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更新于：2025-08-22

Efavirenz

依非韦伦

更新于：2025-08-22

概要

基本信息

药物类型

小分子化药

别名

(S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-benzo[d][1,3]oxazin-2-one、6-chloro-4-(2-cyclopropyl-1-ethynyl)-4-trifluoromethyl-(4S)-1,4-dihydro-2H-benzo[d][1,3]oxazin-2-one、Efavirenz (JAN/USP/INN)

+ [19]

靶点

作用方式

抑制剂

作用机制

RT抑制剂(逆转录酶抑制剂)

治疗领域

免疫系统疾病感染泌尿生殖系统疾病

在研适应症

HIV感染

非在研适应症

获得性免疫缺陷综合征艾滋病相关机会致病菌感染避孕+ [5]

原研机构

Bristol Myers Squibb Co.

在研机构

Teva Pharmaceuticals Europe BVMerck Sharp & Dohme LLCMerck Sharp & Dohme BV

+ [3]

非在研机构

Abbott Laboratories

Merck Sharp & Dohme Corp.

Bristol Myers Squibb Co.

+ [2]

权益机构-

最高研发阶段批准上市

首次获批日期

美国 (1998-09-17),

HIV感染

最高研发阶段(中国)批准上市

特殊审评孤儿药 (日本)、加速批准 (美国)

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结构/序列

分子式C14H9ClF3NO2

InChIKeyXPOQHMRABVBWPR-ZDUSSCGKSA-N

CAS号154598-52-4

关联

289

项与依非韦伦相关的临床试验

NCT06914869

/ Completed临床1期

A Phase I, Randomized, Open-label, Drug-drug Interaction Study to Assess the Effect of Multiple Doses of a Moderate and a Strong CYP3A Inducer on the Pharmacokinetics and Safety of Mavorixafor in Healthy Male and Female Participants

The main purpose of this study is to evaluate drug-drug interaction (DDI) of orally administered mavorixafor with cytochrome P3A (CYP3A) inducers carbamazepine (a strong CYP3A inducer) or efavirenz (a moderate CYP3A inducer) in healthy male and female participants.

开始日期2025-02-18

申办/合作机构

X4 Pharmaceuticals, Inc.

NCT06797674

/ Active, not recruiting临床1期

A Clinical Study to Evaluate the Effect of Multiple Doses of Efavirenz on Single-Dose Pharmacokinetics of MK-7602 in Healthy Participants

The goal of the study is to learn what happens to levels of MK-7602 in a healthy person's body over time. Researchers will compare what happens to MK-7602 in the body when it is given with or without another medicine called efavirenz, and when it is given with or without a meal.

开始日期2025-02-10

申办/合作机构

Merck Sharp & Dohme LLC

NCT06823596

/ RecruitingN/AIIT

Short-term Addition of Efavirenz to Induce CARD8-mediated Reduction of Persistent Nonsuppressible HIV Viremia in People with High Adherence to ART.

Antiretroviral therapy or ART blocks HIV replication reducing plasma viral loads to undetectable levels but has no effect on persistently infected cells in the body, called the virus reservoir. These cells carry infectious HIV capable of restarting HIV replication if therapy is stopped. The reservoir is so stable forcing people to adhere life-long ART. Over 5% of ART adherent individuals continue to have residual non-suppressive viremia (NSV) detected by clinical assays (40-400 copies/ml). Residual viremia reflects a more persistent reservoir and has the potential for increased morbidity. For eg., persistent expression of HIV proteins contributes to inflammation, and can lead to comorbidities. Recently, a novel way to target this reservoir called "TACK" or "Targeted activator of cell killing" is proposed. TACK compounds only target HIV infected cells and directly kill them by inducing a natural killing program (called the inflammasome). Recently the HIV drug, Efavirenz (EFV), which was used to suppress HIV replication for decades, has now been shown to also be a TACK compound. This pilot study will evaluate the impact of Efavirenz (EFV) in reducing HIV persistence by its ability to be a TACK molecule. So in addition to blocking HIV growth, this compound when added to a current ART regimen can kill HIV infected cells in the test tube. We aim to harness this effect to determine whether the addition of EFV to the current ART regimen in people with NSV can suppress the viremia to undetectable levels by killing those cells. NSV represents the "the tip of the iceberg" of those with bigger reservoirs and represents a challenging clinical scenario in dire need of new diagnostic and therapeutic options.
This pilot study will spark larger clinical trials to advance HIV cure strategies, and will provide new tools to improve the clinical management of people living with HIV.

开始日期2025-01-14

申办/合作机构

University of Toronto

[+1]

100 项与依非韦伦相关的临床结果

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100 项与依非韦伦相关的转化医学

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100 项与依非韦伦相关的专利（医药）

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8,484

项与依非韦伦相关的文献（医药）

2025-12-31·HIV Research & Clinical Practice

A combined prospective and retrospective comparative study evaluating renal outcomes after switching from TDF + FTC + EFV to TDF/3TC/DTG (TLD) vs. DTG + 3TC in virologically suppressed Thai people with HIV

Article

作者: Putcharoen, Opass ; Kanogtorn, Sathaporn ; Burimat, Phattarapon ; Patamatamkul, Samadhi

BACKGROUND:

TDF/3TC/DTG (TLD) has been adopted as the first-line therapy for all people with HIV according to the WHO 2019 and Thai HIV guidelines. As a result, people with HIV in Thailand on TDF/FTC/EFV are switched to TLD. However, increasing data demonstrate the efficacy and renal safety of the TDF-sparing dual therapy with DTG + 3TC compared with TDF-based combination ART (cART) as a switching therapy. A direct comparison of estimated glomerular filtration rates (eGFR) among people with HIV treated with TDF-based regimens who switch to TLD vs. DTG + 3TC is yet to be made.

METHODS:

We enrolled virologically suppressed people with HIV aged ≥18 years currently on TDF + FTC + EFV to either switch to TLD or DTG + 3TC at two tertiary care hospitals. The switching regimen was chosen at the physicians' discretion. The primary outcome was the change in eGFR, calculated by creatinine at 24 weeks. Secondary outcomes included changes in LDL, body weight, and BMI at 24 weeks.

RESULTS:

Among 53 recruited participants, 28 and 15 completed the second follow-up in the TLD and DTG + 3TC groups, respectively. The mean age was higher in the TLD group compared to the DTG + 3TC group (Table 1). The median time from HIV diagnosis to switching was 8.5 years. The eGFR reduction was significantly greater in the TLD group than in the DTG + 3TC group: -17.24 ± 9.24 vs. -8.4 ± 9.03 mL/min/1.73 m² (p = 0.004). All participants in both groups achieved virological suppression. There was no significant change in CD4 counts between the two groups. Switching to DTG + 3TC was associated with a significantly smaller decline in eGFR post-switch (mean difference: 6.216 mL/min/1.73 m²; 95% CI 0.169-12.263; p = 0.044) compared to those who switched to TLD.

CONCLUSIONS:

There was a significant reduction in eGFR among people with HIV who switched to TLD compared to those switched to DTG + 3TC. Changes in LDL and BMI were comparable between groups. Dual therapy with DTG + 3TC may be a preferred switching option over TLD for individuals with renal safety concerns. Further randomized prospective trials with longer follow-up are warranted to confirm these findings.

2025-10-01·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel diarypyrimidine derivatives as potent HIV-1 NNRTIs by exploiting the tolerant region I within NNRTI binding pocket

Article

作者: De Clercq, Erik ; Kang, Dongwei ; Gao, Zhen ; Jiang, Xiangyi ; Liu, Xinyong ; Gao, Heng ; Pannecouque, Christophe ; Zhan, Peng ; Ji, Xiangkai

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) serve as an essential component of antiretroviral treatment regimens, but they encounter challenges such as resistance mutations, poor solubility, and adverse effects. This study presents the design, synthesis, and biological evaluation of novel diarylpyrimidine (DAPY)-typed derivatives targeting the tolerant region I within the NNRTI binding pocket (NNIBP). We introduced aliphatic ring structures with high Fsp³ value, aiming to enhance target affinity while simultaneously improving water solubility. Among them, compound 9k demonstrated excellent potency against wild-type HIV-1 (EC₅₀ = 0.0014 μM) and key single-mutant strains K103 N (EC₅₀ = 0.0041 μM) and E138K (EC₅₀ = 0.0077 μM), which outperformed the positive drugs ETR, NVP and EFV. Molecular modeling studies were conducted to elucidate the detailed interactions between RT and 9k, providing insights into the enhanced drug resistance profiles. Additionally, 9k demonstrated a notable improvement in water solubility (1.38 μg/mL, pH = 7) compared to ETR (≪ 1 μg/mL, pH = 7). These findings provide a foundation for further optimization of NNRTIs with improved anti-resistance profiles and pharmacokinetics.

2025-09-01·The Lancet regional health. Southeast Asia

Drug resistance mutations among people living with HIV and ART failure in Bangladesh: a cross-sectional study

Article

作者: Fakhruddin, Mohammad ; Rahman, Mustafizur ; Rahman, Sezanur ; Sarker, Md Safiullah ; Hossain, Md Abir ; Howlader, Rubel ; Sarwar, Golam ; Khan, Sharful Islam ; Hossain, Md Mobarok

Background:

While maintaining a low HIV prevalence among the general population, Bangladesh is among the few countries in the Asia-Pacific region where the incidence of people living with HIV (PLWH) continues to increase. The National Anti-Retroviral Therapy Program still relies on a 'Test and Treat' strategy and faces challenges in treating drug-resistant HIV. This study aims to assess the HIV viral load and drug resistance mutations among key populations (KPs) under anti-retroviral therapy (ART) in Bangladesh.

Methods:

A total of 110 KPs from 20 drop-in-centers across 11 districts in Bangladesh were enrolled from March 2019 to November 2020 for viral load (VL) testing using Xpert® HIV-1 Viral Load kits. Samples with high VL (≥1000 copies/mL) underwent pol gene sequencing to identify drug resistance mutations.

Findings:

Most of the participants were men who have sex with men (MSM, 49.1%) followed by men sex workers (MSW, 34.5%), and transgender women (TGW, 13.6%). The median age of the participants was 28 years (IQR: 24-35) and 80% of them were from the capital city, Dhaka. The median time for ART was 11.5 months (IQR: 4.5-29.1), where 15 participants were naïve to ART. Overall, high VL was observed in 23.8%, and virologic failure was in 17.9% among PLWH who were treated for >30 days. HIV-1 subtype C was predominant (43.8%), followed by A1 (25%), CRF01_AE (25%), and CRF02_AG (6.2%). Seven participants showed resistance against Efavirenz, the common drug received from ART centres, and three of them were additionally resistant against Tenofovir Disoproxil Fumarate. Other drugs supplied by ART centres were also found resistant for participants; i.e. 6 against Emtricitabine, 6 against Lamivudine, and 1 against Etravirine. The spatial distribution indicated HIV transmission occurred within and between KPs and drop-in-centers. Additionally, samples that received different ART also clustered together.

Interpretation:

Evidence suggests that KPs are at a higher risk of virologic failure in Bangladesh, emphasizing the need for routine VL and drug resistance mutation tests as part of the national ART program. This study also advocates for exploring barriers to ART adherence and implementing personalized ART strategies in national ART programs.

Funding:

The Global Fund.

项与依非韦伦相关的新闻（医药）

2025-08-01

·ChenFJMU

新药速递｜2025年7月FDA批准上市5款新药①【解读：从剂型，到临床药理，到合理用药】

ChenFJMU团队编辑（原创）思语湖畔QuoteProgress equals happiness. — Tony RobbinsFDA新药速递【25年7月】看点FDA于2025年7月批准5款新药，分别为治疗复发或难治性多发性骨髓瘤的Lynozyfic；治疗非小细胞肺癌的激酶抑制剂Zegfrovy；治疗遗传性血管性水肿急性发作的血浆激肽释放酶抑制剂Ekterly；治疗成人中重度慢性手部湿疹的Anzupgo；用于治疗成人和儿童苯丙酮尿症患者的高苯丙氨酸血症的Sephience。01针对复发难治性多发性骨髓瘤，双抗Lynozyfic携卓越缓解率重磅登场。02“国产之光”Zegfrovy，精准突破EGFR exon20插入突变困境，为非小细胞肺癌患者点亮新生希望！03首款口服血浆激肽释放酶抑制剂Ekterly获批上市，开启遗传性血管性水肿急性发作治疗新范式。04当皮质类固醇不合适？首款Anzupgo乳膏为慢性手部湿疹支招。05苯丙酮尿症患者的新希望！Sephience降低苯丙酮尿症患者的血液苯丙氨酸水平。细说FDA新药【25年7月】（ChenFJMU）Lynozyfic，01Lynozyfic（Linvoseltamab-gcpt，利诺泽单抗），由再生元制药公司研发，于2025年7月2日获FDA批准上市，是一款靶向B细胞成熟抗原（BCMA）和CD3 T细胞衔接的双特异性抗体，适用于既往已接受过至少四线治疗（包括蛋白酶体抑制剂、免疫调节剂以及抗CD38单克隆抗体）的复发或难治性多发性骨髓瘤成人患者。【黑框警告】细胞因子释放综合征（CRS）：接受Lynozyfic治疗的患者可能发生 CRS，临床体征和症状包括但不限于发热、寒战、缺氧、心动过速和低血压。为降低CRS风险，应采用Lynozyfic递增给药方案开始治疗。一旦出现CRS，应暂停用药直至症状缓解，并根据严重程度调整后续剂量或永久停药。神经系统毒性：接受Lynozyfic治疗的患者可能发生包括免疫效应细胞相关神经毒性综合征（ICANS）在内的严重或致命神经系统毒性。ICANS最常见的临床体征和症状是意识模糊、意识水平降低和嗜睡。治疗期间需密切监测是否出现神经系统毒性的体征或症状。一旦发生神经系统毒性，应暂停用药直至症状缓解，根据严重程度调整后续剂量或永久停药。【结构与剂型处方】Linvoseltamab-gcpt是一种靶向B细胞成熟抗原（BCMA）和CD3 T细胞的双特异性抗体，为重组人源化IgG4单克隆抗体。该药采用重组 DNA技术，于中国仓鼠卵巢（CHO）细胞悬浮培养体系中生产，分子量约146 kDa。Lynozyfic静脉注射用制剂为无菌、无防腐剂、澄清至微乳光、无色至淡黄色的溶液，pH值为6.0。每个Lynozyfic 5 mg/2.5 mL小瓶含5 mg Linvoseltamab-gcpt（浓度：2 mg/mL）。辅料：组氨酸（0.7 mg/mL）、L-组氨酸盐酸盐一水合物（1.1 mg/mL）、聚山梨酯80（1 mg/mL）、蔗糖（100 mg/mL）、注射用水（USP标准）。每个Lynozyfic 200 mg/10 mL小瓶含200 mg Linvoseltamab-gcpt（浓度：20 mg/mL）。辅料：组氨酸（0.7 mg/mL）、L-组氨酸盐酸盐一水合物（1.1 mg/mL）、聚山梨酯80（1 mg/mL）、蔗糖（100 mg/mL）、注射用水（USP标准）。【作用机制】B细胞成熟抗原（BCMA）是肿瘤坏死因子受体（TNF）超家族中的一员，高度表达于多发性骨髓瘤细胞表面，作为肿瘤存活和增殖的关键受体。CD3是T细胞受体（TCR）复合物的重要组成部分，参与T细胞活化信号传导。Linvoseltamab作为一种双特异性抗体，其一边结合多发性骨髓瘤细胞表面上高表达的BCMA，一边结合T细胞上的CD3受体，将细胞毒性T细胞定向募集到肿瘤细胞附近。CD3的结合模拟TCR的自然激活信号，以致活化的T细胞释放穿孔素和颗粒酶，诱导肿瘤细胞凋亡。同时分泌促炎细胞因子（如IFN-γ、TNF-α），进一步强化抗肿瘤免疫反应。【药效学及药代动力学】药效学：在复发性或难治性多发性骨髓瘤患者中，与50 mg每周一次（推荐剂量的0.25倍）给药方案相比，200 mg每周一次给药方案的客观缓解率和完全缓解率更好。尚未充分表征Linvoseltamab-gcpt的暴露-效应关系。短暂性循环细胞因子（IL-2、IL-6和IFN-γ）水平升高主要出现在剂量递增方案期间和首次接受200 mg全剂量给药时，细胞因子水平通常在每次输注后4 h达到峰值，随后逐渐回落。药代动力学：药代动力学（PK）参数在复发/难治性多发性骨髓瘤患者中，按推荐剂量进行评估；如无特别说明，均以几何均值（变异系数 CV%）表示。按推荐给药方案用药后，Linvoseltamab-gcpt的PK暴露数据汇总于表9。在96 mg至800 mg剂量范围内（相当于推荐全剂量 200 mg的0.48–4倍），Linvoseltamab-gcpt的谷浓度（Ctrough）随剂量增加呈高于比例关系的上升。Linvoseltamab-gcpt的最大浓度（Cmax）为127 mg/L（CV 51%），于每两周给药方案首次剂量（即第12次给予200 mg）后达到。表9 Linvoseltamab-gcpt按推荐剂量给药后的几何平均值（变异系数CV%）暴露数据分布：Linvoseltamab-gcpt分布容积（Vd）为7.05 L（33.6%）。消除：Linvoseltamab-gcpt的清除率在基线时为 0.68 L/d（CV 52.2%），稳态时降至 0.43 L/d（CV 83.8%）。其随时间推移而降低的原因在于，药物的消除由两条并行途径共同介导：线性、不可饱和的分解代谢途径；非线性、可饱和的靶点介导途径。停药后，患者体内药物浓度将从Cmax下降97%，所需中位时间为77.7 d（范围18–154 d）。代谢：预计Linvoseltamab-gcpt通过分解代谢途径代谢为小肽。特殊人群用药：①轻度至中度肾功能不全、轻度肝功能不全：Linvoseltamab-gcpt 的药代动力学未观察到具有临床意义的差异;②重度肾功能不全、终末期肾病以及中度至重度肝功能不全： Linvoseltamab-gcpt药代动力学的影响尚不明确。免疫原性：接受 Lynozyfic治疗的192例患者中有1%（2/192）检测到抗Linvoseltamab-gcpt抗体。鉴于抗药物抗体（ADA）发生率极低，目前尚不清楚这些抗体是否会对Linvoseltamab系列产品的药代动力学、药效学、安全性或疗效产生影响。【非临床毒理学】尚未对Linvoseltamab-gcpt生殖毒性、致癌性、遗传毒性进行研究。【临床研究】Lynozyfic的疗效在一项开放标签、多中心、多队列研究LINKER-MM1（NCT03761108）中，针对复发/难治性多发性骨髓瘤患者进行评估。研究纳入80位既往接受过蛋白酶体抑制剂（PI）、免疫调节剂（IMiD）和抗CD38单克隆抗体治疗的多发性骨髓瘤患者。治疗方案采用剂量递增给药：第1天静脉输注5 mg，第8天25 mg，第15天首次治疗剂量200 mg。随后从第4周至第13周每周给药200 mg，改为每两周一次200 mg。至少24周后，达到非常好部分缓解（VGPR）或更佳疗效的II期患者调整为每4周给药200 mg。治疗持续至疾病进展或出现不可耐受毒性。疗效评估基于盲态独立评审委员会（IRC）采用国际骨髓瘤工作组（IMWG）标准判定的客观缓解率（见表10）。中位首次缓解时间为 0.95个月（0.5–6个月）。客观缓解率（ORR）达70%（56/80），95%置信区间（59%-80%），表明超过三分之二的患者对治疗有明确反应，疗效显著。深度缓解（CR或更高）比例为45%（36/80），其中严格完全缓解（sCR）占39%，表明药物可诱导高质量的缓解。【用药指南】Zegfrovy，02Zegfrovy（Sunvozertinib，舒沃替尼），由中国🇨🇳迪哲医药公司研发，于2025年7月2日获FDA批准上市，是一种用于治疗伴有表皮生长因子受体（EGFR）20号外显子插入突变的局部晚期或转移性非小细胞肺癌（NSCLC）成人患者的激酶抑制剂。【结构与剂型处方】Zegfrovy（Sunvozertinib）是一种激酶抑制剂，分子式为C29H35 ClFN7O3，分子量为584.09 g/mol。Sunvozertinib的化学名称为N{5-[（4-{[5-氯-4-氟-2-（1-羟基-1-甲基乙基）苯基]氨基}嘧啶-2-基）氨基]-2-[（3R）-3（二甲基氨基）吡咯烷-1-基]-4-甲氧基苯基}丙-2-烯酰胺。Sunvozertinib具有一个R-构型的手性碳，结构如下图所示：Zegfrovy片剂含有150 mg或200 mg活性成分Sunvozertinib。片剂核心的辅料包括：胶态二氧化硅、交联羧甲纤维素钠、羟丙基纤维素、一水乳糖、硬脂酸镁以及微晶纤维素。薄膜包衣层由羟丙甲纤维素2910、氧化铁黄、二氧化钛和三醋酸甘油酯组成。【作用机制】EGFR exon20插入突变（EGFR exon20ins）是非小细胞肺癌（NSCLC）中一种较为罕见的EGFR基因突变类型，占所有EGFR突变的4%-12%。Sunvozertinib是一种口服、强效、不可逆、选择性的EGFR酪氨酸激酶抑制剂（TKI），主要针对EGFR外显子20插入突变以及EGFR敏感突变、T790M耐药突变和罕见突变，对野生型EGFR活性较弱。通过特异性结合EGFR exon20ins蛋白的ATP结合位点，抑制其异常激活的酪氨酸激酶活性，从而阻断下游信号通路（如RAS/RAF/MEK/ERK、PI3K/AKT/mTOR等），抑制肿瘤细胞增殖并诱导凋亡。【药效学及药代动力学】药效学：暴露-效应关系：在Sunvozertinib200 mg至300 mg（即获批推荐剂量的1.5倍）的暴露范围内，未观察到总体缓解率（ORR）存在具有临床意义的暴露-效应关系。心脏电生理：在1.5倍批准推荐剂量下，未观察到具有临床意义的QTc间期延长。药代动力学：在获批推荐剂量下观察Sunvozertinib稳态药代动力学参数（除特别说明外，数据均以几何平均数CV%表示）：Sunvozertinib全身总暴露量（AUC）和最大血药浓度（Cmax）在50毫克（获批推荐剂量的0.25倍）至400 mg（2倍推荐剂量）范围内呈近似剂量比例性增加。稳态血药浓度在15天内达成，AUC平均蓄积倍数约为3倍。稳态时舒沃替尼的Cmax和AUC分别为412（45%）ng/mL和8060（42%）h*ng/mL。吸收：Sunvozertinib达到最大血药浓度的中位时间tmax约为6 h。分布：表观（口服）分布容积为2116 L（81%）。体外Sunvozertinib血浆蛋白结合率约为89%-94%消除：Sunvozertinib的消除半衰期为50小时（27%），表观（口服）清除率为29 L/h（54%）。代谢：Sunvozertinib主要通过CYP3A酶代谢，生成具有药理活性的去甲基化代谢产物DZ0753。该代谢产物的血药浓度-时间曲线下面积（AUC）约为原型药物AUC的10%。排泄：单次口服放射性标记的Sunvozertinib后，79%的给药剂量经粪便排泄（其中7.3%为原型药物），10%经尿液排泄（5.6%为原型药物）。特殊用药人群：①轻度至中度肾功能、肝功能不全：Sunvozertinib的药代动力学未观察到具有临床意义的差异;②严重肝、肾功能不全：Sunvozertinib药代动力学的影响尚不明确。药物相互作用：[临床研究与模型分析结果]①强效CYP3A抑制剂：联合使用伊曲康唑（强效CYP3A抑制剂，200 mg每日一次）时，Sunvozertinib的AUC增加1.5倍，Cmax增加1.3倍。②强效及中效CYP3A诱导剂：联合使用卡马西平（强效CYP3A诱导剂，300 mg每日两次）时，Sunvozertinib的AUC降低48%，Cmax降低38%。模型预测，联合使用依非韦伦（中效CYP3A诱导剂，600 mg每日一次）时，Sunvozertinib的AUC预计降低44%。③CYP3A底物：联合使用Zegfrovy时，咪达唑仑（敏感CYP3A底物）的AUC降低23%，Cmax降低15%。④P-糖蛋白（P-gp）底物：联合使用Zegfrovy时，地高辛（P-gp底物）的AUC增加1.4倍，Cmax增加1.2倍。⑤BCRP底物：联合使用Zegfrovy时，瑞舒伐他汀（BCRP底物）的AUC增加1.4倍，Cmax增加1.6倍。[其他药物]①联合使用氟康唑（中效CYP3A抑制剂，200 mg每日一次）、地塞米松（弱效CYP3A诱导剂，8 mg每日一次）或抑酸剂（如质子泵抑制剂）对Sunvozertinib的药代动力学无临床显著影响。②地昔帕明（CYP2D6底物）：与Zegfrovy合用时，预计不会对地昔帕明的药代动力学产生具有临床意义的影响。[体外研究]①CYP450酶：Sunvozertinib诱导CYP2C8。②转运蛋白系统：Sunvozertinib是P-gp的底物。Sunvozertinib抑制OATP1B1。【非临床毒理学】Sunvozertinib无遗传毒性，尚未进行致癌性、生殖毒性研究。【临床研究】Zegfrovy的疗效评估基于WU-KONG1B研究（NCT03974022），该研究为一项多中心、开放标签、随机剂量临床试验。研究纳入85位经铂类化疗后疾病进展的EGFR外显子20插入突变局部晚期或转移性非小细胞肺癌（NSCLC）患者。主要疗效终点指标为观缓解率（ORR），另一项疗效终点指标为缓解持续时间（DOR）。客观缓解率（ORR）达46%（95% CI：35–57），说明近半数患者在Zegfrovy治疗后肿瘤显著缩小。中位缓解持续时间（DOR）为11.1个月（95% CI：8.2-NE），缓解患者的疗效平均维持近1年，部分患者可能获益更久。72%的患者DOR≥6个月，说明超七成患者的药效可维持半年以上。【用药指南】Ekterly，03Ekterly（Sebetralstat，塞贝特拉司他），由美国KalVista制药公司研发，于2025年7月3日获FDA批准上市，适用于治疗12岁及以上成人和儿科患者的遗传性血管性水肿（HAE）急性发作。【结构与剂型处方】Sebetralstat为白色至类白色结晶粉末，微溶于乙醇、丙酮和异丙醇，几乎不溶于水。分子式为C26H26FN5O4，分子量为491.5，化学名称为N-[（3-氟-4-甲氧基吡啶-2-基）甲基]-3-（甲氧基甲基）-1-（{4-[（2氧代-1，2-二氢吡啶-1-基）甲基]苯基}甲基）-1H-吡唑-4-甲酰胺。化学结构为：Ekterly是一种300 mg口服薄膜包衣片，活性成分为血浆激肽释放酶抑制剂Sebetralstat。非活性成分为交联羧甲纤维素钠、甘油辛酸癸酸酯、瓜尔胶/瓜尔半乳甘露聚糖、羟丙甲纤维素、氧化铁黑、氧化铁黄、聚乙二醇聚乙烯醇接枝共聚物、硬脂酸镁、麦芽糊精、中链甘油三酯、微晶纤维素、聚乙烯醇、聚维酮、滑石粉和二氧化钛。【作用机制】血浆激肽释放酶(plasma kallikrein, PKa)是一种丝氨酸蛋白酶，可切割高分子量激肽原（HK），释放能引起血管通透性增加，导致炎症和水肿的缓激肽（BK）。Sebetralstat作为一种竞争性、可逆的血浆激肽释放酶抑制剂。通过抑制HK的切割，减少缓激肽BK的生成，从而治疗遗传性血管性水肿（HAE）急性发作的临床症状。此外，Sebetralstat还通过抑制血浆激肽释放酶对激肽释放酶-激肽系统的正反馈作用，减少XIIa因子的活化及后续血浆激肽释放酶的生成。激肽释放酶-激肽系统的激活（Davie Rebecca L, et al. Journal of medicinal chemistry, 2022, 65 (20).）【药效学及药代动力学】药效学：在探索性实验中观察到，血浆激肽释放酶的抑制呈浓度依赖性，表现为其特异性酶活性较基线的降低。健康受试者单次口服600 mg Sebetralstat后，自给药后30 min起即可观察到血浆激肽释放酶活性平均抑制率超过90%，并持续至给药后约6 h。心脏电生理：在健康受试者中，给予Sebetralstat（为最大推荐剂量的 2.5倍）后，QTc间期平均最大延长为10.4 msec（置信区间上限为15.3 msec）。QTc间期的延长呈浓度依赖性。药代动力学：在遗传性血管性水肿（HAE）患者中，单次口服600 mg Sebetralstat后，其几何平均（变异系数CV%）Cmax为6080 ng/mL（40%），AUC0-inf为17600 ng·h/mL（36%）。若在第一剂给药3 h后再次口服600 mg，第二剂的Cmax单剂仅升高10%，而AUC0-inf则增加90%。健康受试者与HAE患者之间的Sebetralstat药代动力学无临床相关差异。吸收：单次口服600 mg Sebetralstat后，血药浓度达峰的中位时间约为 1 h。分布：Sebetralstat 的表观分布容积（Vz/F）估计值为70.1 L（95% CI：64.8，75.4）。其体外血浆蛋白结合率为77%。消除：单次口服600 mg Sebetralstat 后，其平均（SD）消除半衰期为 5.3（2.3）至 8.9（5.1）h；典型表观清除率（CL/F）估计值为 30.7 L/h（95% CI：29.1，32.2）。代谢：Sebetralstat主要由CYP3A4代谢，其次由CYP2C8代谢。排泄：健康男性受试者单次口服600 mg放射性标记Sebetralstat后，约63%的剂量经粪便排出（12.5%为原型药物），32%经尿液排出（8.7%为原型药物）。特殊人群用药：①轻度肾功能不全：Sebetralstat的药代动力学未观察到具有临床意义的差异;②中度至重度肾功能不全：Sebetralstat药代动力学的影响尚不明确。③轻度肝功能不全：与肝功能正常受试者相比，Cmax升高7%，AUC升高16%。④中度肝功能不全：与肝功能正常受试者相比，Cmax升高63%，AUC升高100%。⑤重度肝功能不全：对Sebetralstat 药代动力学的影响尚不明确。药物相互作用：[临床研究与模型分析结果]①强效CYP3A4抑制剂：联合使用伊曲康唑（强效CYP3A4抑制剂, 200 mg每日一次）给药6天后，Sebetralstat的Cmax增加2.4倍，AUC0-inf增加5.2倍。②中效CYP3A4抑制剂：联合使用维拉帕米（中效CYP3A4抑制剂，240 mg每日一次）给药6天后，Sebetralstat的Cmax增加1.8倍，AUC0-inf增加2倍。③强效CYP3A4诱导剂：联合使用苯妥英（强效CYP3A4诱导剂，100 mg每日三次）给药15天后，Sebetralstat的Cmax降低66%，AUC0-inf降低83%。④中效CYP3A4诱导剂：联合使用依非韦伦（中效CYP3A4诱导剂，600 mg每日一次）给药14天后，Sebetralstat的Cmax降低63%，AUC0-inf降低79%。⑤抑酸剂：与pH 0.5相比，在pH 6时Sebetralstat的Cmax预计最多降低56%，AUC0-inf预计最多降低30%。[其他药物]当与奎尼丁（P-gp抑制剂）、艾曲泊帕（BCRP抑制剂）、西咪替丁（评估为弱CYP3A4抑制剂）或莫达非尼伴随给药时，未观察到Sebetralstat药代动力学的临床显著差异。[体外研究]CYP450酶系统：①底物特性：Sebetralstat是CYP3A4和CYP2C8的底物，而非CYP1A2、CYP2A6、CYP2B6、CYP2C9、CYP2C19、CYP2D6或CYP2E1的底物。②抑制作用：Sebetralstat可抑制CYP2C9和CYP3A4，但对CYP1A2、CYP2B6、CYP2C8、CYP2C19及CYP2D6无抑制作用。转运体系统：①底物特性：Sebetralstat是P-gp和BCRP的底物，而非OATP1B1、OATP1B3、OAT1、OAT3、OCT2或MATE1的底物。②抑制作用：Sebetralstat可抑制BCRP、OATP1B1、OATP1B3、OAT3、OCT2、MATE1、MATE2-K及BSEP，但对P-gp和OAT1无抑制作用。【非临床毒理学】无致癌性、致突变性、生殖毒性。【临床研究】在一项双盲、随机、安慰剂对照、多中心交叉临床试验（KONFIDENT [NCT05259917]）中评估Ekterly治疗成人和12岁及以上儿童遗传性血管性水肿（HAE）急性发作的疗效。研究纳入110名患者，采用三向完全交叉设计，比较Ekterly 600 mg、Ekterly 300 mg与安慰剂的效果。研究的主要终点为“症状开始缓解时间”，定义为首次给药后12 h内，患者通过七级量表《患者整体印象变化量表（PGI-C）》（评分范围从“明显加重”到“明显改善”）连续两次评估至少达到“稍有好转”。如图1所示，与安慰剂相比，Ekterly 600 mg在症状缓解起始时间上显著更快。93例接受Ekterly 600 mg治疗的患者中共有71例（76%），而84例接受安慰剂治疗的患者中共有41例（49%）达到主要终点。首次给药后12 h内，Ekterly 600 mg组患者症状缓解起始时间的中位数为2 h（95% CI：1.5-2.8）。首个关键次要终点为“症状严重程度首次减轻时间”，定义为首次给药后12 h内，患者通过五级量表《患者整体严重程度评分（PGI-S）》（评分范围从“无症状”至“严重”）连续两次评估出现严重程度降低。如图2所示，与安慰剂相比，Ekterly 600 mg严重程度首次出现减轻的时间显著缩短。93例接受Ekterly 600 mg治疗的患者中共有49例（53%），而84例接受安慰剂治疗的患者中共有26例（31%）在12 h内达到严重程度减轻。Ekterly 600 mg组患者达到该终点的中位时间为9.1 h（95% CI：3.8-未达到）。第二个关键次要终点为“发作完全消退时间”，定义为首次给药后24 h内患者整体严重程度评分（PGI-S）达到“无症状”。如图3所示，与安慰剂相比，Ekterly 600 mg在“发作消退时间”上显著更快。93例接受Ekterly 600 mg治疗的患者中共有46例（49%），而84例接受安慰剂治疗的患者中共有23例（27%）在24 h内实现发作消退。【用药指南】编辑：周纯情排版：周纯情补充和审核：陈昌买推送：ChenFJMU（欢迎个人转发分享，企业及其他公众号需授权后转载，并注明出处！）

上市批准免疫疗法

2025-07-25

·ir.kalvista.com

KalVista Pharmaceuticals Receives Positive CHMP Opinion for Sebetralstat for the Treatment of Hereditary Angioedema Attacks

If approved, sebetralstat will be the first and only oral on-demand treatment for HAE in the European Union (EU) European Commission decision expected by early October 2025 CAMBRIDGE, Mass. & SALISBURY, England--(BUSINESS WIRE)--Jul. 25, 2025-- KalVista Pharmaceuticals, Inc. (Nasdaq: KALV) today announced that the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) has adopted a positive opinion recommending marketing authorization for sebetralstat, a novel oral plasma kallikrein inhibitor, for symptomatic treatment of acute attacks of hereditary angioedema (HAE) in adults and adolescents aged 12 years and older. The European Commission (EC) final decision is expected by early October. “This positive CHMP opinion is an important step forward for people living with HAE in Europe, where there remains a high need for effective, easy-to-administer on-demand treatments,” said Ben Palleiko, CEO of KalVista. “Coming just weeks after regulatory approvals in the US and UK, this milestone highlights the potential of sebetralstat to transform how HAE is managed globally. Sebetralstat is expected to become the first and only oral on-demand treatment for HAE available in Europe, bringing forward a new treatment approach that enables adherence to guidelines and empowers people to treat attacks quickly, wherever they occur.” The CHMP based its opinion on results from the phase 3 KONFIDENT clinical trial, which was the largest clinical trial ever conducted in HAE. Data from KONFIDENT was published in the New England Journal of Medicine in May 2024, showing that sebetralstat achieved significantly faster symptom relief, reduction in attack severity and attack resolution than placebo, and was well-tolerated with a safety profile similar to placebo.1 The trial randomized 136 HAE patients from 66 clinical sites across 20 countries. “Access to on-demand treatments that offer easy self-administration and rapid symptom relief is critical for patients living with HAE,” said Emel Aygören-Pürsün, M.D., Assistant Professor, Internal Medicine and Hemostaseology, Department for Children and Adolescents, University Hospital Frankfurt. “Until now, on-demand therapies for HAE attacks required parenteral administration via injections. The positive CHMP opinion for sebetralstat is an essential move toward a novel, long-awaited oral on-demand option that could help patients treat attacks early and independently, as advocated by guidelines, with the goal of improving outcomes and normalizing lives.” Sebetralstat is approved in the United States and United Kingdom under the brand name EKTERLY® for the treatment of HAE attacks in people 12 years of age and older. It is currently under review with regulatory authorities in Japan as well as multiple other territories. About Hereditary Angioedema Hereditary angioedema (HAE) is a rare genetic disease resulting in deficiency or dysfunction in the C1 esterase inhibitor (C1INH) protein and subsequent uncontrolled activation of the kallikrein-kinin system. People living with HAE experience painful and debilitating attacks of tissue swelling in various locations of the body that can be life-threatening depending on the area affected. Treatment guidelines recommend treating attacks as early as possible to prevent progression of swelling and shorten the time to attack resolution, and to consider treatment for all attacks, regardless of anatomic location or severity. About Sebetralstat Sebetralstat is a novel plasma kallikrein inhibitor approved in the United States and United Kingdom for the treatment of acute attacks of hereditary angioedema (HAE) in people 12 years of age and older. It is the first and only oral on-demand treatment for HAE. With ongoing studies exploring its use in children aged two to 11 and multiple regulatory applications under review in key global markets, sebetralstat has the potential to become the foundational therapy for HAE management worldwide. U.S. INDICATION AND IMPORTANT SAFETY INFORMATION What is EKTERLY® (sebetralstat)? EKTERLY is a prescription medicine used to treat sudden (acute) attacks of hereditary angioedema (HAE) in adults and children aged 12 years of age and older. It is not known if EKTERLY is safe and effective in children under 12 years of age. IMPORTANT SAFETY INFORMATION Before taking EKTERLY, tell your healthcare provider about all of your medical conditions, including if you: Are pregnant or planning to become pregnant. It is not known if EKTERLY can harm your unborn baby. Are breastfeeding or plan to breastfeed. It is not known if EKTERLY passes into your breast milk. Talk to your healthcare provider about the best way to feed your baby while taking EKTERLY. Have liver problems. Tell your healthcare provider about all of the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Taking EKTERLY with certain other medicines can cause side effects or affect how well EKTERLY or the other medicines work. Especially tell your healthcare provider if you take any of the following, as their use with EKTERLY is not recommended: itraconazole, phenytoin, efavirenz. Know the medicines you take. Keep a list of them to show your healthcare provider or pharmacist when you get a new medicine. What are the possible side effects of EKTERLY? The most common side effects of EKTERLY include headache. For more information, ask your healthcare provider or pharmacist. Talk to your doctor for medical advice about side effects. You are encouraged to report side effects related to KalVista products by calling 1-855-258-4782. If you prefer, you may contact the U.S. Food and Drug Administration (FDA) directly. Visit www.fda.gov/medwatch or call 1-800-FDA-1088. Please click here for full Prescribing Information, including Patient Information. About KalVista Pharmaceuticals, Inc. KalVista Pharmaceuticals, Inc., is a global biopharmaceutical company dedicated to developing and delivering life-changing oral therapies for individuals affected by rare diseases with significant unmet needs. In the U.S., KalVista markets EKTERLY®, the first and only oral on-demand treatment for hereditary angioedema (HAE). The Company has multiple regulatory applications under review in key global markets. For more information about KalVista, please visit www.kalvista.com and follow us on LinkedIn, X, Facebook and Instagram. Forward-Looking Statements This press release contains "forward-looking" statements within the meaning of the safe harbor provisions of the U.S. Private Securities Litigation Reform Act of 1995. Forward-looking statements can be identified by words such as: "anticipate," "intend," "plan," "goal," "seek," "believe," "project," "estimate," "expect," "strategy," "future," "likely," "may," "should," "will" and similar references to future periods. These statements are subject to numerous risks and uncertainties that could cause actual results to differ materially from what we expect. Examples of forward-looking statements include, among others, information relating to our business and business plans, the success of our efforts to commercialize EKTERLY® (sebetralstat), our ability to successfully obtain foreign regulatory approvals for sebetralstat, including approval by the EC, our expectations about the timing of the EC’s final decision, our expectations about the safety and efficacy of sebetralstat and our other product candidates, the timing of clinical trials and their results, our ability to commence clinical studies or complete ongoing clinical studies, including our KONFIDENT-S and KONFIDENT-KID trials, and the ability of EKTERLY to treat HAE. Further information on potential risk factors that could affect our business and financial results are detailed in our filings with the Securities and Exchange Commission, including in our annual report on Form 10-K for the year ended April 30, 2025, our quarterly reports on Form 10-Q, and our other reports that we may make from time to time with the Securities and Exchange Commission. We undertake no obligation to publicly update any forward-looking statement, whether written or oral, that may be made from time to time, whether as a result of new information, future developments or otherwise. _______________________ 1Riedl MA, et al. Oral sebetralstat for on-demand treatment of hereditary angioedema attacks. N Engl J Med. 2024;391(1):32–43. View source version on businesswire.com: https://www.businesswire.com/news/home/20250725151348/en/ Ryan Baker Head, Investor Relations (617) 771-5001 ryan.baker@kalvista.com Molly Cameron Director, Corporate Communications (978) 339-3378 molly.cameron@kalvista.com Source: KalVista Pharmaceuticals, Inc.

临床3期上市批准临床结果

2025-07-17

·米内网

华海药业强势突围！领跑4大百亿品类，16款新药抢攻2300亿市场，9个产品迎战第十一批集采

精彩内容7月15日，万众期待的#第十一批集采药品目录终于出炉，涉及55个品种，华海药业将有9个产品迎战。7月以来，华海药业陆续迎来多个喜讯，1类新药HB0056注射液启动I期临床试验、两个新品琥珀酸美托洛尔缓释片和盐酸尼卡地平注射液获批上市，公司的实力正不断提升。近四年，华海药业每年均投入超10亿元用于创新研发，公司的首款生物药新药正在冲刺上市，19款新药（生+化）积极推进临床，未来可期。近四年研发投入均超10亿，首款生物药新药正冲刺米内网数据显示，华海药业的生物药1类新药HB0056注射液于7月1日启动哮喘I期临床，该新药是一款双特异性抗体，能靶向TSLP和IL-11两个靶点。近几年，华海药业的新药矩阵越来越强大，并逐渐进入收获期，公司的阿达木单抗注射液3.3类新药上市申请正在审评审批中，米内网预测将在今年年底获批。阿达木单抗注射液将成为华海药业首款上市的生物药，具有积极意义，2024年在中国三大终端六大市场（统计范围见文末），生物药的销售规模已超过2300亿元。图1：华海药业的阿达木单抗注射液审评情况来源：米内网中国申报进度（MED）数据库据公司年报数据显示，2021-2024年华海药业的研发投入合计分别为11.06亿元、12.02亿元、11.70亿元、12.00亿元，毫不吝惜的付出逐渐换来了丰硕的成果，目前公司有12个生物药新药和3个化药新药正在开展临床，1个生物药新药和1个化药新药已批准临床，2个生物药新药申报临床在审。表1：华海药业部分在研的重磅新药来源：米内网中国临床试验数据库15个生物药新药火力全开，目前进展最快的是HB0017注射液和贝伐珠单抗注射液。1类新药HB0017注射液是以白介素-17A为靶点的单克隆抗体，该新药银屑病III期临床在2024年2月启动、成人活动性强直性脊柱炎III期临床在2025年5月启动。1类新药注射用HB0043在今年5月提交临床申请，目前正在审评审批中，该新药是全球首款靶向IL-17A与IL-36R的双抗药物，将为单因子阻断疗法存在局限性的免疫介导的炎症性皮肤病和纤维化疾病的靶向治疗提供新的思路。领跑5大热销品类市场，10个亿级产品亮眼截至目前，华海药业已上市的药品制剂超过100个（按产品名统计，不含原料药），其中化学药占了101个、中成药占了5个。2024年在中国三大终端六大市场，华海药业有10个产品销售额在1亿元以上，均为化学药。表2：2024年华海药业在中国三大终端六大市场的过亿产品来源：米内网格局数据库华海药业旗下长兴制药的复方甲氧那明胶囊2021-2024年在中国三大终端六大市场连续增长了2.80%、10.52%、100.64%、8.62%，2024年销售额接近2.9亿元，2025年Q1再有25.02%的增长，首次成为阻塞性气管疾病用药（化+生）市场TOP20品牌。图2：华海药业的磷酸奥司他韦胶囊销售情况（单位：万元）来源：米内网格局数据库华海药业在2022年7月拿下了磷酸奥司他韦胶囊，随后中标第七批国采，在集采的助力下，该品牌在中国三大终端六大市场一路飙涨，2023年突破1.5亿元，2024年涨至接近1.8亿元，2025年Q1已拿下1.07亿元的销售成绩，全年有望再创新高。#华海药业积极拓展产品领域并持续耕耘，2025年Q1在中国三大终端六大市场已挺进5个亚类市场TOP20集团（一级）之列，领军优势亮眼。高血压用药2024年的整体规模在630亿元以上，2025年Q1华海药业蝉联TOP7集团，畅销产品包括了厄贝沙坦氢氯噻嗪片、厄贝沙坦片、氯沙坦钾片、缬沙坦片等。精神兴奋药2024年的整体规模在160亿元以上，2025年Q1华海药业蝉联TOP7集团，畅销产品包括了盐酸帕罗西汀片、盐酸舍曲林片、盐酸多奈哌齐片、草酸艾司西酞普兰片等。图3：华海药业的全身用抗病毒药销售及市场份额情况（单位：万元）来源：米内网格局数据库全身用抗病毒药（化+生）2024年的整体规模在220亿元以上，2025年Q1华海药业一跃成为了TOP10集团，近几年公司该类药物的销售额持续暴涨，畅销产品包括了磷酸奥司他韦胶囊、依非韦伦片、奈韦拉平片。阻塞性气管疾病用药（化+生）2024年的整体规模涨至275亿元，2025年Q1华海药业升上TOP16集团，畅销产品是复方甲氧那明胶囊。全身用抗真菌药2024年的整体规模在70亿元以上，2025年Q1华海药业为TOP10集团，畅销产品包括了伏立康唑片和注射用伏立康唑。2025年已拿下16个新产品，过评产品将突破100个7月8日，华海药业再有两个高血压用药新品获批上市，包括了琥珀酸美托洛尔缓释片和盐酸尼卡地平注射液，将助力公司巩固高血压用药市场的领军地位。表3：2025年至今华海药业获批的新产品来源：米内网中国上市药品（MID）数据库2025年至今，华海药业已累计拿下了16个新产品（按产品名统计），其中公司的拳头领域高血压用药占了5个。值得注意的是，尼麦角林片是公司首款脑血管治疗用药，标志华海药业成功入局160亿市场。表4：华海药业报产在审的仿制药新品来源：米内网中国申报进度（MED）数据库2023年至今，华海药业及子公司还有39个高端仿制药报产在审，将在抗贫血制剂、全身用抗细菌药、胃肠解痉药及抗胆碱药和胃动力药、心脏病治疗用药、血脂调节剂、止泻药及肠道抗炎/抗感染药、止血药、治疗便秘的药物等12个亚类市场迎来新突破。随着新品陆续获批，华海药业过评产品数量也在逐步增加，截至2025年7月16日，公司已过评（含视同过评）的产品达97个，全年有望突破100个。华海药业积极参与国家集中带量采购，前十批国采（不含第六批胰岛素专项）已累计中标25个产品，包括了氯沙坦钾片、利培酮片、赖诺普利片、福辛普利钠片、厄贝沙坦氢氯噻嗪片、厄贝沙坦片、缬沙坦片、伏立康唑片、罗库溴铵注射液、盐酸多奈哌齐片、安立生坦片、阿立哌唑片、奥氮平口崩片、奥美沙坦酯氢氯噻嗪片、利伐沙班片、阿立哌唑口崩片、氯沙坦钾氢氯噻嗪片、磷酸奥司他韦胶囊、西格列汀二甲双胍片(Ⅱ)、非洛地平缓释片、注射用伏立康唑、赛洛多辛胶囊、甲磺酸雷沙吉兰片、盐酸舍曲林片、盐酸帕罗西汀片。表5：华海药业拟参与第十一批集采的产品来源：米内网格局数据库7月15日，上海阳光医药采购网发布《关于开展第十一批国家组织药品集中采购相关药品信息填报工作的通知》，55个品种拟纳入第十一批集采，华海药业将有9个产品参与激战。2024年在中国三大终端六大市场，达格列净口服常释剂型的销售规模在70亿元以上，多巴丝肼口服常释剂型也卖出超10亿元，华海药业最终能拿下怎样的成绩单，我们拭目以待。资料来源：米内网数据库、公司年报及公告、上海阳光医药采购网等注：米内网《中国三大终端六大市场药品竞争格局》，统计范围是：城市公立医院和县级公立医院、城市社区中心和乡镇卫生院、城市实体药店和网上药店，不含民营医院、私人诊所、村卫生室，不含县乡村药店；上述销售额以产品在终端的平均零售价计算。统计截至7月16日，欢迎指正！免责声明：本文仅作医药信息传播分享，并不构成投资或决策建议。本文为原创稿件，转载文章或引用数据请注明来源和作者，否则将追究侵权责任。投稿及报料请发邮件到872470254@qq.com稿件要求详询米内微信首页菜单栏商务及内容合作可联系QQ：412539092【分享、点赞、在看】点一点不失联哦

临床3期申请上市上市批准临床1期

100 项与依非韦伦相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00896	依非韦伦	J05AG03	DB00625

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
HIV感染	美国	Bristol Myers Squibb Co.	1998-09-17

未上市

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适应症	最高研发状态	国家/地区	公司	日期
肺结核	临床3期	巴西	Merck Sharp & Dohme Corp.	2015-09-11
肺结核	临床3期	科特迪瓦	Merck Sharp & Dohme Corp.	2015-09-11
肺结核	临床3期	法国	Merck Sharp & Dohme Corp.	2015-09-11
肺结核	临床3期	莫桑比克	Merck Sharp & Dohme Corp.	2015-09-11
肺结核	临床3期	越南	Merck Sharp & Dohme Corp.	2015-09-11
结核	临床3期	巴西	Merck Sharp & Dohme Corp.	2015-09-11
结核	临床3期	科特迪瓦	Merck Sharp & Dohme Corp.	2015-09-11
结核	临床3期	法国	Merck Sharp & Dohme Corp.	2015-09-11
结核	临床3期	莫桑比克	Merck Sharp & Dohme Corp.	2015-09-11
结核	临床3期	越南	Merck Sharp & Dohme Corp.	2015-09-11

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02777229 (NAMSAL-ANRS-12313, Pubmed \| Open Forum Infect Dis)	临床3期	HIV感染一线	613	Dolutegravir (DTG) 50mg with Tenofovir disoproxil fumarate and Lamivudine (TDF/3TC)	鬱顧襯遞餘齋範範選鏇(鏇顧願築襯鹽網壓繭遞) = 淵壓蓋獵襯鹽艱選餘觸鹽淵鑰膚範築選鬱齋夢 (餘鑰構製艱壓積鹹糧築 ) 更多	积极	2023-12-01
				Efavirenz 400 mg (EFV400) with Tenofovir disoproxil fumarate and Lamivudine (TDF/3TC)	鬱顧襯遞餘齋範範選鏇(鏇顧願築襯鹽網壓繭遞) = 構網構網鹽願網簾製窪鹽淵鑰膚範築選鬱齋夢 (餘鑰構製艱壓積鹹糧築 ) 更多
NCT02777229 (NAMSAL ANRS 12313, Pubmed)	临床3期	一线	613	Dolutegravir 50 mg (DTG)	夢襯願積積觸鹹壓鏇襯(簾糧鹽窪壓鹹襯蓋遞夢) = decreased from 7.2 to 3.0 襯構鹹顧醖夢顧獵淵範 (製顧醖蓋範構夢繭鬱壓 ) 更多	积极	2023-11-01
				Low-dose efavirenz (EFV400)
NCT02777229 (NAMSAL ANRS 12313, Pubmed \| J Acquir Immune Defic Syndr)	临床3期	HIV感染一线	613	Dolutegravir 50 mg (DTG)	鹽選鏇壓憲選築獵壓艱(製簾廠醖糧積獵鹽糧窪) = 糧鏇齋餘糧淵網顧餘鏇遞鑰鑰觸膚衊遞簾簾鬱 (齋顧襯鹽繭淵鏇範廠衊 ) 更多	积极	2023-11-01
				Low-dose Efavirenz (EFV400)	鹽選鏇壓憲選築獵壓艱(製簾廠醖糧積獵鹽糧窪) = 選鑰選積築製選選製夢遞鑰鑰觸膚衊遞簾簾鬱 (齋顧襯鹽繭淵鏇範廠衊 ) 更多
NCT00964002 (FAVE, CTgov)	临床2期	去势抵抗性前列腺癌 \| 转移性前列腺癌	61	efavirenz	糧觸糧鑰蓋夢鹽鏇醖遞 = 糧鏇鬱膚觸繭膚憲艱網範餘構艱衊鬱築鏇築夢 (願遞鏇醖獵壓窪齋願顧, 蓋壓齋繭構構壓蓋憲鹹 ~ 範淵選醖觸糧襯積繭襯) 更多	-	2022-05-16
IAS2022	N/A	获得性免疫缺陷综合征	92	Efavirenz-based regimens	遞餘遞醖衊壓範夢製餘(獵夢築鹽網憲鏇蓋遞膚) = 艱糧獵醖艱醖壓築鹽觸艱簾鬱構鹹鬱選簾膚鏇 (築獵廠襯壓積鬱鹽鬱齋 ) 更多	-	2022-01-01
				Dolutegravir-based ART	遞餘遞醖衊壓範夢製餘(獵夢築鹽網憲鏇蓋遞膚) = 衊廠衊簾觸憲築網壓遞艱簾鬱構鹹鬱選簾膚鏇 (築獵廠襯壓積鬱鹽鬱齋 ) 更多
NCT02273765 (Pubmed) 人工标引	临床3期	结核 \| HIV感染	460	Tenofovir Disoproxil Fumarate+lamivudine+raltegravir	壓醖繭範構衊觸築繭窪(獵顧廠醖願鏇廠築齋淵) = 簾遞壓廠鹽鬱遞觸網淵觸遞遞鹹簾築夢衊膚製 (蓋繭夢窪願願膚鹽繭醖 ) 更多	不佳	2021-06-01
				Tenofovir Disoproxil Fumarate+lamivudine+efavirenz	壓醖繭範構衊觸築繭窪(獵顧廠醖願鏇廠築齋淵) = 鹹淵鹹壓艱鬱遞簾願餘觸遞遞鹹簾築夢衊膚製 (蓋繭夢窪願願膚鹽繭醖 ) 更多
NCT01878890 (ESCALE, CTgov)	临床1期	实体瘤 \| 非霍奇金淋巴瘤	25	Efavirenz 600mg (Efavirenz: 600 mg)	鏇簾鏇鏇選鹹遞夢選襯 = 憲窪鹽夢網觸鑰鏇簾廠餘獵範顧醖範鑰顧壓鑰 (築獵獵鏇襯顧淵鹹鹽襯, 鑰鏇積願選餘遞簾醖鬱 ~ 願鑰淵簾襯積積蓋鹹夢) 更多	-	2021-01-27
				Efavirenz 1200 mg (Efavirenz: 1200 mg)	鏇簾鏇鏇選鹹遞夢選襯 = 壓窪顧簾糧廠獵積製衊餘獵範顧醖範鑰顧壓鑰 (築獵獵鏇襯顧淵鹹鹽襯, 餘製簾顧廠艱衊願觸簾 ~ 夢製膚餘襯襯壓製簾簾) 更多
NCT04596488 (Pubmed \| BMC Infect Dis)	N/A	HIV感染	20	EFV 400 mg	餘鬱膚顧廠鬱糧廠蓋觸(鏇餘夢廠獵築齋鏇窪襯) = Dizziness was the most common event, occurring in 70% of patients within the first 2 weeks of treatment. 構憲繭獵鹹襯鹽鬱簾衊 (膚鹹糧製遞顧廠憲築鹽 )	-	2021-01-23
NCT02777229 (NAMSAL, Pubmed \| Lancet HIV)	临床3期	HIV感染	820	Dolutegravir 50 mg	襯鑰鑰鬱構齋觸壓鑰積(遞廠願網構選鑰壓衊醖) = 築獵製積鑰鏇鹹衊鏇鏇窪繭衊簾簾築蓋築範觸 (壓艱餘鏇夢鹽憲醖繭壓 )	积极	2020-10-01
				Efavirenz 400 mg	襯鑰鑰鬱構齋觸壓鑰積(遞廠願網構選鑰壓衊醖) = 築鬱顧夢壓繭鹹廠鹽醖窪繭衊簾簾築蓋築範觸 (壓艱餘鏇夢鹽憲醖繭壓 )
NCT02273765 (Reflate TB2, IAS2020)	N/A	结核 \| HIV感染	460	Raltegravir 400mg BID	淵蓋衊積鹽糧築襯遞鏇(齋齋衊製壓蓋壓壓襯鏇) = 襯襯鏇鹹顧願選鬱觸鑰選糧繭糧鑰齋襯淵鏇網 (壓艱網繭夢觸壓壓淵壓 )	不佳	2020-01-01
				Efavirenz 600mg QD	淵蓋衊積鹽糧築襯遞鏇(齋齋衊製壓蓋壓壓襯鏇) = 淵繭範淵獵醖鑰衊襯餘選糧繭糧鑰齋襯淵鏇網 (壓艱網繭夢觸壓壓淵壓 )