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更新于：2026-08-04
Bepirovirsen
贝普若韦生
更新于：2026-08-04
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21
项与 贝普若韦生 相关的临床试验NCT07696520
Bepirovirsen Liver Biopsy Study
NCT07168356
A Phase 1, Open-Label, Single-Dose, Parallel Group, 2-Part Study to Evaluate the Pharmacokinetics of Bepirovirsen in Adult Participants With Severe or Moderate Renal Impairment Compared to Matched Healthy Control Participants
NCT06537414
A Phase 2b, Multi-centre, Randomized, Partially Placebo-controlled, Double-blind Study to Investigate the Safety and Efficacy of Sequential Therapy With Daplusiran/Tomligisiran Followed by Bepirovirsen in Participants With Chronic Hepatitis B Virus on Background Nucleos(t)Ide Analogue Therapy (B-United)
100 项与 贝普若韦生 相关的临床结果
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100 项与 贝普若韦生 相关的转化医学
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100 项与 贝普若韦生 相关的专利（医药）
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28
项与 贝普若韦生 相关的文献（医药）2026-06-25NEW ENGLAND JOURNAL OF MEDICINE
Phase 3 Results of Bepirovirsen Treatment for Chronic Hepatitis B Virus Infection
Article
作者: Heo, Jeong ; Liang, Xieer ; Franca, Alex ; Peng, Cheng-Yuan ; Asselah, Tarik ; Chen, Chien-Hung ; Idriz, Nevin ; Sevastianos, Vasileios ; Mehta, Rajiv ; Lin, Jianmei ; Lukić, Tamara ; Holmes, Jacinta ; Yim, Hyung Joon ; Hlebowicz, Maria ; Cernat, Roxana ; Xie, Qing ; Jeng, Wen-Juei ; Chuang, Wan-Long ; Yuen, Man-Fung ; Hou, Jinlin ; Qiu, Yunqing ; Cremer, Jennifer ; Quinn, Geoff ; Stocker, Hartmut ; Lim, Seng-Gee ; Ratziu, Vlad ; Terrault, Norah ; Agarwal, Kosh ; Tanaka, Yasuhito ; Lim, Tien Huey ; Riachi, Ghassan ; Nguyen, Huy ; Leerapun, Apinya ; Fujiyama, Shigetoshi ; Gomes da Silva, Monica M. ; Buti, Maria ; Xie, Yao ; Elston, Robert ; Gane, Edward ; Tao, Yu ; Lampertico, Pietro ; Suzuki, Yuichiro ; Plein, Helene ; Theodore, Dickens ; Gadano, Adrian ; Paff, Melanie ; Coffin, Carla S. ; Andreone, Pietro
BACKGROUND:
Treatment with bepirovirsen, an antisense oligonucleotide targeting hepatitis B virus (HBV) transcripts, has the potential to result in a functional cure, defined by at least 24 weeks of a sustained HBV DNA level below the lower limit of quantification (LLOQ) and hepatitis B surface antigen (HBsAg) loss after fixed-duration therapy.
METHODS:
In two replicate, double-blind trials (B-Well 1 and B-Well 2), we randomly assigned adults with noncirrhotic chronic HBV infection in a 2:1 ratio to receive subcutaneous bepirovirsen (at a weekly dose of 300 mg) or placebo for 24 weeks. All the patients were receiving stable nucleoside or nucleotide analogue (NA) therapy and had an HBsAg level of more than 100 to 3000 IU per milliliter. Eligible patients discontinued NA therapy at 48 weeks. The primary outcome was a functional cure at week 72.
RESULTS:
The percentage of patients with a functional cure at week 72 was significantly higher with bepirovirsen than with placebo both in the B-Well 1 trial (in 127 of 650 patients [20%] vs. none of 328 patients) and in the B-Well 2 trial (in 106 of 570 patients [19%] vs. none of 286 patients). In a pooled analysis at 72 weeks, adverse events were reported in 91% of the patients in the bepirovirsen groups and in 73% of those in the placebo groups; serious adverse events were reported in 7% and 4% of the patients, respectively. During the treatment period, adverse events of grade 3 or higher were reported in 16% of the patients who received bepirovirsen and in 3% of those who received placebo; increases in the alanine aminotransferase level were the most common grade 3 adverse events with bepirovirsen (in 6% of the patients).
CONCLUSIONS:
In two phase 3 trials involving patients with chronic HBV infection, a functional cure after the discontinuation of NA therapy was reported in significantly more patients treated with bepirovirsen than in those who received placebo. (Funded by GSK; ClinicalTrials.gov numbers, NCT05630807 and NCT05630820.).
2026-06-01JHEP Reports
Bepirovirsen induces innate immune activation in the liver potentially through TLR8 signaling
Article
作者: DeHart, Anne ; Tarrant, Jimmy ; Hoang, Bao ; Terry, Rebecca L ; Austin, Daren ; Das, Amitabh ; Galwey, Nicholas ; Jordan, William ; Jones, Kristen ; Ray, Avijit ; Ermler, Megan E ; Delahaye, Jared L ; Theodore, Dickens ; Singh, Jennifer M ; Sherina, Valeriia ; Paff, Melanie ; You, Shihyun ; Nivarthi, Usha
BACKGROUND & AIMS:
Bepirovirsen is an unconjugated antisense oligonucleotide in Phase 3 trials for chronic hepatitis B virus (HBV) infection. Post hoc analyses from a Phase 2a study (chronic HBV participants) indicated immediate cytokine production upon dosing of bepirovirsen, leading to the hypothesis that bepirovirsen may have innate immune stimulatory activity via pattern recognition receptors (PRRs) in hepatic non-parenchymal cells, alongside its known direct antiviral mechanism in hepatocytes.
METHODS:
Cytokine production was evaluated in Phase 2a serum and plasma samples using Myriad RBM, Olink, or MSD panels. Preclinical studies used PBMCs from healthy donors (MSD, flow cytometry) and PRR-overexpressing HEK or THP-1 cells to assess innate immune activation by bepirovirsen. Cytokine protein levels were measured with Luminex or MSD in wild-type (WT) and hTLR8 transgenic mice, while gene expression (RT-qPCR, RNAscope) was analyzed in vivo exclusively in hTLR8 transgenic mice from Shanghai Model Organisms Center (SMOC).
RESULTS:
Many pro-inflammatory cytokines for immune cell recruitment and activation were upregulated in bepirovirsen-treated participants. Similar findings were seen preclinically in PBMCs from healthy donors following bepirovirsen treatment in vitro. Analysis of innate immune activation in PRR-overexpressing cells revealed weak, yet positive (p = 0.00085), induction only when human Toll-like receptor 8 (TLR8) was present. In hTLR8 transgenic mice, but not wild-type mice, bepirovirsen treatment induced pro-inflammatory cytokines, similar to the TLR8 agonist selgantolimod. Kupffer cells and macrophages were identified as the primary responders to bepirovirsen in hTLR8 mouse livers.
CONCLUSIONS:
Clinical and preclinical data show that bepirovirsen elicits an innate immune response, evidenced by induction of inflammatory cytokines. This effect is mediated at least in part by TLR8 agonism, complementing its established antiviral mechanism.
IMPACT AND IMPLICATIONS:
The aim of this study was to characterize additional mechanisms of action for bepirovirsen, including immune activation through PRRs, based on the hypothesis that bepirovirsen may elicit an innate immune response in addition to its antiviral mechanism. Using Phase 2a study samples we show that bepirovirsen induces IFN-γ, TNF, and other cytokines, while in vitro we demonstrate that that bepirovirsen harbors innate immune stimulatory activity, potentially through human TLR8. Furthermore, we show that the innate immune activation induced by bepirovirsen is distinct from that of other ASOs. This study demonstrates that bepirovirsen can induce an innate immune response, likely through TLR8 agonism, in addition to its known antiviral mechanism; however, the clinical impact of this immunomodulatory effect remains unclear and requires further investigation.
2026-05-01JOURNAL OF HEPATOLOGY
Single nucleotide polymorphisms in the bepirovirsen binding site have limited impact on treatment response in chronic hepatitis B
Article
作者: Angelini, Elise ; You, Shihyun ; Yates, Phillip ; Galwey, Nicholas ; Maynard, Lauren ; Walker, Jill ; Lau, Chi ; Savarese, Michael ; Theodore, Dickens ; Elston, Rob ; Cremer, Jennifer ; Koenig, Alexander ; Speer, Scott D ; Paff, Melanie ; Livingston, Christine M ; Bouquet, Jerome
BACKGROUND & AIMS:
Single nucleotide polymorphisms (SNPs) in the HBV genome may impact the efficacy of novel drugs for chronic HBV infection. This analysis of the B-Clear study (NCT04449029) evaluated the frequency of baseline and treatment-emergent SNPs in the bepirovirsen binding site and their association with virological response.
METHODS:
HBV sequencing was attempted for all baseline samples collected from B-Clear participants and for selected post-baseline samples from participants meeting predefined resistance-monitoring criteria. Participants were categorized according to nucleos(t)ide analogue (NA) treatment status and hepatitis B surface antigen (HBsAg) response. SNPs were identified using next-generation sequencing and reported if the allelic frequency was ≥5%. The effects of binding site SNPs on viral fitness and susceptibility to bepirovirsen were assessed in vitro.
RESULTS:
Baseline sequences were obtained for 40% (90/226) and 96% (219/229) of On-NA and Not-on-NA participants, respectively. Baseline SNPs were identified in 7% (22/309) of participants. These participants showed numerically smaller HBsAg reductions than those without SNPs, but 18% (4/22) achieved transient HBsAg loss. Post-baseline sequences were obtained for 22% (49/226) and 62% (143/229) of On-NA and Not-on-NA participants, respectively. Of 16 post-baseline SNPs, eight were treatment-emergent. SNPs were detected at 12 of the 20 binding site positions; however, only two SNPs had an allelic frequency >50% (C1589A [max 99%] and C1600T [max 99%]). Six SNPs showed sufficient viral fitness to be evaluated for susceptibility to bepirovirsen in vitro. C1589A demonstrated the largest reduction in susceptibility (4.1-fold) to bepirovirsen.
CONCLUSIONS:
Most participants achieved >1 log reductions in HBsAg, including transient HBsAg loss in some. Although participants with baseline SNPs showed numerically smaller HBsAg reductions, further investigation is required to better understand potential mechanisms of resistance to bepirovirsen.
IMPACT AND IMPLICATIONS:
HBV sequence polymorphisms can contribute to antiviral resistance in the treatment of chronic HBV infection. Therefore, it is important for healthcare professionals to understand the prevalence and emergence of single nucleotide polymorphisms (SNPs) within the bepirovirsen binding site and their potential impact on virological response. Findings from this phase IIb clinical study demonstrate that the vast majority (92%) of non-responders, partial responders, or relapsers did not harbor bepirovirsen binding site SNPs. Moreover, participants with binding site SNPs (7% of participants) still achieved reductions in hepatitis B surface antigen. These results suggest that routine testing for specific HBV variants prior to bepirovirsen administration is not currently warranted, and that resistance due to altered sequence complementarity is likely minimal and multifactorial. Ongoing phase III studies of bepirovirsen will provide additional context to further evaluate the need for variant testing and to better elucidate potential resistance mechanisms.
100 项与 贝普若韦生 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 病毒感染 | 申请上市 | 加拿大 | 2026-05-01 | |
| 慢性乙型肝炎 | 申请上市 | 日本 | 2026-02-26 |
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临床结果
临床结果
适应症
分期
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临床1期 | 46 | (Bepirovirsen: Four-Dose SC Injection) | 繭窪餘壓艱鑰憲醖憲鑰(鹹廠繭繭餘鹽鑰餘鹹鏇) = 膚網鹽觸艱淵壓齋膚鏇 鑰壓觸積襯醖醖觸構鑰 (觸糧襯顧範鏇範艱蓋製, 範願鏇膚網醖淵選鏇襯 ~ 鬱齋糧顧構醖鹽選鏇獵) 更多 | - | 2026-07-10 | ||
(Bepirovirsen: Three-Dose SC Injection) | 繭窪餘壓艱鑰憲醖憲鑰(鹹廠繭繭餘鹽鑰餘鹹鏇) = 衊積衊夢鑰觸窪壓簾襯 鑰壓觸積襯醖醖觸構鑰 (觸糧襯顧範鏇範艱蓋製, 蓋艱願壓繭齋範顧網夢 ~ 艱鑰壓艱鏇觸窪衊顧糧) 更多 | ||||||
临床3期 | 1,254 | 壓糧醖醖膚壓衊窪膚鑰(鏇願構製蓋遞夢網襯製) = 醖築鹽壓獵鏇獵憲餘鹽 膚齋淵鬱壓鹽衊網網鏇 (簾繭壓夢糧築糧廠艱壓 ) 更多 | 积极 | 2026-06-25 | |||
Placebo | 壓願淵廠憲構壓壓衊願(糧衊窪觸壓築獵觸築獵) = 願遞鬱憲餘願獵構選壓 製衊醖襯繭夢廠蓋淵齋 (夢憲積顧築醖範鬱齋鬱 ) 更多 | ||||||
临床3期 | 1,800 | 襯網壓廠糧鹽觸餘糧獵(憲廠築顧廠壓夢蓋襯構) = Bepirovirsen demonstrated a statistically significant and clinically meaningful functional cure rate 範範鬱淵餘鏇壓襯簾願 (壓鑰選鏇蓋範構遞糧醖 ) 达到 | 积极 | 2026-01-07 | |||
Placebo | |||||||
临床1期 | 160 | (Bepirovirsen 300 mg Vial by HCP) | 範顧鹽鏇憲築鑰鏇餘鏇(蓋構簾鹽鹹鹹製鬱膚襯) = 構鹹顧醖醖淵膚簾艱齋 鑰鏇鹽選遞鏇選艱遞鹽 (顧壓繭鹹遞積獵範鹽蓋, 0.049) 更多 | - | 2025-07-18 | ||
(Bepirovirsen 300 mg PFS SSD by HCP) | 範顧鹽鏇憲築鑰鏇餘鏇(蓋構簾鹽鹹鹹製鬱膚襯) = 觸廠憲衊製顧醖鑰夢壓 鑰鏇鹽選遞鏇選艱遞鹽 (顧壓繭鹹遞積獵範鹽蓋, 0.048) 更多 | ||||||
临床2期 | 慢性乙型肝炎 HBsAg | HBV DNA | 108 | 窪餘襯鹹鑰窪醖觸餘鏇(觸醖鹽積獵顧窪網膚艱) = The proportions of participants with adverse events and treatment-related adverse events in both treatment windows were similar between treatment arms 選觸遞繭製壓選網憲築 (齋膚糧製築艱網醖廠壓 ) | 积极 | 2025-02-01 | ||
临床2期 | 12 | Nucleos(t)ide therapy+GSK3228836 | 齋膚夢膚淵鹽壓積餘窪 = 鹹膚艱積築顧艱鹹網鬱 齋築構蓋簾積製膚鹹蓋 (築壓範觸鏇窪製構蓋襯, 遞簾憲淵淵艱蓋糧壓襯 ~ 觸鹽遞鑰築淵憲憲範積) 更多 | - | 2024-12-19 | ||
临床1期 | 24 | (hepatic impairment participants) | 願選窪顧顧淵淵壓襯鹹(醖糧襯鹽鏇鹹蓋簾壓艱): Geometric Mean Ratio = 0.69 更多 | 积极 | 2024-09-13 | ||
(healthy participants) | |||||||
临床2期 | 108 | PegIFN+GSK3228836 (GSK3228836 300 mg (24 Weeks) + PegIFN 180 mcg (24 Weeks)) | 鬱築鏇襯構艱蓋獵遞襯 = 憲艱繭鬱獵範鏇壓築淵 築範淵範觸膚憲鏇憲壓 (糧襯憲醖壓夢憲鹽鏇壓, 鹽範艱廠窪餘遞膚積願 ~ 製鏇夢鬱構鬱膚鹹襯廠) 更多 | - | 2024-05-02 | ||
PegIFN+GSK3228836 (GSK3228836 300 mg (12 Weeks) + PegIFN 180 mcg (24 Weeks)) | 醖繭衊醖繭積壓廠襯觸 = 選淵範願醖鬱齋襯憲壓 觸獵選糧淵糧艱願齋繭 (醖窪獵鏇鹽膚獵選襯襯, 襯鹹構壓選窪衊壓簾觸 ~ 鹽繭遞構鏇艱願顧築鑰) 更多 | ||||||
临床2期 | 慢性乙型肝炎 HBsAg | HBV DNA | ALT | 108 | Arm 1 (BPV 300 mg for 24 weeks + PegIFN 180 mcg QW for 24 weeks) | 鏇觸鬱蓋衊鬱選醖膚簾(齋艱餘築膚鹽窪鬱鬱蓋) = 糧觸簾願積積鬱築鹽鹹 網遞遞顧餘網觸膚積鏇 (蓋壓遞鬱顧觸遞鏇選衊 ) | - | 2023-11-10 | |
临床2期 | - | Arm 1 (BPV 24 wk) | 獵獵鬱醖築獵淵鹽襯觸(構製廠獵艱餘簾淵糧範) = 窪繭遞製鏇壓醖憲鑰鬱 膚觸繭鬱顧遞鏇顧膚艱 (願夢觸齋糧範齋壓積艱 ) | - | 2023-11-10 | ||
Arm 2 (BPV 12 wk) | 獵獵鬱醖築獵淵鹽襯觸(構製廠獵艱餘簾淵糧範) = 憲蓋齋鏇糧遞觸淵願簾 膚觸繭鬱顧遞鏇顧膚艱 (願夢觸齋糧範齋壓積艱 ) |
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