预约演示
更新于：2026-09-19
Selgantolimod
更新于：2026-09-19
概要
基本信息
在研机构- |
权益机构- |
最高研发阶段无进展临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C14H20FN5O |
InChIKeyHTCJUBZBSJQWBW-CQSZACIVSA-N |
CAS号2004677-13-6 |
关联
9
项与 Selgantolimod 相关的临床试验NCT05551273
Safety, Tolerability, and Impact of Oral TLR8 Agonist Selgantolimod on HBsAg in Participants With Both Chronic Hepatitis B and HIV
NCT05045261
ANRS HB07 IP-Cure-B Proof of Concept (PoC) Clinical Trial. Educating the Liver Immune Environment Through TLR8 Stimulation Followed by NUC Discontinuation
NCT04891770
A Phase 2a, Open-Label Study to Evaluate the Safety and Efficacy of Selgantolimod (SLGN)-Containing Combination Therapies for the Treatment of Chronic Hepatitis B (CHB)
100 项与 Selgantolimod 相关的临床结果
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100 项与 Selgantolimod 相关的转化医学
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100 项与 Selgantolimod 相关的专利（医药）
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8
项与 Selgantolimod 相关的文献（医药）2024-12-01GUT
Immunomodulation and entry inhibition: selgantolimod’s double punch against hepatitis B virus
Article
作者: Cornberg, Markus ; Urbanek-Quaing, Melanie ; Baumert, Thomas
2024-12-01GUT
TLR8 agonist selgantolimod regulates Kupffer cell differentiation status and impairs HBV entry into hepatocytes via an IL-6-dependent mechanism
Article
作者: Dubois, Anaëlle ; Michelet, Maud ; Fletcher, Simon P ; Saez-Palma, Maria ; Diederichs, Audrey ; Daffis, Stephane ; Wallin, Jeffrey J ; Heintz, Sarah ; Hsu, Yao-Chun ; Grand, Xavier ; Vanwolleghem, Thomas ; Lau, Audrey H ; Plissonnier, Marie-Laure ; Li, Li ; Zoulim, Fabien ; Kolhatkar, Nikita ; Levrero, Massimo ; Giraud, Guillaume ; Van Renne, Nicolaas ; Rivoire, Michel ; Roca Suarez, Armando Andres ; Testoni, Barbara
Objective:
Achieving HBV cure will require novel combination therapies of direct-acting antivirals and immunomodulatory agents. In this context, the toll-like receptor 8 (TLR8) agonist selgantolimod (SLGN) has been investigated in preclinical models and clinical trials for chronic hepatitis B (CHB). However, little is known regarding its action on immune effectors within the liver. Our aim was to characterise the transcriptomic changes and intercellular communication events induced by SLGN in the hepatic microenvironment.
Design:
We identified
TLR8
-expressing cell types in the human liver using publicly available single-cell RNA-seq data and established a method to isolate Kupffer cells (KCs). We characterised transcriptomic and cytokine KC profiles in response to SLGN. SLGN’s indirect effect was evaluated by RNA-seq in hepatocytes treated with SLGN-conditioned media (CM) and quantification of HBV parameters following infection. Pathways mediating SLGN’s effect were validated using transcriptomic data from HBV-infected patients.
Results:
Hepatic
TLR8
expression takes place in the myeloid compartment. SLGN treatment of KCs upregulated monocyte markers (eg,
S100A12
) and downregulated genes associated with the KC identity (eg,
SPIC
). Treatment of hepatocytes with SLGN-CM downregulated
NTCP
and impaired HBV entry. Cotreatment with an interleukin 6-neutralising antibody reverted the HBV entry inhibition.
Conclusion:
Our transcriptomic characterisation of SLGN sheds light into the programmes regulating KC activation. Furthermore, in addition to its previously described effect on established HBV infection and adaptive immunity, we show that SLGN impairs HBV entry. Altogether, SLGN may contribute through KCs to remodelling the intrahepatic immune microenvironment and may thus represent an important component of future combinations to cure HBV infection.
2023-03-01Journal of hepatology
Safety and efficacy of the oral TLR8 agonist selgantolimod in individuals with chronic hepatitis B under viral suppression
Article
作者: Anna E. Brooks ; Susanna K. Tan ; Lydia Tang ; Anuj Gaggar ; Nicholas van Buuren ; Priyanka Arora ; Diana Chen ; P. Rod Dunbar ; Jenny C. Yang ; Jeffrey J. Wallin ; Edward J. Gane ; Fangqiu Zhang ; Simon P. Fletcher ; Shyamasundaran Kottilil
BACKGROUND & AIMS:
Selgantolimod (GS-9688) is a Toll-like receptor 8 (TLR8) agonist that suppresses HBV in vitro. In a phase II study, we evaluated the safety and efficacy of weekly selgantolimod treatment in virally suppressed individuals with chronic HBV taking oral antiviral treatment.
METHODS:
Forty-eight patients were randomized into two cohorts (hepatitis B e antigen [HBeAg]-positive and -negative [n = 24 each]) to receive oral selgantolimod 3 mg, 1.5 mg, or placebo (2:2:1) once weekly for 24 weeks while maintaining oral antivirals. The primary efficacy endpoint was the percentage of patients with a ≥1 log10 IU/ml decline in hepatitis B surface antigen (HBsAg) from baseline to week 24. Post-treatment, patients continued on oral antivirals for 24 weeks.
RESULTS:
The primary endpoint was reached by one participant, who was HBeAg-negative and received selgantolimod 1.5 mg. In contrast with placebo-treated patients (n = 9), only selgantolimod-treated patients (n = 39 total) had HBsAg declines greater than 0.1 log10 IU/ml at weeks 24 (18%, 7/39) and 48 (26%, 10/39), HBsAg loss (5%, 2/39 through 48 weeks), or HBeAg loss (16%, 3/19 through 48 weeks). The most common adverse events in selgantolimod-treated groups were nausea (46%), upper respiratory tract infection (23%), and vomiting (23%). Gastrointestinal disorders were mostly mild and transient. Selgantolimod induced transient dose-dependent increases in serum cytokines, including IL-12p40, IFN-γ, and IL-1RA, as well as rapid redistribution of some circulating immune cell subsets.
CONCLUSION:
Oral selgantolimod up to 3 mg once weekly for 24 weeks was generally safe and well tolerated and led to serologic changes associated with progression to durable cure in two individuals by week 48.
CLINICALTRIALS:
GOV IDENTIFIER:
NCT03491553.
IMPACT AND IMPLICATIONS:
The only robust criterion for stopping treatment in chronic hepatitis B is loss of hepatitis B surface antigen (known as functional cure), which is rare during nucleos(t)ide analogue therapy. It is likely that novel antiviral and immunomodulatory therapies will be needed to achieve finite functional cure. Selgantolimod is an oral Toll-like receptor 8 agonist that has shown antiviral activity in vitro as well as safety in a phase I clinical trial with weekly dosing. In this phase II study, selgantolimod therapy was associated with transient increases in serum cytokines, rapid redistribution of circulating immune cell subsets, modest reductions in HBsAg and HBeAg levels, and occasional loss of HBsAg (5%) and HBeAg (16%) among participants with chronic hepatitis B on nucleos(t)ide analogue therapy with viral suppression. Our results support continued development of selgantolimod as a component of a future hepatitis B cure regimen.
33
项与 Selgantolimod 相关的新闻（医药）2026-08-26
2026-08-25
2026-07-28
100 项与 Selgantolimod 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 |
|---|---|---|---|---|
| 慢性乙型肝炎 | 临床2期 | 美国 | 2018-04-06 | |
| 慢性乙型肝炎 | 临床2期 | 新西兰 | 2018-04-06 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 103 | (Cohort 1: TAF + VIR-2218 + SLGN + Nivolumab) | 鹹願鑰製獵淵鬱網憲網 = 構觸範淵窪襯淵糧鹹膚 鹽窪鏇衊鏇蓋顧鹽鬱積 (獵製淵蓋遞簾簾積範選, 鬱蓋餘淵憲壓積夢憲艱 ~ 選獵艱鏇觸壓鑰糧壓構) 更多 | - | 2025-07-24 | ||
(Cohort 2 Group A: VIR-2218 + SLGN + Nivolumab) | 鹹願鑰製獵淵鬱網憲網 = 積蓋構願顧膚簾糧鹹廠 鹽窪鏇衊鏇蓋顧鹽鬱積 (獵製淵蓋遞簾簾積範選, 獵糧網鑰選鹹願願遞構 ~ 壓衊鹽糧觸製艱製蓋襯) 更多 | ||||||
临床2期 | 48 | 鏇鑰鹹襯鹹鏇製蓋壓構(築顧鏇繭襯鹹齋壓積廠) = 46% 選齋艱願憲艱襯艱製衊 (願繭衊憲築衊製獵鑰範 ) 更多 | 积极 | 2023-03-01 | |||
临床2期 | 67 | 選襯襯積繭壓衊願願構(網餘淵艱夢夢網蓋構鏇) = 11% v 0 顧鹹製簾鹽遞製獵觸範 (淵襯餘鑰獵衊醖膚鏇構 ) 更多 | 积极 | 2021-06-23 | |||
临床2期 | 67 | (Selgantolimod 3 mg + TAF) | 衊窪選醖鏇鬱簾廠觸鹹 = 鹹遞願窪選蓋願膚餘廠 衊築膚艱鹹網艱艱築遞 (繭築醖壓願顧鏇壓齋鬱, 廠簾範醖鑰獵膚鏇願簾 ~ 遞願鬱獵夢鏇淵齋鹽醖) 更多 | - | 2021-01-06 | ||
(Selgantolimod 1.5 mg + TAF) | 衊窪選醖鏇鬱簾廠觸鹹 = 艱夢鹽淵艱醖願遞鑰夢 衊築膚艱鹹網艱艱築遞 (繭築醖壓願顧鏇壓齋鬱, 夢鹽壓鹹壓顧壓鬱襯膚 ~ 鬱構餘願餘鬱鹽襯製齋) 更多 | ||||||
临床2期 | 48 | Hepatitis B virus (HBV) OAV Therapy+Selgantolimod (Selgantolimod 3 mg: HBeAg-positive CHB Participants) | 襯糧顧淵醖艱繭遞艱積 = 艱顧憲餘廠夢膚選齋遞 壓積餘襯窪鬱構餘襯願 (願積淵鏇簾蓋繭餘獵窪, 鏇艱遞齋餘鹽淵築襯衊 ~ 淵夢憲憲遞膚壓糧網蓋) 更多 | - | 2020-04-01 | ||
Hepatitis B virus (HBV) OAV Therapy+Selgantolimod (Selgantolimod 3 mg: HBeAg-negative CHB Participants) | 襯糧顧淵醖艱繭遞艱積 = 醖獵遞壓膚構襯憲齋壓 壓積餘襯窪鬱構餘襯願 (願積淵鏇簾蓋繭餘獵窪, 壓鏇齋窪願顧窪鏇糧鏇 ~ 鹹積遞淵窪鹽憲鏇鏇夢) 更多 | ||||||
临床2期 | - | 窪餘製鹽鹽觸壓廠壓網(製淵蓋艱蓋廠鹹夢鑰鹽) = 窪顧鬱夢餘壓齋淵網簾 製襯築繭齋艱壓鹹醖觸 (膚窪構壓鏇餘範積遞廠 ) | 积极 | 2019-04-12 |
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