An Open-label, Phase 1 Study to Characterize the Effects of Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF) on the Pharmacokinetics of MK-8527 in Healthy Participants

The goal of this study is to learn what happens to MK-8527 in a healthy person's body over time, called a pharmacokinetic (PK) study. Researchers want to learn if there is a difference in the healthy person's body when MK-8527 is taken as a single dose (Treatment A) or with the medication Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF) (Treatment B).

开始日期2025-02-21

申办/合作机构

Merck Sharp & Dohme LLC

NCT06560684

/ Recruiting临床2期IIT

A PHASE 2 CROSSOVER STUDY OF ON-DEMAND PREP FORMULATIONS COMPARING RECTAL AND ORAL TENOFOVIR-BASED PREP EVALUATING EXTENDED SAFETY, ACCEPTABILITY, AND PHARMACOKINETICS/PHARMACODYNAMICS

This is a Phase 2, multi-site, two-period, open label randomized crossover (Period 1 and 2) study. Participants are randomized 1:1 to one of two 8-week on-demand product sequences - TFV douche then oral F/TDF or oral F/TDF then TFV douche - with a 2 to 4-week washout period in between. Domains of safety, acceptability, adherence, and PK/PD (sub-study only) are assessed for each product.

开始日期2024-10-29

申办/合作机构

National Institute of Allergy & Infectious Diseases

NCT06513312

/ Recruiting临床2期

A Phase 2, Open-label, Multicenter, Randomized Study to Evaluate the Persistence, Safety, Acceptability, and Pharmacokinetics of Twice Yearly Long-acting Subcutaneous Lenacapavir for HIV Pre-Exposure Prophylaxis (PrEP) in People Who Would Benefit From PrEP

The goals of this clinical study are to learn more about the study drug lenacapavir (LEN), by comparing the consistent and continuous use of LEN and emtricitabine/tenofovir disoproxil fumarate (coformulated; Truvada®) (F/TDF), then by observing the safety of LEN and F/TDF, evaluating the acceptability of LEN injections and oral F/TDF, and observe how LEN moves throughout the body in people who would benefit from pre-exposure prophylaxis (PrEP).
The primary objective of this study is to compare LEN and F/TDF consistent and continuous use among people who would benefit from PrEP.

开始日期2024-10-07

申办/合作机构

Gilead Sciences, Inc.

100 项与恩曲他滨替诺福韦相关的临床结果

登录后查看更多信息

100 项与恩曲他滨替诺福韦相关的转化医学

登录后查看更多信息

100 项与恩曲他滨替诺福韦相关的专利（医药）

登录后查看更多信息

452

项与恩曲他滨替诺福韦相关的文献（医药）

2025-04-01·Therapeutic Advances in Infectious Disease

Exploring pregnant women’s experiences with dapivirine vaginal ring insertion during the MTN-042/DELIVER study in Uganda: a description of secondary data

Article

作者: Ssemambo, Phionah Kibalama ; Nalwoga, Justine ; Ssekasi, Annette Miwanda ; Mirembe, Brenda Gati ; Nakabiito, Clemensia ; Nansimbe, Joselyne ; Byogero, Rose

Background::

Involving pregnant women in HIV prevention trials is key to ensuring that they benefit from efficacious products. MTN-042/DELIVER was a phase IIIb, open-label, multi-site, randomized safety study, the first of its kind to enroll HIV-negative pregnant women into a prevention trial using oral Truvada ® once daily and the Dapivirine Vaginal Ring (DVR) every month. There is limited data on pregnant women’s experiences with ring insertion, which we explored.

Objectives::

To explore the experiences of pregnant women with DVR insertion during the MTN-042/DELIVER study at MU-JHU Care Limited in Kampala, Uganda.

Design::

A description of secondary data from the MTN-042/DELIVER study.

Methods::

Participant randomization was to either DVR or Truvada in varying ratios into three successive cohorts (based on gestational age). Ring self-insertion was required at enrolment and every 4 weeks until delivery. Pre-insertion counselling and supervised ring placement assessment were done. Enrollment data were collected to include counselling sessions, insertion tactics, ring self-insertion scores (Very difficult: 3+ attempts and/or pain, severe discomfort, Difficult: 2 attempts and/or moderate discomfort, Easy: 1 attempt with some ring repositioning and/or mild discomfort, Very easy: Smooth insertion and positioning in one attempt with no discomfort), assistance during insertion, encountered challenges and ring expulsion during use.

Results::

Out of 154 participants, 73% were randomized to the ring. At enrolment, all participants attempted self-insertion. Only one participant required additional counselling. The squatting position was uniformly favoured. Across all cohorts, 95% of participants had easy/very easy ring self-insertion. Five percent had difficult ring self-insertion, with some variations across cohorts. Challenges included difficulty in folding, gripping, inserting the ring far enough, requiring multiple attempts and reluctance to insert it. No expulsions during ring use were reported.

Conclusion::

Most pregnant women managed to insert the Ring themselves. However, participants above 36 weeks required more help with ring insertion compared to others. This suggests that it may be beneficial to encourage pregnant women to start using this HIV prevention method early in pregnancy, to minimize potential initial insertion challenges in late pregnancy.

Trial registration::

The primary study, MTN-042/DELIVER is registered as ID NCT03965923 at https://www.ClinicalTrials.gov .

2024-12-01·Journal of Family Medicine and Primary Care

Bariatric surgery and HIV: Joint venture between family, primary care, and HIV physicians

Article

作者: Ahmed, Mohamed H. ; Saidi, Raniah Al ; Choi, Ji Soo ; Aydemir, Ceren ; Mital, Dushyant

ABSTRACT:

We report a case of a 49-year-old female with a history of HIV infection for 12 years. The patient had excellent compliance with antiretroviral medications, raltegravir 400 mg twice daily and truvada once daily for HIV. Over the years, she maintained an undetectable viral load with a CD4+ count >200 cells/μL. She has a history of type II diabetes, hypertension, bipolar manic depression, endometriosis, recurrent herpes simplex attacks, arthritis in both shoulders, irritable bowel syndrome (IBS), and nonalcoholic fatty liver disease (NAFLD). She weighed 148 kg with a body mass index (BMI) of 52.08 kg/m2. Her medication included diltiazem 60 mg once a day, glyceryl trinitrate (GTN) spray, metformin 1 g twice daily, and linagliptin 500 mg once daily for her type II diabetes with glycated hemoglobin (HbA1c) of 8.4%. She has full capacity and elected to have bariatric surgery; 4 months postprocedure, she lost 28 kg with a reduced BMI of 38.62 kg/m2 with no postoperative complications. Her diabetes control improved, and she no longer required linagliptin and metformin. Following the procedure, she was given supplements including ferrous sulfate, vitamin B12, vitamin D, and calcium. She was also prescribed lansoprazole. The case illustrates that bariatric surgery is an effective and safe operation for people living with HIV. Due to complex needs and the need for regular follow-up; primary care, family, and HIV physicians can all collaborate in the care of individuals living with HIV and who underwent bariatric surgery.

2024-11-01·PHYTOMEDICINE

Potential of 6′‑hydroxy justicidin B from Justicia procumbens as a therapeutic agent against coronavirus disease 2019

Article

作者: Hwang, Yunha ; Kim, Yong-Bum ; Lee, Byoung-Seok ; Seo, Joung-Wook ; Lee, Sangho ; Eom, Han Young ; Yoo, Min Heui ; Im, Wan-Jung ; Ko, Kyong-Cheol ; Youm, Jihyun ; Kim, Seungtaek ; Han, Kang-Hyun

BACKGROUND:

Since the onset of the coronavirus disease 2019 (COVID-19) pandemic, remarkable advances have been made in vaccine development to reduce mortality. However, therapeutic interventions for COVID-19 are comparatively limited despite these intensive efforts. Furthermore, the rapid mutation capability of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), a characteristic of its RNA structure, has led to the emergence of multiple variants, necessitating a shift from a predominantly vaccine-centric approach to one that encompasses therapeutic strategies. 6'-Hydroxy justicidin B (6'-HJB), an arylnaphthalene lignan isolated from Justicia procumbens, a traditional Chinese medicine, is known for its antiviral properties.

HYPOTHESIS/PURPOSE:

The aim of the present study was to assess the effectiveness and safety of 6'-HJB against SARS-CoV-2 in order to determine its potential as a therapeutic agent against COVID-19.

METHODS:

The efficacy of 6'-HJB was evaluated both in vitro using Vero and Calu-3 cell lines and in vivo using ferrets. The safety assessment included toxicokinetics, safety pharmacology, and Good Laboratory Practice (GLP)-compliant toxicity evaluations following single- and repeated-dose toxicity studies in dogs.

RESULTS:

The anti-SARS-CoV-2 efficacy of 6'-HJB was evaluated through dose-response curve (DRC) analysis using immunofluorescence; 6'-HJB demonstrated superior inhibition of SARS-CoV-2 growth and lower cytotoxicity than remdesivir. In SARS-CoV-2-infected ferret, 6'-HJB showed efficacy comparable to that of the positive control, Truvada. Further GLP toxicity studies corroborated the safety profile of 6'-HJB. Single-dose and 4-week repeated oral toxicity studies in Beagle dogs demonstrated minimal harmful effects at the highest dosages. The lethal dose of 6'-HJB exceeded 2,000 mg kg^-1 in Beagle dogs. Toxicokinetic and GLP safety pharmacology studies demonstrated no adverse effects of 6'-HJB on metabolic processes, respiratory or central nervous systems, or cardiac functions.

CONCLUSION:

This research highlights both the antiviral efficacy and safety profile of 6'-HJB, underscoring its potential as a novel COVID-19 treatment option. The potential of 6'-HJB was demonstrated using modern scientific methodologies and standards.

176

项与恩曲他滨替诺福韦相关的新闻（医药）

2025-03-13

·SYNAPSE

2025年3月13日全球新药进展早知道

1. 诺华「司库奇尤单抗」化脓性汗腺炎新适应症在华获批 3月12日，诺华宣布司库奇尤单抗（商品名：可善挺）获得国家药品监督管理局批准，用于治疗中重度化脓性汗腺炎（反常性痤疮）的成人患者。可善挺®是目前中国唯一获批化脓性汗腺炎（HS）的生物制剂。作为一款全人源白介素IL-17A抑制剂，该药可显著减少炎性结节和脓肿，控制病情的复燃，为HS治疗提供了全新选择。两项随机、双盲、安慰剂对照、多中心的III期临床研究，即SUNSHINE和SUNRISE研究评估了司库奇尤单抗在HS患者中的疗效和安全性。结果显示，两项研究的Q2W组均达到主要疗效终点。其中，SUNSHINE研究Q2W组的HS应答率为45%，显著高于安慰剂组的34%；SUNRISE研究Q2W组的HS应答率为42%，同样显著高于安慰剂组的31%。 2. 潜在首款，儿童近视眼药水疗法在美国递交新药申请 3月12日，Sydnexis宣布，美国FDA已受理该公司为在研疗法SYD-101提交的新药上市申请（NDA），预计在2025年10月23日之前完成审评。新闻稿指出，如果获批，SYD-101将成为美国FDA批准的首个用于治疗儿童近视进展的药物。该NDA申请基于3期临床试验STAR研究的主要及次要终点数据。该研究旨在评估SYD-101减缓儿童近视进展及相关合并症风险的效果。SYD-101是一种在研低剂量硫酸阿托品滴眼液，旨在达到治疗儿童近视疗效的同时，增强药理稳定性和减少不适，以改善治疗的连续性。SYD-101无需降低pH值，并能在室温下达到长达3年的有效期。 3. 辉瑞启动全球首个CD25 ADC临床试验 3月11日，辉瑞在clinical trials网站上，登记了CD25 ADC药物PF-08046032的首个临床试验（NCT06870487），在多种淋巴瘤或实体瘤患者中探索单药或者和PD-1抗体sasanlimab联用，该临床预计于2025年3月启动，入组人数为220例。该临床分为三个部分，第一个部分为PF-08046032单药爬坡，第二个部分为和PD-1抗体联用剂量优化，第三部分为PD-1抗体联用扩展试验。2024年SITC会议上，辉瑞首次公布了PF-08046032的产品信息，由低亲和力的抗CD25抗体与MMAE进行偶联。除了辉瑞，ADC药物研发巨头第一三共和阿斯利康，也均也进行了CD25 ADC的专利布局。 4. 挑战度普利尤单抗！诺华BTK抑制剂瑞米布替尼启动新III期临床 3月10日，全球临床试验收录网站clinicaltrials显示，诺华启动了新型、高选择性、口服、共价不可逆BTK抑制剂瑞米布替尼（Remibrutinib）对比度普利尤单抗的头对头III期研究（RECLAIM）。该研究是一项在美国开展的多中心、随机、双盲、双模拟IIIb期临床试验（n=400），旨在评估瑞米布替尼（25mg，每日2次）对比度普利尤单抗（300mg，每2周1次）在早期时间点作为附加治疗用于治疗二代H1抗组胺药控制不佳的中重度慢性自发性荨麻疹（CSU）成人患者的有效性和安全性。研究的主要终点是基线至第4周患者的每周荨麻疹活动度评分（UAS7）的绝对变化。 5. 只需每年一针，长效HIV预防疗法挺进3期临床日前，吉利德公布了两种每年一次的lenacapavir配方，作为暴露前预防（PrEP）疗法，在1期临床试验中的积极结果。数据支持每年一次lenacapavir用于PrEP的未来开发。该结果已发表于医学期刊《柳叶刀》。吉利德科学公司计划于2025年下半年启动3期临床试验。1期临床试验数据显示，每年一次、肌肉注射的两种lenacapavir配方达到并维持了超出在3期临床试验PURPOSE 1和PURPOSE 2试验中观察到的与HIV预防疗效相关的血浆浓度。此前报道的PURPOSE 1和PURPOSE 2数据显示，每年两次皮下注射lenacapavir在降低HIV感染方面显示出优于背景HIV发病率和每日一次口服Truvada。 1. 53亿美元！罗氏与Zealand合作开发胰淀素类似物Petrelintide 3月12日，罗氏宣布已与Zealand Pharma（纳斯达克哥本哈根：ZEAL）签订了独家合作和许可协议（CVR-no.20045078）。根据该协议条款，两家公司将合作开发和商业化petrelintide，这是Zealand Pharma的长效胰淀素类似物（amylin analog），作为独立疗法，以及与罗氏领先的肠促胰岛素（incretin）资产CT-388的固定剂量组合。Petrelintide目前处于2期临床开发阶段，适合每周皮下注射一次。根据协议条款，Zealand将获得16.5亿美元的预付现金、12亿美元的开发里程碑以及24亿美元的销售里程碑，对Zealand的总对价高达53亿美元。Petrelintide和Petrelintide/CT-388的损益将在美国和欧洲按50/50的比例分摊，Zealand有资格在世界其他地区的净销售额中获得两位数的特许权使用费，最高可达15%。 2. 3500万美元D轮融资，开发首个靶向Hippo-YAP通路抑制剂 3月12日，加利福尼亚州圣马特奥，Vivace Therapeutics，一家开发针对Hippo通路的一流癌症疗法的小分子发现和开发公司，宣布完成3500万美元的D轮融资。本轮融资由现有投资者RA Capital Management领投，包括其他现有投资者Canaan Partners和Cenova Capital（千骥资本）的投资。所得款项将用于支持该公司一流的转录增强相关结构域（TEAD）自线粒体酰化抑制剂VT3989的持续临床开发，最初重点是间皮瘤。迄今为止，该公司已累计融资1.05亿美元。在融资的同时，RA Capital Management的合伙人Jake Simson博士加入了该公司的董事会。内容来源于网络，如有侵权，请联系删除。

申请上市临床研究抗体药物偶联物合作融资

2025-03-12

·药明康德

一年只需一针的长效HIV疗法；罗氏合作开发潜在“best-in-class”减肥疗法……

▎药明康德内容团队编辑只需每年一针，长效HIV预防疗法挺进3期临床吉利德科学（Gilead Sciences）公司日前公布了两种每年一次的lenacapavir配方，作为暴露前预防（PrEP）疗法，在1期临床试验中的积极结果。数据支持每年一次lenacapavir用于PrEP的未来开发。该结果已发表于医学期刊《柳叶刀》。吉利德科学公司计划于2025年下半年启动3期临床试验。 1期临床试验数据显示，每年一次、肌肉注射的两种lenacapavir配方达到并维持了超出在3期临床试验PURPOSE 1和PURPOSE 2试验中观察到的与HIV预防疗效相关的血浆浓度。此前报道的PURPOSE 1和PURPOSE 2数据显示，每年两次皮下注射lenacapavir在降低HIV感染方面显示出优于背景HIV发病率和每日一次口服Truvada。两种配方的受试者血浆中lenacapavir浓度在至少56周内均高于95%有效浓度。此外，两种每年一次lenacapavir配方在第52周的中位谷浓度（分别为57.0 ng/mL和65.6 ng/mL）均高于PURPOSE 1和PURPOSE 2试验中每年两次lenacapavir在第26周观察到的23.4 ng/mL。 Lenacapavir是一种“first-in-class”长效HIV病毒衣壳抑制剂，可以干扰HIV病毒衣壳蛋白的组装和拆卸，在病毒生命周期的多个阶段发挥作用。它已经获得美国FDA授予的突破性疗法认定，用于HIV病毒感染暴露前预防。2024年，《科学》期刊也将lenacapavir评为年度科学突破，表示这一“first-in-class”药物为艾滋病的长效治疗与预防带来了新的曙光。维持HIV病毒抑制48周，默沙东双药疗法达两项3期临床主要终点默沙东（MSD）公司今日宣布，在研每日一次口服双药方案doravirine/islatravir（DOR/ISL）在两项关键性3期试验中获得积极结果。在两项试验中，DOR/ISL与活性对照组相比达到非劣效性标准。基于这些积极结果，默沙东计划在2025年中期启动向监管机构提交上市申请。在双盲试验MK-8591A-052中，主要终点（HIV-1 RNA≥50拷贝/毫升）结果显示，在接受克替拉韦/恩曲他滨/替诺福韦艾拉酚胺（BIC/FTC/TAF）治疗下已实现病毒抑制的成人患者中，第48周切换至DOR/ISL的受试者中有1.5%病毒载量达到或超过50拷贝/毫升，而BIC/FTC/TAF组为0.6%（治疗差异0.9%，95% CI：-1.9，2.9）。第48周切换至DOR/ISL的受试者中有91.5%维持了病毒抑制，而继续接受BIC/FTC/TAF治疗的受试者中这一比例为94.2%（治疗差异-2.6%，95% CI：-7.1，2.6）。在开放标签试验MK-8591A-051中，在接受基线抗病毒治疗（bART）并获得病毒抑制的成人患者中，第48周切换接受DOR/ISL治疗的受试者中有1.4%病毒载量达到或超过50拷贝/毫升，而继续接受bART治疗的患者这一数值为4.9%（治疗差异-3.6%，95% CI：-7.8，-0.8）。第48周切换至DOR/ISL的受试者中有95.6%维持了病毒抑制，而继续接受bART的受试者中这一比例为91.9%（治疗差异3.7%，95% CI：-0.3，8.9）。 4个月一次，长效HIV抗体疗法组合3期临床结果积极 ViiV Healthcare今日宣布，其长效HIV抗体疗法N6LS，在2b期临床试验EMBRACE中取得积极结果。数据显示，每四个月一次给药的N6LS，与每月一次长效cabotegravir（CAB LA）联用，可成功使已稳定接受治疗的HIV成年患者保持病毒抑制，并且耐受性良好。 EMBRACE研究在六个月主要终点时的结果显示，静脉注射60 mg/kg的N6LS组中96%的受试者，以及皮下注射3000 mg的N6LS组中88%的受试者维持了HIV-1 RNA水平低于50拷贝/毫升，而标准治疗组为96%。基于试验中观察到的积极结果，ViiV Healthcare将在EMBRACE的第二部分试验中，进一步评估六个月一次静脉注射N6LS与CAB LA联用的效果。罗氏合作开发潜在“best-in-class”胰淀素类似物 Zealand Pharma今日宣布，与罗氏（Roche）达成全球合作及许可协议，共同开发Zealand Pharma的胰淀素类似物petrelintide，作为体重管理的基石性疗法，同时迅速扩展至相关适应症。新闻稿指出，petrelintide具有成为“best-in-class”疗法的潜力。根据协议，双方将共同开发和商业化petrelintide及其组合产品，包括petrelintide与罗氏的潜在“best-in-class”胰高血糖素样肽-1（GLP-1）、葡萄糖依赖性促胰岛素多肽（GIP）受体双重激动剂CT-388构成的固定剂量组合产品。双方将在美国和欧洲共同商业化petrelintide及本次合作产生的其他产品，而罗氏获得全球其他地区的独家商业化权益。Zealand Pharma可在美国和欧洲参与最多50%的商业化活动。 Zealand Pharma将获得16.5亿美元的前期付款。Zealand Pharma还将有资格获得12亿美元的研发里程碑付款（主要与petrelintide单药治疗3期临床试验启动相关）及24亿美元的销售里程碑付款。 Petrelintide为一种长效胰淀素类似物，适合每周一次皮下注射。该药物在设计时注重化学和物理稳定性，在中性pH值下无纤维化现象，从而可与其他肽类药物实现联合配方及联合给药。超9亿美元助力反义寡核苷酸疗法开发 Ono Pharmaceutical（ONO）宣布已与Ionis Pharmaceuticals签订许可协议，获得反义寡核苷酸（ASO）疗法sapablursen的开发及商业化权益。Sapablursen是一种用于治疗真性红细胞增多症（PV）的在研ASO药物，目前正在2期临床试验IMPRSSION中针对成人PV患者进行评估。Sapablursen已于2024年1月获得美国FDA授予的快速通道资格，并于2024年8月获得孤儿药资格。根据协议，ONO将获得全球范围内开发和商业化sapablursen的独家许可。Ionis将继续负责完成正在进行的2期临床试验IMPRSSION，而ONO将全权负责后续开发、监管申报及商业化工作。ONO将支付2.8亿美元前期付款，并根据达到研发、监管及销售里程碑，支付高达6.6亿美元的额外里程碑付款。 Sapablursen的设计旨在降低TMPRSS6基因编码的跨膜蛋白酶丝氨酸6的产生，从而增加铁稳态关键调控因子铁调素（hepcidin）的表达。通过提高铁调素的产生，sapablursen有望对真性红细胞增多症等血液疾病产生积极影响。 ▲欲了解更多前沿技术在生物医药产业中的应用，请长按扫描上方二维码，即可访问“药明直播间”，观看相关话题的直播讨论与精彩回放参考资料： [1] First Clinical Data for Gilead’s Investigational Once-Yearly Lenacapavir for HIV Prevention Presented at CROI 2025 and Published in The Lancet. Retrieved March 12, 2025, from https://www.gilead.com/news/news-details/2025/first-clinical-data-for-gileads-investigational-once-yearly-lenacapavir-for-hiv-prevention-presented-at-croi-2025-and-published-in-the-lancet [2] Merck Announces Positive Data from Phase 3 Trials that Show the Investigational, Once-Daily, Oral, Two-Drug Regimen of Doravirine/Islatravir (DOR/ISL) Maintained HIV-1 Viral Suppression at Week 48. Retrieved March 12, 2025, from https://www-merck-com.libproxy1.nus.edu.sg/news/merck-announces-positive-data-from-phase-3-trials-that-show-the-investigational-once-daily-oral-two-drug-regimen-of-doravirine-islatravir-dor-isl-maintained-hiv-1-viral-suppression-at-week-48/ [3] ViiV HEALTHCARE’S INVESTIGATIONAL BROADLY NEUTRALISING ANTIBODY - N6LS - SUCCESSFULLY MAINTAINS VIRAL SUPPRESSION IN LONG-ACTING TREATMENT OF HIV. Retrieved March 12, 2025, from https://viivhealthcare.com/hiv-news-and-media/news/press-releases/2025/march/investigational-broadly-neutralising-antibody/ [4] Zealand Pharma and Roche enter collaboration and license agreement to co-develop and co-commercialize petrelintide as a future foundational therapy for people with overweight and obesity. Retrieved March 12, 2025, from https://www.globenewswire.com/news-release/2025/03/12/3041113/0/en/Zealand-Pharma-and-Roche-enter-collaboration-and-license-agreement-to-co-develop-and-co-commercialize-petrelintide-as-a-future-foundational-therapy-for-people-with-overweight-and-o.html [5] Ono Enters into License Agreement with Ionis Pharmaceuticals for Sapablursen for the Treatment of Polycythemia Vera. Retrieved March 12, 2025, from https://www.businesswire.com/news/home/20250311080840/en 免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：本文来自药明康德内容团队，欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

临床结果临床3期突破性疗法临床2期

2025-03-12

·PipelineReview

First Clinical Data for Gilead’s Investigational Once-Yearly Lenacapavir for HIV Prevention Presented at CROI 2025 and Published in The Lancet

– Phase 1 Data Indicate Potential for Use of Once-Yearly Lenacapavir for HIV Prevention, with Plans to Launch a Phase 3 Trial in 2H 2025 – – Also at CROI: New PURPOSE 1 Data Showcasing Preference for Twice-Yearly Lenacapavir vs. Once-Daily Orals and In-Depth Look at Adolescent Pharmacokinetic, Safety and Efficacy Data – FOSTER CITY, CA, USA I Marcch 11, 2025 I Gilead Sciences, Inc. (Nasdaq: GILD) today presented the first data from its ongoing Phase 1 study investigating two novel, once-yearly formulations of lenacapavir, the company’s injectable HIV-1 capsid inhibitor, for the investigational use of HIV prevention as pre-exposure prophylaxis (PrEP). The data were presented during an oral abstract session at the Conference on Retroviruses and Opportunistic Infections (CROI 2025) and were also published today in The Lancet . Data will support the future development of once-yearly lenacapavir for PrEP, for which Gilead plans to launch a Phase 3 study in the second half of 2025. The Phase 1 study data showed that the two different formulations of once-yearly lenacapavir administered via intramuscular injection achieved and maintained plasma concentrations exceeding those associated with HIV prevention efficacy observed in the Phase 3 PURPOSE 1 trial ( NCT04994509 ) and PURPOSE 2 trial ( NCT04925752 ). The previously reported PURPOSE 1 and PURPOSE 2 data showed that twice-yearly subcutaneous lenacapavir demonstrated superiority at reducing HIV infections when compared to background HIV incidence (bHIV) and once-daily oral Truvada® (emtricitabine 200mg and tenofovir disoproxil fumarate 300mg; F/TDF) in a broad and geographically diverse range of people. “Gilead is continuing to innovate in our work to develop additional person-centered long-acting injectable and oral options to help people find an HIV prevention choice that is right for them,” said Jared Baeten, MD, PhD, Senior Vice President, Virology Therapeutic Area Head, Gilead Sciences. “Once-yearly lenacapavir, if approved, could become an important new HIV prevention option that could help address PrEP adherence and persistence challenges for individuals who need or want PrEP around the world.” Promising once-yearly lenacapavir for PrEP pharmacokinetic profiles over 52 weeks The Phase 1 study evaluated the pharmacokinetics, safety and tolerability of two intramuscular single-dose 5000mg lenacapavir formulations. The trial included 40 healthy adults at low risk of HIV acquisition, between the ages of 18 and 55 years, with a body mass index of less than or equal to 35.0 kg/m 2 . Lenacapavir plasma concentrations for participants remained above the 95% effective concentration for at least 56 weeks with both formulations. Furthermore, median trough concentrations of both formulations of once-yearly lenacapavir at Week 52 (57.0 ng/mL and 65.6 ng/mL) were higher than those observed with twice-yearly lenacapavir in the PURPOSE 1 and PURPOSE 2 trials at Week 26 (23.4 ng/mL). Data from the study confirmed that both once-yearly formulations of lenacapavir warrant further investigation. Safety data demonstrated both formulations of once-yearly lenacapavir for PrEP were well tolerated, with no new safety signals Once-yearly lenacapavir is being investigated as an intramuscular injection. This is different from the subcutaneous formulation of lenacapavir, which is being investigated for twice-yearly dosing. The most commonly reported adverse event for both intramuscular formulations studied was injection site pain, which was mostly mild in severity and resolved within 1 week (occurred in 80% of participants receiving formulation 1, and 75% receiving formulation 2), and was reduced by pretreatment with an ice pack. Medication-emergent adverse events were similar between the two cohorts and mostly mild to moderate in severity. New PrEP modality preference data demonstrate preference for twice-yearly lenacapavir vs. once-daily orals in PURPOSE 1 survey participants New quantitative survey data and late-breaking qualitative survey data from the PURPOSE 1 trial, evaluating twice-yearly subcutaneous lenacapavir for PrEP among cisgender women in sub-Saharan Africa, were also presented at CROI in two poster sessions. An interim analysis of surveys included 2,561 trial participants’ self-reported preferences for twice-yearly lenacapavir for PrEP injections and once-daily pills, with approximately two-thirds of survey respondents preferring twice-yearly lenacapavir at Week 52 of their trial participation, compared to fewer than one-third of respondents preferring once-daily pills. Additionally, at Week 52, most respondents (61%) reported they would feel more protected from HIV with twice-yearly PrEP injections compared with once-daily pills, and 61% of respondents also reported they would feel more confident about not missing a PrEP dose with twice-yearly injections compared with once-daily pills. Qualitative data among 108 participants also showed that respondents, particularly adolescents aged 16 and 17 years, noted that twice-yearly injections better suited their lifestyles compared with once-daily pills. New study population data from PURPOSE 1 show comparable pharmacokinetic and safety profiles for both adolescent and adult trial participants Additional adolescent-related data from the PURPOSE 1 trial were also presented at CROI yesterday during an oral abstract session and press conference. PURPOSE 1 is the first adult Phase 3 HIV prevention trial to intentionally include adolescents aged 16 and 17 years, and trial enrollment was much higher than in typical adolescent-dedicated studies (124 adolescents, 56 of whom were assigned to the lenacapavir group). The data showed that observed lenacapavir plasma concentrations were comparable between adolescent and adult trial groups, with participants in both groups experiencing the same most common adverse events. There were zero incident HIV infections across the adolescent and adult groups receiving lenacapavir. Given these results, data submitted to regulatory authorities support the potential use of twice-yearly lenacapavir for adolescents who need or want PrEP The use of lenacapavir for the prevention of HIV is investigational and has not been determined to be safe or efficacious and is not approved anywhere globally. There is currently no cure for HIV or AIDS. About Lenacapavir Lenacapavir is approved in multiple countries for the treatment of adults with multi-drug resistant HIV in combination with other antiretrovirals. The use of lenacapavir for HIV prevention is investigational and the safety and efficacy of lenacapavir for this use have not been established. The multi-stage mechanism of action of lenacapavir is distinguishable from other currently approved classes of antiviral agents. While most antivirals act on just one stage of viral replication, lenacapavir is designed to inhibit HIV at multiple stages of its lifecycle and has no known cross resistance exhibited in vitro to other existing drug classes. Lenacapavir is being evaluated as a long-acting option in multiple ongoing and planned early and late-stage clinical studies in Gilead’s HIV prevention and treatment research program. Lenacapavir is being developed as a foundation for potential future HIV therapies with the goal of offering both long-acting oral and injectable options with several dosing frequencies, in combination or as a mono agent, that help address individual needs and preferences of people and communities affected by HIV. Science Magazine named lenacapavir its 2024 “Breakthrough of the Year.” About the PURPOSE Program Gilead’s landmark PURPOSE program is the most comprehensive and diverse HIV prevention trial program ever conducted. The program comprises five HIV prevention trials around the world that are focused on innovation in science, trial design, community engagement and health equity. The PURPOSE trials are evaluating the safety and efficacy of an investigational, twice-yearly injectable medicine, lenacapavir, to reduce the chance of getting HIV. The Phase 2 and 3 program, consisting of PURPOSE 1-5, is assessing the potential of lenacapavir to help a diverse range of people around the world who could benefit from PrEP. More information about the PURPOSE program, including individual trial descriptions, populations and locations, can be found at www.purposestudies.com . About Gilead HIV For more than 35 years, Gilead has been a leading innovator in the field of HIV, driving advances in treatment, prevention and cure research. Gilead researchers have developed 12 HIV medications , including the first single-tablet regimen to treat HIV, the first antiretroviral for pre-exposure prophylaxis (PrEP) to help reduce new HIV infections, and the first long-acting injectable HIV treatment medication administered twice-yearly. Our advances in medical research have helped to transform HIV into a treatable, preventable, chronic condition for millions of people. Gilead is committed to continued scientific innovation to provide solutions for the evolving needs of people affected by HIV around the world. Through partnerships , collaborations and charitable giving, the company also aims to improve education, expand access and address barriers to care, with the goal of ending the HIV epidemic for everyone, everywhere. Gilead was recognized as one of the leading philanthropic funders of HIV-related programs in a report released by Funders Concerned About AIDS. SOURCE: Gilead Sciences

临床3期临床结果临床1期临床2期上市批准

100 项与恩曲他滨替诺福韦相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
-	恩曲他滨替诺福韦	J05AR03	-

研发状态

批准上市

10 条最早获批的记录,

后查看更多信息

适应症	国家/地区	公司	日期
HIV感染	美国	Gilead Sciences, Inc.	2004-08-02

未上市

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
乙型肝炎	临床3期	法国	Gilead Sciences, Inc.	2007-01-01
慢性乙型肝炎	临床3期	美国	Gilead Sciences, Inc.	2005-02-01
慢性乙型肝炎	临床3期	澳大利亚	Gilead Sciences, Inc.	2005-02-01
慢性乙型肝炎	临床3期	保加利亚	Gilead Sciences, Inc.	2005-02-01
慢性乙型肝炎	临床3期	加拿大	Gilead Sciences, Inc.	2005-02-01
慢性乙型肝炎	临床3期	捷克	Gilead Sciences, Inc.	2005-02-01
慢性乙型肝炎	临床3期	法国	Gilead Sciences, Inc.	2005-02-01
慢性乙型肝炎	临床3期	德国	Gilead Sciences, Inc.	2005-02-01
慢性乙型肝炎	临床3期	希腊	Gilead Sciences, Inc.	2005-02-01
慢性乙型肝炎	临床3期	意大利	Gilead Sciences, Inc.	2005-02-01

登录后查看更多信息

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


NCT04692077 (CTgov)	临床2期	HIV感染	9	CAB LA+Tenofovir disoproxil fumarate/emtricitabine (TDF/FTC) tablet	積憲顧餘鏇蓋簾夢遞選(願窪廠襯艱繭鹽壓醖壓) = 齋齋壓顧範齋齋繭願構蓋齋積衊糧艱廠鏇憲衊 (鏇糧積選鑰鹽夢顧壓獵, 1.3) 更多	-	2025-01-29
NCT03048422 (IMPAACT 2010 (VESTED), Pubmed \| J Acquir Immune Defic Syndr)	临床3期	bone mineral density \| creatinine clearance	-	Dolutegravir + emtricitabine/tenofovir alafenamide (DTG + FTC/TAF)	廠積獵網夢鑰構遞壓淵(願鹽糧艱選鬱鹹鑰衊鑰) = 遞築鬱範製餘簾繭繭鹹築觸夢憲壓鏇鑰構蓋淵 (網壓網選積餘積壓鏇選 )	积极	2024-10-01
				Dolutegravir + emtricitabine/tenofovir disoproxil fumarate (DTG + FTC/TDF)	廠積獵網夢鑰構遞壓淵(願鹽糧艱選鬱鹹鑰衊鑰) = 襯夢壓簾遞鹹範壓艱獵築觸夢憲壓鏇鑰構蓋淵 (網壓網選積餘積壓鏇選 )
NCT04298697 (CTgov)	临床4期	HIV感染	43	Tenofovir disoproxil fumarate/emtricitabine (TDF/FTC) (TDF/FTC for 1 Week)	淵壓鬱鬱範簾齋獵網製(鹽艱鏇願築餘範網顧觸) = 淵觸艱齋鹹觸鹽鬱窪觸壓壓膚鬱醖夢蓋艱網夢 (顧構簾選齋窪夢鑰廠鏇, 獵願壓築鹹網觸製壓願 ~ 衊遞膚衊餘選夢範齋鏇) 更多	-	2024-09-19
				Tenofovir disoproxil fumarate/emtricitabine (TDF/FTC) (TDF/FTC for 13 Weeks)	淵壓鬱鬱範簾齋獵網製(鹽艱鏇願築餘範網顧觸) = 窪淵獵願製窪鑰製鑰構壓壓膚鬱醖夢蓋艱網夢 (顧構簾選齋窪夢鑰廠鏇, 範願範鏇簾壓顧構憲範 ~ 醖願襯簾觸艱艱蓋廠觸) 更多
NCT04870671 (CTgov)	早期临床1期	获得性免疫缺陷综合征	14	Tenofovir Disoproxil Fumarate/Emtricitabine (TDF/FTC) (High Adherence)	繭窪襯艱齋網膚膚範餘(範憲遞築選簾壓觸餘鬱) = 窪廠壓願鏇繭選襯簾積齋觸鏇願衊構憲鏇廠積 (廠壓壓鹹製觸窪淵廠壓, 夢鏇鹹選觸糧構醖構鑰 ~ 齋糧衊壓範襯範鑰衊鏇) 更多	-	2024-01-30
				Tenofovir Disoproxil Fumarate/Emtricitabine (TDF/FTC) (Low Adherence)	繭窪襯艱齋網膚膚範餘(範憲遞築選簾壓觸餘鬱) = 鏇襯獵觸蓋鏇廠積夢膚齋觸鏇願衊構憲鏇廠積 (廠壓壓鹹製觸窪淵廠壓, 夢獵壓鹽鹹遞餘願蓋餘 ~ 襯艱繭餘築簾鬱觸製網) 更多
NCT03593655 (MTN-034/REACH, Pubmed \| Lancet HIV)	临床2期	HIV感染	396	Dapivirine vaginal ring	壓鹹憲齋範築鹹觸壓夢(夢範廠壓膚鑰淵獵築網) = 遞構鬱獵構願獵窪顧選衊鹽選鏇壓鬱壓廠鬱醖 (鬱壓選窪顧醖膚觸遞鏇 )	积极	2023-12-01
				Emtricitabine plus tenofovir disoproxil fumarate	壓鹹憲齋範築鹹觸壓夢(夢範廠壓膚鑰淵獵築網) = 襯艱網鹽膚鏇憲襯憲蓋衊鹽選鏇壓鬱壓廠鬱醖 (鬱壓選窪顧醖膚觸遞鏇 )
NCT04140266 (MTN-043, CTgov)	临床3期	HIV感染	394	Dapivirine (Group A: Dapivirine (DPV) Vaginal Ring (VR)-004)	壓選廠構窪網餘顧製壓 = 壓蓋遞膚鬱壓鏇製網壓簾憲鏇製膚餘窪願遞選 (簾廠選艱鹹顧鏇鑰衊鏇, 鑰鹹壓蓋遞鬱積獵願窪 ~ 衊鹹廠蓋壓鹹遞鹽獵襯)	-	2023-08-04
				Truvada Tablet (Group B: Truvada Tablet)	壓選廠構窪網餘顧製壓 = 遞壓衊壓窪夢獵積膚積簾憲鏇製膚餘窪願遞選 (簾廠選艱鹹顧鏇鑰衊鏇, 網簾鏇鬱膚衊鹽衊餘齋 ~ 網範遞範獵鏇壓選選選)
NCT02213328 (CTgov)	临床2期	HIV感染	148	Truvada	襯鹹淵願蓋餘遞衊獵糧 = 壓蓋廠繭繭鹹觸襯夢簾蓋餘鏇憲積鏇遞選憲憲 (窪膚衊選願蓋範壓襯糧, 齋醖顧壓蓋醖簾淵遞願 ~ 鹽觸廠繭壓製壓鹽製夢) 更多	-	2023-07-03
NCT03164564 (HPTN 084, CTgov)	临床3期	HIV感染	3,224	Oral CAB+CAB LA+Oral TDF/FTC (Arm A: CAB + Placebo TDF/FTC + CAB LA)	蓋艱衊蓋選齋觸齋鏇製 = 衊築蓋窪膚襯製齋艱夢鹽艱構繭廠網範願襯網 (製遞積積遞憲顧鏇廠選, 廠遞廠淵憲鏇蓋齋蓋壓 ~ 鬱廠鹽醖構鬱鑰衊鑰壓) 更多	-	2023-03-28
				Placebo for CAB LA+Oral TDF/FTC (Arm B: TDF/FTC + Placebo CAB + Placebo CAB LA)	蓋艱衊蓋選齋觸齋鏇製 = 積廠遞糧夢壓壓膚簾遞鹽艱構繭廠網範願襯網 (製遞積積遞憲顧鏇廠選, 遞蓋簾鑰鬱夢繭壓願構 ~ 壓鬱構簾觸觸顧憲鹹鹽) 更多
NCT03593655 (MTN-034/REACH, CTgov)	临床2期	HIV感染	247	Dapivirine vaginal ring+FTC/TDF (Sequence A: Dapivirine Vaginal Ring + FTC/TDF)	膚醖廠窪糧鬱選鬱觸鹹 = 觸鹽遞鏇膚憲鹽壓積鑰壓網構鹹願壓網獵衊壓 (齋範齋構窪觸鏇鏇艱顧, 鹹鬱鏇襯網鬱蓋範範繭 ~ 築廠餘顧鏇選醖鏇蓋膚) 更多	-	2023-02-03
				Dapivirine vaginal ring+FTC/TDF (Sequence B: FTC/TDF + Dapivirine Vaginal Ring)	膚醖廠窪糧鬱選鬱觸鹹 = 鏇衊製網蓋遞廠齋齋積壓網構鹹願壓網獵衊壓 (齋範齋構窪觸鏇鏇艱顧, 觸選選鬱廠鏇襯顧膚鏇 ~ 鹹膚簾齋壓鏇衊糧艱鹹) 更多
NCT02870790 (EPIC-NSW, Pubmed \| Clin Infect Dis)	临床3期	丙型肝炎	9,596	Coformulated tenofovir disoproxil fumarate and emtricitabine	齋糧鹽衊築築簾衊範網(壓願鏇願鏇膚廠遞繭衊) = 簾築鹽繭壓廠夢餘憲構鹽廠糧齋醖衊願鹹糧遞 (鹹範鹽廠鬱艱膚膚醖願, .1 ~ .3) 更多	积极	2022-10-29