预约演示
更新于：2026-09-21
Sorfequiline
更新于：2026-09-21
概要
基本信息
非在研机构- |
权益机构- |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)临床1期 |
特殊审评- |
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结构/序列
分子式C31H37BrN4O7 |
InChIKeyHHDDKDPLFXIPBX-DLFZDVPBSA-N |
CAS号2332841-25-3 |
关联
5
项与 Sorfequiline 相关的临床试验NCT07672405
A Phase 2b, Randomised, Multi-center, Partially Blinded Trial Assessing the Safety and Efficacy of Regimens Containing Sorfequiline, Pretomanid and Linezolid in Adults With Newly Diagnosed, Drug-sensitive, Smear Positive Pulmonary Tuberculosis
NCT06058299
A Phase 2, Partially-blinded, Randomised Trial Assessing the Safety and Efficacy of TBAJ-876 or Bedaquiline, in Combination With Pretomanid and Linezolid in Adult Participants With Newly Diagnosed, Drug-sensitive, Smear-positive Pulmonary Tuberculosis
NCT05526911
A Phase 1, Drug-Drug Interaction Study to Evaluate the Safety, Tolerability, and the Induction Potential of TBAJ-876 on CYP3A4 and P-glycoprotein and the Inhibition Potential of TBAJ-876 on P-glycoprotein in Healthy Adult Subjects
100 项与 Sorfequiline 相关的临床结果
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100 项与 Sorfequiline 相关的转化医学
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100 项与 Sorfequiline 相关的专利（医药）
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27
项与 Sorfequiline 相关的文献（医药）2026-05-01JOURNAL OF CONTROLLED RELEASE
Development of high-concentration long-acting injectable formulations of TBAJ-587 and TBAJ-876 as an extended treatment strategy against tuberculosis
Article
作者: Holm, René ; Hansen, Mads Fahnøe ; Zulbeari, Nadina ; Hopper, Chloe ; Morgen, Per
This study investigated the potential of developing long-acting injectable (LAI) formulations of the next-generation diarylquinoline antibacterial compounds TBAJ-587 and TBAJ-876, which have the potential to impact the tuberculosis (TB) treatment by providing an extended treatment option. The performance of these compounds, formulated as LAIs, were evaluated based on particle size stability, drug loading capacity, and in vivo pharmacokinetics in rats. The data showed that particularly high drug loadings could be obtained in aqueous suspensions using the salt forms of TBAJ-587 and TBAJ-876, with concentrations up to 750 mg/mL TBAJ-587 fumarate and 650 mg/mL TBAJ-876 tartrate, expressed as the equivalent concentration of free base. A long-term stability study of the TBAJ-876 tartrate formulation suggested that a relatively stable suspension was defined when stored at both ambient temperature and at 40 °C. In contrast, the TBAJ-587 fumarate suspension formulation showed significant particle size growth as a function of time, indicating physical instability in the colloidal system. Analysis of both compounds by X-ray powder diffraction (XRPD) revealed no major changes in the crystal structure following milling or after 24 weeks of storage at 40 °C. The in vivo pharmacokinetic study in rats showed that the suspensions containing either TBAJ-587 fumarate or TBAJ-876 tartrate offered a promising LAI option for the prolonged treatment of TB, as all formulations achieved prolonged drug plasma exposure for at least three months following administration.
2026-03-04ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Cardiodynamic evaluation of sorfequiline (TBAJ-876): results from a first-in-human study
Article
作者: Xue, Hongqi ; Kleiman, Robert ; Lombardi, Antonio ; Nedelman, Jerry ; Darpo, Borje ; Hickman, Dean ; Bruning-Barry, Rebecca
ABSTRACT:
Sorfequiline (TBAJ-876) is a novel diarylquinoline under development for tuberculosis. In a first-in-human, multiple-ascending-dose study, electrocardiogram and pharmacokinetic data were analyzed to assess cardiac repolarization. Placebo-corrected change-from-baseline in QTcF (ΔΔQTcF) ranged from −11.4 to +2.4 ms without dose dependency. Concentration–QTc modeling showed a shallow, non-significant slope. The predicted mean effect on ΔΔQTcF at the maximum geometric mean C
max
of sorfequiline’s M3 metabolite was −1.1 ms (90% CI −9.5 to 7.4).
CLINICAL TRIALS:
This study is registered with ClinicalTrials.gov as
NCT06058299.
2026-02-01INTERNATIONAL JOURNAL OF PHARMACEUTICS
Potential correlations between the energies at the solid/liquid interfaces and the physical stability of pharmaceutical suspensions
Article
作者: Simonsen, Adam Cohen ; Dixen, Magnus Jæger ; Zulbeari, Nadina ; Holm, René ; Stolborg, Lau Marold ; Black, Sebastian ; Hansen, Mads Fahnøe ; Lund, Frederik Wendelboe
This study investigated the interfacial behaviors of non-ionic surfactants at the air-liquid and solid-liquid interfaces including the work of adhesion derived from surface tension and contact angle measurements and explored their potential link to the physical stability of pharmaceutical suspensions. Surface tension measurements using pendant drop tensiometry revealed varying capacities of seven non-ionic surfactants to reduce the surface tension of water, with polysorbate 20 achieving the lowest equilibrium surface tension (36.07 ± 1.08 mN/m) and poloxamer 188 the highest (48.89 ± 0.20 mN/m). Contact angle measurements were performed between 0.5 mM, 1 mM, and 2 mM surfactant solutions and thin spin-coated drug films of eight model compounds to assess solid-liquid wettability and calculate the work of adhesion. All surfactant solutions exhibited contact angles below 90°, suggesting favorable spreading on drug compound surfaces, though compound-specific differences in wettability were observed. Some surfactant-drug compound combinations, such as polysorbate 20 with naproxen or TBAJ-876, showed contact angles near 0°, potentially indicating superspreading behavior. The work of adhesion, derived from surface tension and contact angles, generally decreased in the presence of surfactants compared to water, and slightly increased with higher surfactant concentration. Pharmaceutical suspensions with the eight model drug compounds were evaluated for physical stability, assessed by monitoring the particle size profiles for 28 days at 40 °C to assess stabilization efficiency to maintain the sizes of drug particles during storage. While some correlations between low work of adhesion and poor stabilizer performance were noted - such as vitamin E TPGS with bedaquiline and poloxamer 188 with haloperidol - no consistent trend was observed across all surfactants and drug compounds. Most data clustered closely, with outliers offering limited predictive value between interfacial measurements and particle size profiles. These findings therefore suggested that although interfacial energy measurements provided valuable insight into surfactant behavior and solid-liquid interactions, they were not sufficient as standalone predictors of physical stability in pharmaceutical suspensions.
100 项与 Sorfequiline 相关的药物交易
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研发状态
10 条进展最快的记录, 后查看更多信息
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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2期 | 美国 | 2023-10-31 | |
| 肺结核 | 临床2期 | 菲律宾 | 2023-10-31 | |
| 肺结核 | 临床2期 | 南非 | 2023-10-31 | |
| 肺结核 | 临床2期 | 坦桑尼亚 | 2023-10-31 | |
| 肺结核 | 临床2期 | 乌干达 | 2023-10-31 | |
| 耐多药结核病 | 临床1期 | 美国 | 2020-06-08 | |
| 潜伏性结核 | 临床前 | 美国 | 2025-10-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 309 | (TBAJ876 25 mg) | 簾衊壓遞膚醖糧餘繭齋(餘糧選淵遞夢築廠蓋網) = 獵選鏇鑰製壓觸顧顧鏇 醖鹹網製糧簾鏇觸願襯 (鹹簾鏇齋廠壓窪繭製築, 願糧襯願齋鹹壓獵鬱醖 ~ 憲鑰鏇膚窪艱鹽膚獵壓) | - | 2026-06-24 | ||
(TBAJ876 50 mg) | 簾衊壓遞膚醖糧餘繭齋(餘糧選淵遞夢築廠蓋網) = 網醖鑰蓋憲網積願壓糧 醖鹹網製糧簾鏇觸願襯 (鹹簾鏇齋廠壓窪繭製築, 簾窪廠鹹醖糧衊築繭廠 ~ 艱製廠願製獵窪製繭範) | ||||||
临床1期 | 28 | 製網淵襯鹹鬱齋夢糧醖(範簾廠製鹽構顧淵齋淵) = 鹽積觸築醖糧顧鬱鹹鹽 顧鏇簾構築醖觸淵鹹選 (鏇齋鏇築繭憲獵膚壓鬱, 鹹衊獵糧選膚壓蓋壓壓 ~ 鏇齋糧積憲範廠餘壓鏇) 更多 | - | 2024-10-08 |
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