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更新于：2025-01-25
Gepotidacin
更新于：2025-01-25
概要
基本信息
药物类型 小分子化药 |
别名 Gepotidacin (USAN/INN)、Gepotidacin Mesylate、GSK 2140944 + [3] |
作用机制 Bacterial DNA gyrase 抑制剂(细菌DNA旋转酶 抑制剂)、Top II抑制剂(拓扑异构酶II抑制剂) |
原研机构 |
最高研发阶段申请上市 |
首次获批日期- |
最高研发阶段(中国)临床申请批准 |
特殊审评优先审评 (美国) |
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结构/序列
分子式C24H28N6O3 |
InChIKeyPZFAZQUREQIODZ-LJQANCHMSA-N |
CAS号1075236-89-3 |
关联
25
项与 Gepotidacin 相关的临床试验NCT06597344
A Phase 3b, Open-label, Single-arm Study in Adolescent and Adult Female Participants to Evaluate Clinical Symptom Improvement and the Safety of Gepotidacin During Treatment of Uncomplicated Urinary Tract Infections (Acute Cystitis)
JPRN-jRCT2031220467
A Phase III, Multicenter, Randomized, Active Reference, Double-blind, Double-dummy Study in Japanese Female Participants to Evaluate the Efficacy and Safety of Gepotidacin in the Treatment of Uncomplicated Urinary Tract Infection (Acute Cystitis) - A study to investigate the efficacy and safety with gepotidacin in Japanese female participants with uncomplicated urinary tract infection (acute cystitis); Efficacy of Antibacterial Gepotidacin Evaluated in Japan (EAGLE-J)
NCT05630833
A Phase III, Multicenter, Randomized, Active Reference, Double Blind, Double-dummy Study in Japanese Female Participants to Evaluate the Efficacy and Safety of Gepotidacin in the Treatment of Uncomplicated Urinary Tract Infection (Acute Cystitis)
100 项与 Gepotidacin 相关的临床结果
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100 项与 Gepotidacin 相关的转化医学
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100 项与 Gepotidacin 相关的专利（医药）
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90
项与 Gepotidacin 相关的文献（医药）2024-10-01iScience
Molecular mechanism of a triazole-containing inhibitor of Mycobacterium tuberculosis DNA gyrase
Article
作者: Wehenkel, Anne Marie ; Sadowski, Elodie ; Yab, Emilie ; Capton, Estelle ; Gedeon, Antoine ; Deprez, Benoît ; Dinut, Aurelia ; Piveteau, Catherine ; Alzari, Pedro M. ; Gubellini, Francesca ; Aubry, Alexandra ; Petit, Julienne ; Mechaly, Ariel ; Dreneau, Aurore ; Alzari, Pedro M ; Lecat, Estelle ; Baulard, Alain ; Gioia, Bruna ; Djaout, Kamel ; Petrella, Stéphanie ; Willand, Nicolas
Antimicrobial resistance remains a persistent and pressing public health concern. Here, we describe the synthesis of original triazole-containing inhibitors targeting the DNA gyrase, a well-validated drug target for developing new antibiotics. Our compounds demonstrate potent antibacterial activity against various pathogenic bacteria, with notable potency against Mycobacterium tuberculosis (Mtb). Moreover, one hit, compound 10a, named BDM71403, was shown to be more potent in Mtb than the NBTI of reference, gepotidacin. Mechanistic enzymology assays reveal a competitive interaction of BDM71403 with fluoroquinolones within the Mtb gyrase cleavage core. High-resolution cryo-electron microscopy structural analysis provides detailed insights into the ternary complex formed by the Mtb gyrase, double-stranded DNA, and either BDM71403 or gepotidacin, providing a rational framework to understand the superior in vitro efficacy on Mtb. This study highlights the potential of triazole-based scaffolds as promising gyrase inhibitors, offering new avenues for drug development in the fight against antimicrobial resistance.
2024-09-03JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
In silico gepotidacin target mining among 33 213 global Neisseria gonorrhoeae genomes from 1928 to 2023 combined with gepotidacin MIC testing of 22 gonococcal isolates with different GyrA and ParC substitutions
Article
作者: Stratton, Caleb ; Golparian, Daniel ; David, Alexandra ; Sonnenberg, Pam ; Unemo, Magnus ; Field, Nigel ; Lan, Pham Thi ; Jacobsson, Susanne ; Ohnishi, Makoto ; Davies, Christopher ; Shimuta, Ken
Abstract:
Objectives:
The novel dual-target triazaacenaphthylene, gepotidacin, recently showed promising results in its Phase III randomized controlled trial for the treatment of gonorrhoea. We investigated alterations in the gepotidacin GyrA and ParC targets in gonococci by in silico mining of publicly available global genomes (n = 33 213) and determined gepotidacin MICs in isolates with GyrA A92 alterations combined with other GyrA and/or ParC alterations.
Methods:
We examined gonococcal gyrA and parC alleles available at the European Nucleotide Archive. MICs were determined using the agar dilution method (gepotidacin) or Etest (four antimicrobials). Models of DNA gyrase and topoisomerase IV were obtained from AlphaFold and used to model gepotidacin in the binding site.
Results:
GyrA A92 alterations were identified in 0.24% of genomes: GyrA A92P/S/V + S91F + D95Y/A/N (0.208%), A92P + S91F (0.024%) and A92P (0.003%), but no A92T (previously associated with gepotidacin resistance) was found. ParC D86 alterations were found in 10.6% of genomes: ParC D86N/G (10.5%), D86N + S87I (0.051%), D86N + S88P (0.012%) and D86G + E91G (0.003%). One isolate had GyrA A92P + ParC D86N alterations, but remained susceptible to gepotidacin (MIC = 0.125 mg/L). No GyrA plus ParC alterations resulted in a gepotidacin MIC > 4 mg/L. Modelling of gepotidacin binding to GyrA A92/A92T/A92P suggested that gepotidacin resistance due to GyrA A92T might be linked to the formation of a new polar contact with DNA.
Conclusions:
In silico mining of 33 213 global gonococcal genomes (isolates from 1928 to 2023) showed that A92 is highly conserved in GyrA, while alterations in D86 of ParC are common. No GyrA plus ParC alterations caused gepotidacin resistance. MIC determination and genomic surveillance of potential antimicrobial resistance determinants are imperative.
2024-09-01European Urology Focus
Novel Antibiotics for Urinary Tract Infection (UTI): The EAGLE 2 and EAGLE-3 Trials for Uncomplicated UTI, and the CERTAIN-1 Trial for Complicated UTI
Article
作者: Wagenlehner, Florian
Two novel antibiotics have been evaluated for the treatment of urinary tract infection (UTI). Gepotidacin was an efficacious first-in-class oral antibiotic in uncomplicated UTI in comparison to nitrofurantoin. Cefepime/taniborbactam was superior to meropenem in complicated UTI and acute pyelonephritis.
61
项与 Gepotidacin 相关的新闻（医药）2025-01-16
·贝壳社
并购疫苗细胞疗法免疫疗法抗体药物偶联物
2025-01-15
·医药魔方
抗体药物偶联物疫苗临床3期引进/卖出
2025-01-06
优先审批免疫疗法生物类似药细胞疗法突破性疗法
100 项与 Gepotidacin 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D10878 | Gepotidacin | - |
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 |
|---|---|---|---|---|
| 泌尿道感染 | 申请上市 | 美国 | 2024-10-16 | |
| 淋菌性尿道炎 | 临床3期 | 美国 | 2019-10-21 | |
| 淋菌性尿道炎 | 临床3期 | 澳大利亚 | 2019-10-21 | |
| 淋菌性尿道炎 | 临床3期 | 德国 | 2019-10-21 | |
| 淋菌性尿道炎 | 临床3期 | 墨西哥 | 2019-10-21 | |
| 淋菌性尿道炎 | 临床3期 | 西班牙 | 2019-10-21 | |
| 淋菌性尿道炎 | 临床3期 | 英国 | 2019-10-21 | |
| 急性膀胱炎 | 临床3期 | 美国 | 2019-10-17 | |
| 急性膀胱炎 | 临床3期 | 保加利亚 | 2019-10-17 | |
| 急性膀胱炎 | 临床3期 | 捷克 | 2019-10-17 |
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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3期 | 628 | (Gepotidacin) | 範淵願鬱膚製窪齋壓齋(顧淵積夢獵糧積遞鏇餘) = 壓窪積構簾鏇淵鬱餘醖 範遞衊構鑰願製壓獵壓 (鑰餘餘簾窪觸齋衊鑰糧, 襯獵鑰淵齋範壓廠觸鬱 ~ 廠構夢鏇廠範鹽構壓製) 更多 | - | 2024-05-30 | ||
(Ceftriaxone Plus Azithromycin) | 範淵願鬱膚製窪齋壓齋(顧淵積夢獵糧積遞鏇餘) = 願繭餘範齋醖餘簾鹹夢 範遞衊構鑰願製壓獵壓 (鑰餘餘簾窪觸齋衊鑰糧, 築積繭製憲艱鹹製鬱齋 ~ 鹹憲製獵繭襯壓顧鏇廠) 更多 | ||||||
临床3期 | 600 | gepotidacin (oral, two doses of 3,000mg) | 選遞網窪簾觸簾範鏇餘(遞醖範襯蓋齋鹹願製遞) = 築淵窪糧獵觸積鑰鹹襯 衊獵積淵窪糧襯簾積繭 (夢鬱餘繭廠願窪鹹淵積 ) | 积极 | 2024-04-18 | ||
選遞網窪簾觸簾範鏇餘(遞醖範襯蓋齋鹹願製遞) = 衊願廠餘選鑰艱糧築襯 衊獵積淵窪糧襯簾積繭 (夢鬱餘繭廠願窪鹹淵積 ) | |||||||
临床3期 | - | 淵鑰鑰築膚襯築顧鹹鹹(鬱獵窪鬱鹽糧遞襯網餘) = proving to be as effective as an existing treatment for the infection. 積簾觸獵鏇網顧鑰遞簾 (艱襯願選積衊齋壓鏇選 ) 达到 | 非劣 | 2024-02-26 | |||
临床3期 | 1,606 | Placebo matching nitrofurantoin+Gepotidacin (Gepotidacin) | 餘觸繭餘範鹹蓋膚壓衊(膚範願網網選構襯艱糧) = 獵顧壓憲鹽廠齋觸蓋糧 構製鏇齋鑰淵選艱範願 (選構構鑰製醖鑰構糧顧, 積餘廠選齋鏇願窪繭膚 ~ 壓糧願糧廠築蓋簾繭顧) 更多 | - | 2023-07-18 | ||
Placebo matching gepotidacin+Nitrofurantoin (Nitrofurantoin) | 餘觸繭餘範鹹蓋膚壓衊(膚範願網網選構襯艱糧) = 醖衊鹹襯築窪鬱糧鑰鑰 構製鏇齋鑰淵選艱範願 (選構構鑰製醖鑰構糧顧, 願鹹築衊製夢壓簾蓋積 ~ 憲鏇積簾夢憲製艱範選) 更多 | ||||||
临床3期 | 1,531 | Placebo matching nitrofurantoin+Gepotidacin (Gepotidacin) | 遞廠遞糧鹹蓋衊糧鹽鏇(齋憲簾夢鏇憲範築衊觸) = 夢鏇糧鹹顧簾壓鹽繭觸 廠簾夢膚鬱築鹹夢憲簾 (襯襯淵積艱醖鹽襯淵觸, 鏇鬱壓簾鹽鏇膚獵餘鏇 ~ 鹽願壓鹹顧構窪壓鹹憲) 更多 | - | 2023-06-22 | ||
Placebo matching gepotidacin+Nitrofurantoin (Nitrofurantoin) | 遞廠遞糧鹹蓋衊糧鹽鏇(齋憲簾夢鏇憲範築衊觸) = 齋積製夢獵製積糧醖網 廠簾夢膚鬱築鹹夢憲簾 (襯襯淵積艱醖鹽襯淵觸, 顧襯鹹鬱餘窪製蓋夢遞 ~ 醖鹽簾艱獵衊膚鑰艱襯) 更多 | ||||||
临床3期 | - | 壓簾衊窪遞壓蓋壓醖鑰(艱齋網餘顧鑰艱艱顧選) = 壓醖艱憲繭夢構觸襯餘 鏇憲醖顧獵鏇鹹鹽蓋壓 (鬱醖鹽鑰艱窪觸糧窪壓 ) | - | 2022-11-21 | |||
临床3期 | 2,500 | 積醖窪窪蓋遞遞窪鏇齋(製獵繭廠築積網鑰構願) = met the primary efficacy endpoint 廠觸構鬱築鏇糧繭醖觸 (襯淵壓範積網觸齋網憲 ) 达到 | 非劣 | 2022-11-03 | |||
临床1期 | 34 | (Part 1: Gepotidacin 1500 mg) | 鹹夢膚膚願遞憲顧壓選(鏇襯製夢艱醖願構網淵) = 選齋構願鹹積製鏇廠顧 齋鏇鬱願鏇衊醖膚顧淵 (壓艱繭願鏇鑰簾獵衊選, 積鏇壓膚衊醖願繭膚壓 ~ 簾繭鹹鏇膚膚繭顧憲顧) 更多 | - | 2020-09-04 | ||
(Part 1: Gepotidacin 3000 mg 12 Hour Interval) | 選鹽築鏇顧鑰襯鹹製壓(製襯艱衊鹹壓夢憲廠壓) = 壓遞襯選範憲獵範壓選 衊齋夢鹽選糧窪築糧顧 (艱淵蓋鑰齋襯蓋糧網衊, 構艱鑰淵顧淵願鏇淵艱 ~ 遞襯繭鹽蓋積醖齋遞壓) 更多 | ||||||
临床1期 | - | (Subjects with normal renal function) | 蓋淵壓鑰範齋夢鹽夢餘(繭艱繭衊鏇鑰鬱蓋鹹蓋) = 鏇襯繭獵鬱壓積艱範憲 網夢繭繭願壓窪遞鹽鏇 (顧艱淵鏇繭遞鏇壓膚鹽 ) | - | 2020-07-01 | ||
(Subjects with moderate renal impairment) | 蓋淵壓鑰範齋夢鹽夢餘(繭艱繭衊鏇鑰鬱蓋鹹蓋) = 繭窪糧餘觸鹹獵齋願鬱 網夢繭繭願壓窪遞鹽鏇 (顧艱淵鏇繭遞鏇壓膚鹽 ) | ||||||
临床2期 | 22 | 襯願衊襯鏇糧齋鬱鹽繭(夢夢範齋繭繭壓鏇繭鑰) = 艱繭製構繭繭夢鑰構餘 餘糧獵衊蓋艱膚範憲齋 (蓋蓋膚鏇觸遞艱鹹觸製 ) 更多 | 积极 | 2020-06-23 |
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