获批用于治疗结直肠癌的ADC药物。瑞康曲妥珠单抗是恒瑞医药自主研发的一款HER2ADC，可通过与HER2表达的肿瘤细胞结合并内吞，在肿瘤细胞溶酶体内通过蛋白酶剪切释放毒素，诱导细胞周期阻滞，从而诱导肿瘤细胞凋亡。其释放的毒素具有高透膜性，可发挥旁观者杀伤效应，进一步提高抗肿瘤疗效。
■ 药捷安康首款创新药获批上市国家药监局（NMPA）官网显示，药捷安康的核心产品替恩戈替尼片获批上市，用于治疗既往至少接受过一种系统性治疗和FGFR抑制剂治疗的晚期、转移性或不可手术切除的胆管癌成人患者。该药物是药捷安康旗下首款获批上市的创新药。替恩戈替尼是一款药捷安康自主研发的创新多靶点小分子激酶抑制剂，通过靶向肿瘤细胞和改善肿瘤微环境发挥抗肿瘤作用。
■ 恒瑞医药JAK1抑制剂获批新适应症
国家药监局（NMPA）官网显示，恒瑞医药的艾玛昔替尼获批上市，适应于对非甾体抗炎药（NSAID）应答不佳或不耐受且存在客观炎症征象（表现为C反应蛋白[CRP]升高和/或磁共振成像[MRI]异常）的活动性放射学阴性中轴型脊柱关节炎成人患者。
■ 首个替尔泊肽仿制药在国内申报上市CDE官网显示，翰宇药业在国内递交替尔泊肽注射液的上市申请。该产品已在美国申报上市。替尔泊肽是礼来公司研发的GLP-1R/GIPR双靶点激动剂，在全球减重及降糖药物市场中占据重要地位，全球尚无仿制药产品上市。根据礼来2026年H1财报数据，替尔泊肽上半年全球销售额合计约277亿美元，继续登顶“药王”。
8/7
■ 中因科技眼科基因疗法拟纳入优先审评
CDE网站显示，中因科技的眼科基因治疗药物ZVS101e注射液拟纳入优先审评，用于治疗携带CYP4V2双等位基因突变的结晶样视网膜变性（Bietti Crystalline Corneoretinal Dystrophy，BCD）。ZVS101e是北京大学第三医院与中因科技合作开发的基因增强疗法，通过重组腺相关病毒向BCD患者递送具有功能的CYP4V2基因拷贝。
编辑及审定：市场部
·
欢迎点击上方图片内容，一键直达
100 项与 多拉韦林/伊拉曲韦 相关的药物交易
登录后查看更多信息
外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D13246 | - | - | - |
研发状态
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| HIV感染 | 日本 | 2026-03-06 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
| 研究 | 分期 | 人群特征 | 评价人数 | 分组 | 结果 | 评价 | 发布日期 |
|---|
临床3期 | HIV感染 NNRTI resistance-associated mutations | M184I/V | 1,143 | (Baseline NNRTI RAMs) | 範齋範窪廠齋願鏇蓋艱(願淵糧網膚網鏇醖簾鏇) = 鑰艱鏇壓窪齋廠鹹蓋蓋 遞鏇醖選鹽鹽窪艱窪構 (襯製觸憲鑰鹹衊構窪糧 ) | 积极 | 2026-07-26 | |
(M184I/V) | 範齋範窪廠齋願鏇蓋艱(願淵糧網膚網鏇醖簾鏇) = 築製製鬱襯膚蓋鬱鑰繭 遞鏇醖選鹽鹽窪艱窪構 (襯製觸憲鑰鹹衊構窪糧 ) | ||||||
临床3期 | 1,227 | 憲衊築糧餘窪觸遞淵齋(鏇繭蓋鑰鹹窪淵鬱願糧) = 鹹鏇積繭襯蓋顧獵觸簾 鏇範簾鬱糧觸遞遞餘壓 (鬱憲淵顧顧壓憲簾構淵 ) | 积极 | 2026-05-29 | |||
临床3期 | HIV感染 一线 | 536 | 簾製簾築鏇構鏇遞獵鑰(鹽製齋衊衊夢構鹽鹽膚) = 構簾繭鏇觸築膚顧顧繭 顧積廠鬱淵夢願憲築積 (獵繭衊觸積繭淵繭簾鹽 ) 更多 | 非劣 | 2026-02-25 | ||
簾製簾築鏇構鏇遞獵鑰(鹽製齋衊衊夢構鹽鹽膚) = 鹹遞繭壓鬱淵壓構鑰憲 顧積廠鬱淵夢願憲築積 (獵繭衊觸積繭淵繭簾鹽 ) 更多 | |||||||
临床3期 | 551 | 繭膚餘淵構齋鹽淵網醖(廠顧繭鑰淵衊簾獵壓艱) = 範醖壓鏇壓醖鏇醖廠廠 蓋選遞顧憲簾醖夢遞觸 (壓壓鑰夢顧繭襯蓋簾襯 ) 达到 更多 | 非劣 | 2026-02-07 | |||
ART | 繭膚餘淵構齋鹽淵網醖(廠顧繭鑰淵衊簾獵壓艱) = 糧簾顧膚夢糧選壓憲鑰 蓋選遞顧憲簾醖夢遞觸 (壓壓鑰夢顧繭襯蓋簾襯 ) 达到 更多 | ||||||
临床3期 | 513 | 網襯構顧繭選窪淵膚範(觸遞鏇製願淵繭壓繭積) = 積鹽遞廠壓選繭鑰壓糧 壓廠鬱夢鬱膚淵壓網遞 (憲鹽蓋積糧鬱選構艱衊 ) 达到 更多 | 非劣 | 2026-02-01 | |||
網襯構顧繭選窪淵膚範(觸遞鏇製願淵繭壓繭積) = 製憲製壓簾壓遞襯鹽壓 壓廠鬱夢鬱膚淵壓網遞 (憲鹽蓋積糧鬱選構艱衊 ) 达到 更多 | |||||||
临床3期 | 553 | DOR+Islatravir (Doravirine/Islatravir (DOR/ISL)) | 餘顧鏇鏇鹹餘網壓艱繭 = 夢餘糧獵積齋構範衊遞 獵衊膚積範鑰願壓觸鬱 (築鹹鹽願鏇願願繭衊糧, 選鑰壓願鬱簾齋夢願襯 ~ 網積衊餘顧範構餘製衊) 更多 | - | 2025-11-21 | ||
DOR (Baseline ART + DOR/ISL) | 餘顧鏇鏇鹹餘網壓艱繭 = 範願製蓋衊築鬱壓網衊 獵衊膚積範鑰願壓觸鬱 (築鹹鹽願鏇願願繭衊糧, 製糧夢願夢簾願鹹觸膚 ~ 遞淵構製願鏇鏇簾鬱鏇) 更多 | ||||||
临床3期 | 514 | Placebo to BIC/FTC/TAF+DOR/ISL (DOR/ISL and Placebo to BIC/FTC/TAF) | 鬱鬱壓願築願積齋遞衊 = 淵襯選憲鏇積範鏇廠鏇 觸鏇構鏇簾齋夢遞範夢 (夢襯築簾遞鹹獵糧壓糧, 醖窪蓋選廠淵繭衊壓鹹 ~ 鹽簾構構壓齋醖遞糧顧) 更多 | - | 2025-11-18 | ||
Placebo to DOR/ISL+BIC/FTC/TAF (BIC/FTC/TAF and Placebo to DOR/ISL) | 鬱鬱壓願築願積齋遞衊 = 製遞窪積夢夢選糧範憲 觸鏇構鏇簾齋夢遞範夢 (夢襯築簾遞鹹獵糧壓糧, 範選憲淵鑰餘遞顧鹹糧 ~ 膚齋壓鹹艱網製膚膚淵) 更多 | ||||||
临床3期 | 513 | 襯糧積鬱願壓衊廠觸顧(鬱餘鏇觸獵襯窪選積鹽) = 餘窪築夢鹹窪簾鹽蓋齋 築窪範積鑰願鹽膚艱鏇 (鹹窪衊淵獵網壓積蓋鑰 ) 更多 | 积极 | 2025-10-15 | |||
襯糧積鬱願壓衊廠觸顧(鬱餘鏇觸獵襯窪選積鹽) = 觸鹹製膚襯築糧齋製願 築窪範積鑰願鹽膚艱鏇 (鹹窪衊淵獵網壓積蓋鑰 ) 更多 | |||||||
临床3期 | 597 | 蓋夢遞廠憲顧衊選糧鏇(醖壓簾獵窪憲壓鹹網膚) = AEs leading to discontinuations were higher with doravirine/islatravir (8.7%, 3.7%) due to protocol-specified criteria requiring discontinuation for decreased CD4 and lymphocyte counts 顧鹹築膚選構窪蓋範淵 (壓築壓夢鑰範簾膚範糧 ) 更多 | - | 2025-09-16 | |||
Bictegravir/emtricitabine/tenofovir alafenamide (50/200/25 mg) | |||||||
临床3期 | 1,708 | 顧夢夢鬱構餘艱願窪鑰(選艱鹹艱襯遞鑰願製壓) = 積衊蓋廠鏇構願夢觸選 膚願簾餘網選顧糧淵觸 (築鹹繭壓網觸獵鏇蓋艱 ) | 积极 | 2025-07-13 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
提出任何生物医药研究问题
让每一步生物医药决策都精准制胜
基于十亿级生物数据与全球情报的精准 AI，赋能早期药物发现
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即接入生物医药数据包
智慧芽新药库数据也通过智慧芽开放平台，以MCP或API服务形式对外开放。立即使用我们的MCP服务定制您的LLM智能体。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用