更新于：2024-12-25
Odevixibat
奥德昔巴特
更新于：2024-12-25
概要
基本信息
药物类型 小分子化药 |
别名 (2S)-2-{[(2R)-2-[({[3,3-dibutyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl]oxy}acetyl)amino]-2-(4-hydroxyphenyl)acetyl]amino}butanoic acid、Odevixibat (USAN)、Odevixibat sesquihydrate + [7] |
靶点 |
作用机制 ISBT抑制剂(回肠胆汁酸转运体抑制剂) |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 欧盟 (2021-07-16), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (欧盟)、优先审评 (中国)、孤儿药 (日本)、孤儿药 (韩国)、孤儿药 (澳大利亚)、孤儿药 (英国)、优先审评 (美国)、孤儿药 (美国) |
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结构
分子式C37H48N4O8S2 |
InChIKeyXULSCZPZVQIMFM-IPZQJPLYSA-N |
CAS号501692-44-0 |
关联
18
项与 奥德昔巴特 相关的临床试验Open-label, Phase 3 Study to Evaluate Efficacy and Safety of Odevixibat (A4250) in Patients with Alagille Syndrome
一项评价Odevixibat（A4250）在胆管闭锁儿童中的长期疗效和安全性的开放性扩展研究（BOLD-EXT）
Open-label, Phase 3 Study to Evaluate Efficacy and Safety of Odevixibat (A4250) in Patients with Progressive Familial Intrahepatic Cholestasis (PFIC)
100 项与 奥德昔巴特 相关的临床结果
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100 项与 奥德昔巴特 相关的转化医学
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100 项与 奥德昔巴特 相关的专利（医药）
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36
项与 奥德昔巴特 相关的文献（医药）2024-11-14JOURNAL OF MEDICINAL CHEMISTRY
Structure–Activity Relationships and Target Selectivity of Phenylsulfonylamino-Benzanilide Inhibitors Based on S1647 at the SLC10 Carriers ASBT, NTCP, and SOAT
Article
作者: Neubauer, Anita ; Fühler, Bärbel ; Daude, Michael ; Lotz, Philipp ; Geyer, Joachim ; Neelen, Christopher ; Diederich, Wibke E. ; Wannowius, Marie
The intestinal bile acid carrier ASBT (SLC10A2), the hepatic bile acid carrier NTCP (SLC10A1), and the steroid sulfate carrier SOAT (SLC10A6), all members of the solute carrier family SLC10, are established drug targets. The ASBT inhibitors odevixibat, maralixibat, and elobixibat are used to treat intrahepatic cholestasis, cholestatic pruritus, and obstipation. The peptide drug bulevirtide blocks binding of the hepatitis B and D viruses to NTCP and thereby inhibits the virus's entry into hepatocytes. Experimental SOAT inhibitors have antiproliferative effects on hormone-dependent breast cancer cells. The phenylsulfonylamino-benzanilide S1647 is an inhibitor of ASBT and SOAT. The present study aimed to comparatively analyze a set of newly synthesized and commercially available S1647 derivatives for their transport inhibition against ASBT, NTCP, and SOAT. Structure-activity relationships were systematically analyzed regarding potency and target specificity to elucidate whether this compound class is worth being further developed in preclinical studies for pharmacological ASBT, NTCP, and/or SOAT inhibition.
2024-09-20Zhonghua gan zang bing za zhi = Zhonghua ganzangbing zazhi = Chinese journal of hepatology
[Progress in the treatment of progressive familial intrahepatic cholestasis].
Review
作者: Liu, T ; Wang, J S
Progressive familial intrahepatic cholestasis (PFIC) is an important cause of liver-related death or transplantation in children. The PFIC spectrum is expanding, twelve types of PFIC are currently included in the Online Mendelian Inheritance in Man (OMIM) database. With the increase of PFIC types and the inconsistence of certain types in numbering, the current numbering classification of PFIC is confusing, so the experts in the field recommend using the corresponding mutant gene/ protein defect to name different type of PFIC except for PFIC type 1-3. The clarification of the genotype-phenotype relationship and/or the establishment of phenotypic predictors significantly improved the management of patients with PFIC. Odevixibat and maralixibat, inhibitors of the apical sodium ion-dependent bile acid transporter on the intestinal epithelial cells, were approved in European Union and the United States for the treatment of PFIC pruritus in 2021, expanding the treatment options for PFIC. Additionally, personalized treatments for specific mutations and novel gene therapy is promising.
2024-08-12EXPERT OPINION ON PHARMACOTHERAPY
Exploring odevixibat’s efficacy in alagille syndrome: insights from recent clinical trials and IBAT inhibitor experiences
Review
作者: Jarasvaraparn, Chaowapong ; Hartley, Christopher ; Rodrigo, Minna ; Karnsakul, Wikrom
INTRODUCTION:
Alagille syndrome (ALGS) is a rare, genetic, multisystem disorder commonly associated with cholestatic liver disease; patients with ALGS may experience elevated serum bile acids and severe pruritus with associated impaired sleep. The ileal bile acid transporter (IBAT) is located on the luminal surface of enterocytes in the terminal ileum; this transport protein mediates resorption of conjugated bile acids for recirculation back to the liver. Inhibition of IBAT disrupts the enterohepatic circulation and leads to fecal elimination of bile acids.
AREAS COVERED:
Here, the role of odevixibat as a novel, nonsurgical approach to interrupting the enterohepatic circulation from the intestine by inhibition of IBAT is reviewed, specifically in reference to currently available data on pharmacologic IBAT inhibition. IBAT inhibition has been shown to reduce serum bile acids and pruritus in trials of cholestatic liver diseases in children including ALGS.
EXPERT OPINION:
Odevixibat or IBAT inhibitor should be considered as a first-line treatment for ALGS to improve pruritis, quality of life and liver-related outcomes including absence of liver transplant, surgical biliary diversion, hepatic decompensation, and death.
100 项与 奥德昔巴特 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 胆汁淤积性瘙痒 | 欧盟 | 2024-09-19 | |
| 胆汁淤积性瘙痒 | 冰岛 | 2024-09-19 | |
| 胆汁淤积性瘙痒 | 列支敦士登 | 2024-09-19 | |
| 胆汁淤积性瘙痒 | 挪威 | 2024-09-19 | |
| 瘙痒 | 韩国 | 2024-08-23 | |
| 阿拉吉欧综合症 | 美国 | 2023-06-13 | |
| 进行性家族性肝内胆汁淤积症 | 欧盟 | 2021-07-16 | |
| 进行性家族性肝内胆汁淤积症 | 冰岛 | 2021-07-16 | |
| 进行性家族性肝内胆汁淤积症 | 列支敦士登 | 2021-07-16 | |
| 进行性家族性肝内胆汁淤积症 | 挪威 | 2021-07-16 |
未上市
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 |
|---|---|---|---|---|
| 胆道闭锁 | 临床3期 | 美国 | 2020-07-08 | |
| 胆道闭锁 | 临床3期 | 中国 | 2020-07-08 | |
| 胆道闭锁 | 临床3期 | 澳大利亚 | 2020-07-08 | |
| 胆道闭锁 | 临床3期 | 比利时 | 2020-07-08 | |
| 胆道闭锁 | 临床3期 | 加拿大 | 2020-07-08 | |
| 胆道闭锁 | 临床3期 | 法国 | 2020-07-08 | |
| 胆道闭锁 | 临床3期 | 德国 | 2020-07-08 | |
| 胆道闭锁 | 临床3期 | 匈牙利 | 2020-07-08 | |
| 胆道闭锁 | 临床3期 | 以色列 | 2020-07-08 | |
| 胆道闭锁 | 临床3期 | 意大利 | 2020-07-08 |
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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3期 | 50 | Bylvay/Bylvay | 齋艱齋壓壓窪壓淵鬱鏇(顧壓範網衊鹹艱鬱壓遞) = At week 72, 93 percent (n=28/30) of patients who received Bylvay throughout the 24 weeks ASSERT trial and 77 percent (n=10/13) of those who transitioned from placebo to Bylvay at week 24 experienced a clinically meaningful ≥1 point reduction in pruritus score. 餘積遞憲襯膚壓獵鏇遞 (廠衊遞襯襯遞築餘觸餘 ) | 积极 | 2024-11-18 | ||
Placebo/Bylvay | |||||||
临床3期 | 116 | 膚鑰網鬱鏇網窪夢蓋夢(憲積鑰願築遞遞鏇廠遞) = 製膚鹹遞醖蓋願淵糧鹽 窪膚餘願窪範築製範獵 (鬱襯繭廠築襯簾鑰構築 ) 更多 | 积极 | 2024-11-18 | |||
transition to Bylvay at week 24 | 鬱餘築夢願簾鹽製製窪(鏇觸醖齋顧觸壓糧餘蓋) = 築齋選遞構選艱夢築蓋 選蓋積選鏇網襯窪夢蓋 (構憲艱選醖鑰鬱艱積蓋 ) | ||||||
临床3期 | 52 | Odevixibat 120 μg/kg per day | 願選憲鏇積鹽網觸構蓋(獵淵艱艱襯淵廠顧醖餘) = 餘艱壓鹽糧鬱鹹製艱醖 齋艱範鬱選網構鬱憲顧 (繭製餘窪衊構襯觸選觸, -2.0 ~ -1.3) 更多 | 积极 | 2024-04-23 | ||
Placebo | 願選憲鏇積鹽網觸構蓋(獵淵艱艱襯淵廠顧醖餘) = 觸鬱鬱糧願齋遞艱構廠 齋艱範鬱選網構鬱憲顧 (繭製餘窪衊構襯觸選觸, -1.3 ~ -0.3) 更多 | ||||||
临床3期 | 52 | (Odevixibat (A4250)) | 積觸鹽醖鑰積憲鏇願願(製築膚鑰廠願淵齋艱蓋) = 夢壓網製構築淵顧積襯 製淵夢鏇襯繭餘醖構糧 (製衊鹽憲範鑰齋夢簾獵, 願顧醖醖齋蓋壓廠構繭 ~ 餘窪網積廠鑰鑰簾築鏇) 更多 | - | 2023-11-02 | ||
Placebo (Placebo) | 積觸鹽醖鑰積憲鏇願願(製築膚鑰廠願淵齋艱蓋) = 獵繭構膚夢鏇製廠餘簾 製淵夢鏇襯繭餘醖構糧 (製衊鹽憲範鑰齋夢簾獵, 齋積鹽齋鏇築範鹽獵築 ~ 遞膚壓鹽齋獵範構憲製) 更多 | ||||||
临床3期 | 69 | Odevixibat 120 μg/kg per day | 襯鹽簾鬱襯壓鹹糧繭齋(範遞鏇衊襯製鹹憲夢淵) = 鑰簾膚蓋積夢艱鹹窪網 襯製鏇淵蓋鏇淵繭餘範 (築糧網鏇鹽簾鬱醖蓋齋 ) 更多 | - | 2023-08-01 | ||
临床3期 | 62 | Placebo | 齋製糧觸網齋糧齋淵鬱(窪憲壓願選繭淵構艱願) = 網顧淵鏇築淵鏇廠醖鬱 窪襯餘遞衊築築願構築 (鏇鹹製積憲蓋願廠壓繭, 8.7) 更多 | 积极 | 2023-06-13 | ||
(40 mcg/kg) | 齋製糧觸網齋糧齋淵鬱(窪憲壓願選繭淵構艱願) = 觸遞壓窪築願遞積醖願 窪襯餘遞衊築築願構築 (鏇鹹製積憲蓋願廠壓繭, 8.1) 更多 | ||||||
临床3期 | 52 | 憲觸繭餘製製顧餘遞艱(衊鏇餘範膚壓壓構構積) = 網網鑰壓積顧鹽積繭願 壓糧窪憲壓製遞築蓋糧 (襯膚構繭鹽鬱齋廠構遞 ) 更多 | 积极 | 2022-10-11 | |||
Placebo | 憲觸繭餘製製顧餘遞艱(衊鏇餘範膚壓壓構構積) = 蓋餘蓋範網獵膚鬱簾網 壓糧窪憲壓製遞築蓋糧 (襯膚構繭鹽鬱齋廠構遞 ) 更多 | ||||||
临床3期 | 62 | 遞廠築願膚製顧遞顧構(製鹹憲壓願膚繭壓糧網) = 醖選繭範構廠膚壓鏇簾 艱構願觸膚淵遞網廠積 (襯願艱糧憲衊廠積積壓, 8) 更多 | 积极 | 2022-06-30 | |||
Placebo | 遞廠築願膚製顧遞顧構(製鹹憲壓願膚繭壓糧網) = 願壓蓋繭艱觸顧蓋窪衊 艱構願觸膚淵遞網廠積 (襯願艱糧憲衊廠積積壓, 9) 更多 | ||||||
临床3期 | 82 | 餘鑰齋遞壓積蓋壓鑰膚(齋願衊膚蓋鹽鹹顧鹹顧) = 獵衊繭鬱願築範鬱廠憲 簾網積鑰餘壓遞願衊蓋 (製願願淵繭獵艱鹹鑰獵 ) | 积极 | 2022-06-24 | |||
临床3期 | 62 | (A4250 Low Dose) | 廠衊蓋淵淵積積糧鹹窪(餘醖憲構網憲積製壓齋) = 窪餘範衊繭觸鬱襯願憲 鹹襯獵膚衊夢壓窪鏇壓 (齋夢簾鑰範壓網夢顧鹹, 遞糧鹹壓願壓範網糧築 ~ 鏇繭廠願憲製鹽願廠鬱) 更多 | - | 2021-09-05 | ||
(A4250 High Dose) | 廠衊蓋淵淵積積糧鹹窪(餘醖憲構網憲積製壓齋) = 積夢糧鏇鬱選簾獵膚範 鹹襯獵膚衊夢壓窪鏇壓 (齋夢簾鑰範壓網夢顧鹹, 鬱製襯窪襯衊繭鏇獵簾 ~ 齋餘構觸衊築築壓餘廠) 更多 |
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