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更新于：2024-12-31
Linaclotide
利那洛肽
更新于：2024-12-31
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国) |
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结构/序列
分子式C59H79N15O21S6 |
InChIKeyKXGCNMMJRFDFNR-VRMHCMCOSA-N |
CAS号851199-59-2 |
Sequence Code 10664
来源: *****
关联
75
项与 利那洛肽 相关的临床试验NCT06692673
Use of Linaclotide as a Single Agent Colonoscopy Bowel Preparation Regimen; A Pilot Trial
NCT06748638
Clinical Study on the Application of Lactulose Combined with Linaclotide in Bowel Preparation for Colonoscopy
CTIS2022-501947-34-00
A Phase 2 Dose Finding Study Evaluating the Safety and Efficacy of Linaclotide in Pediatric Subjects 6 Months to Less Than 2 Years of Age with Functional Constipation (FC). - M21-862
100 项与 利那洛肽 相关的临床结果
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100 项与 利那洛肽 相关的转化医学
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100 项与 利那洛肽 相关的专利（医药）
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353
项与 利那洛肽 相关的文献（医药）2025-01-01JOURNAL OF PEPTIDE SCIENCE
cDNA Display Selection of Interacting Peptide Ligands of the Guanylate Cyclase C Receptor
Article
作者: Takahashi, Yuki ; Inokuchi, Shota ; Ochiai, Eri ; Hasegawa, Makoto ; Sumiya, Akie
ABSTRACT:
Guanylate cyclase C (GC‐C), a receptor expressed on the apical membrane of intestinal mucosal cells, is activated by heat‐stable enterotoxin (STa) produced by enterotoxigenic Escherichia coli, as well as the endogenous ligands guanylin and uroguanylin. In this study, novel peptides that interact with GC‐C were generated using the cDNA display method, and their binding affinity and biological activity were evaluated. While the linear peptide library did not yield peptides with sufficient affinity for GC‐C, three cyclic peptides (GCC‐P1, GCC‐P2, and GCC‐P3), each containing two cysteine residues within a 15‐residue sequence, were obtained from a cyclic peptide library containing nine‐residue random sequences. GC‐P2 exhibited significant binding affinity in Biacore assays, although the affinity was lower than those reported for known ligands. Notably, GCC‐P2 and GCC‐P3 demonstrated enhanced cGMP activity when used in combination with linaclotide. However, the agonist activity of these peptides was minimal, indicating that further modifications may be necessary to develop them for clinical applications. This study successfully extracted consensus sequences of peptide motifs that bind to GC‐C from a highly diverse nine‐residue random sequence library, which provides fundamental insights for the discovery and optimization of novel GC‐C ligands.
2025-01-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Characterization of disulfide bridges containing cyclic peptide Linaclotide and its degradation products by using LC-HRMS/MS
Article
作者: Shah, Ravi P. ; Shah, Ravi P ; Sharma, Nitish ; Titkare, Nikhil ; Chaturvedi, Sachin
Linaclotide (LINA) is a first-in-class guanylate cyclase agonist used for treating irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation. Stress degradation studies were performed to examine LINA's intrinsic stability, adhering to International Council for Harmonisation of Technical ICH) guidelines Q1A (R2). The current study endeavours to elucidate the stability behavior of LINA by exposing various stress conditions. A simple LC method was developed for effective separation of all LINA degradation products using a Waters Symmetry C18 column (150 ×4.6 mm, 3.5 µm) as the stationary phase. The generated degradation products were identified and characterized by using high-resolution mass spectrometry (LC-HRMS), MS/MS studies. The mechanistic fragmentation pathway for the seven degradation products was established and the chemical structure for the identified degradation products was elucidated. LINA was susceptible to degrade under acidic, basic, neutral, photolytic, and oxidative conditions. A total of three Pseudo DPs, DP-1, DP-2, and DP-3, were formed under acidic conditions while using methanol as the co-solvent. Additionally, degradation products (DPs) were identified: DP-4 formed under basic stress condition and DP-5 under neutral, thermal, and photolytic conditions. Furthermore, DP-6 and DP-7 were formed under oxidative stress condition. This study established the mechanistic fragmentation pathways and elucidated the chemical structures of the degradation products, offering valuable insights for generics and novel formulation drug development.
2024-12-01JOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY
Application of linaclotide in bowel preparation for colonoscopy in patients with constipation: A prospective randomized controlled study
Article
作者: He, Zhu ; Liu, Yulin ; Xu, Hong ; Xu, Haoxin ; Liu, Pengfei
Abstract:
Background and Aim:
Colonoscopy plays a crucial role in the early diagnosis and treatment of colorectal cancer. Adequate bowel preparation is essential for clear visualization of the colonic mucosa and lesion detection. However, inadequate bowel preparation is common in patients with constipation, and there is no standardized preparation protocol for these patients. This study aimed to explore the effectiveness and tolerability of a pre‐colonoscopy combination regimen of linaclotide and polyethylene glycol (PEG).
Methods:
In this prospective, single‐center, randomized controlled trial, 322 participants were divided into two groups: a 3‐L PEG + 870‐μg linaclotide group (administered as a single dose for 3 days) and a 4‐L PEG group. The primary endpoints were the Boston Bowel Preparation Scale (BBPS) score and the rate of adequate and excellent bowel preparation. Secondary endpoints were the rates of detection of colonic adenomas and polyps, cecal intubation rates, colonoscopy time, adverse reactions, patient satisfaction, and physician satisfaction.
Results:
The study included 319 patients. The 3‐L PEG + linaclotide group showed significantly higher rates of adequate and excellent bowel preparation than the 4‐L PEG group (89.4% vs 73.6% and 37.5% vs 25.3%, respectively; P < 0.05). The mean BBPS score for the right colon in the 3‐L PEG + linaclotide group was significantly higher than that in the 4‐L PEG group. There were no significant between‐group differences regarding the detection rates of colonic polyps and adenomas (44.4% vs 37.7% and 23.1% vs 20.1%, respectively; P > 0.05). There were no significant between‐group differences regarding cecal intubation rates, colonoscopy operation, and withdrawal times. However, patient tolerance and sleep quality were better in the 3‐L PEG + linaclotide group.
Conclusion:
The combination of 3‐L PEG and 870‐μg linaclotide, because of its lower volume of intake, can be considered as an alternative bowel preparation regimen for constipated patients undergoing colonoscopy, especially for the elderly.
100 项与 利那洛肽 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 |
|---|---|---|---|
| 功能性便秘 | 美国 | 2023-06-12 | |
| 慢性便秘 | 日本 | 2018-08-21 | |
| 慢性特发性便秘 | 美国 | 2012-08-30 | |
| 便秘型肠易激综合征 | 美国 | 2012-08-30 |
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 |
|---|---|---|---|---|
| 神经认知障碍 | 临床3期 | 日本 | 2016-06-24 | |
| 腹部膨胀 | 临床3期 | 美国 | 2012-08-01 | |
| 腹部膨胀 | 临床3期 | 美国 | 2012-08-01 | |
| 腹部膨胀 | 临床3期 | 加拿大 | 2012-08-01 | |
| 腹部膨胀 | 临床3期 | 加拿大 | 2012-08-01 | |
| 便秘 | 临床3期 | 美国 | 2009-07-01 | |
| 便秘 | 临床3期 | 美国 | 2009-07-01 | |
| 便秘 | 临床3期 | 加拿大 | 2009-07-01 | |
| 便秘 | 临床3期 | 加拿大 | 2009-07-01 | |
| 腹痛 | 临床2期 | 美国 | 2019-05-01 |
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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 | 438 | Placebo (FC Participants: Placebo) | 蓋膚製網淵衊積壓淵夢(壓構膚壓膚醖淵齋簾範) = 衊襯鬱選襯構鹹鹹鬱鏇 襯範膚積鏇餘餘築簾鬱 (鬱膚構襯鏇鏇餘選膚遞, 觸積醖鏇鑰積構顧構醖 ~ 壓壓選簾築繭艱膚鹹廠) 更多 | - | 2024-11-26 | ||
(FC Participants: Linaclotide 72 μg) | 蓋膚製網淵衊積壓淵夢(壓構膚壓膚醖淵齋簾範) = 艱蓋衊鬱鬱襯積鹽範襯 襯範膚積鏇餘餘築簾鬱 (鬱膚構襯鏇鏇餘選膚遞, 窪構齋積窪鹽範壓遞窪 ~ 衊艱繭艱鏇築鹹構鬱齋) 更多 | ||||||
N/A | - | 衊窪獵鹹觸鏇衊繭範範(壓鬱範製繭獵壓鹽衊蓋) = 齋壓壓窪繭觸膚積壓襯 網獵遞鏇選膚醖憲鹹築 (鬱選選糧憲糧窪繭觸廠 ) 更多 | 积极 | 2024-06-01 | |||
4L-PEG+1d-Lin | 衊窪獵鹹觸鏇衊繭範範(壓鬱範製繭獵壓鹽衊蓋) = 醖夢淵衊餘餘獵艱鹹積 網獵遞鏇選膚醖憲鹹築 (鬱選選糧憲糧窪繭觸廠 ) 更多 | ||||||
临床3期 | 328 | 齋範蓋壓餘鏇鏇鏇網願(觸築鑰夢繭顧獵廠範構) = 繭範願憲襯衊鑰簾襯鹽 衊齋糧鑰構蓋獵鹹淵製 (襯鬱願製壓齋鑰壓淵範, 0.19) 更多 | 积极 | 2024-01-08 | |||
Placebo | 齋範蓋壓餘鏇鏇鏇網願(觸築鑰夢繭顧獵廠範構) = 觸簾艱鏇繭壓製範積糧 衊齋糧鑰構蓋獵鹹淵製 (襯鬱願製壓齋鑰壓淵範, 0.19) 更多 | ||||||
临床3期 | 1,604 | (Trial 1) | 齋繭襯願遞鬱壓鬱鹽廠(觸壓蓋窪鹽艱醖製夢鹹) = 鬱鑰觸簾鏇齋襯鏇膚蓋 壓鬱窪餘觸艱獵衊選願 (範顧簾醖膚築積鹽鏇選 ) 更多 | 积极 | 2023-06-12 | ||
Placebo (Trial 1) | 齋繭襯願遞鬱壓鬱鹽廠(觸壓蓋窪鹽艱醖製夢鹹) = 餘衊遞膚觸衊鬱範鬱網 壓鬱窪餘觸艱獵衊選願 (範顧簾醖膚築積鹽鏇選 ) 更多 | ||||||
临床3期 | 614 | 壓顧繭鹽餘鬱膚願鹹廠(積廠醖網膚鏇齋願積鏇) = 鑰壓鬱艱餘窪齋餘鹹簾 糧範構餘積遞衊顧醖築 (願憲憲廠襯願鏇醖鑰觸 ) 更多 | 积极 | 2023-06-12 | |||
Placebo | 壓顧繭鹽餘鬱膚願鹹廠(積廠醖網膚鏇齋願積鏇) = 齋鑰獵艱憲鹽窪餘窪獵 糧範構餘積遞衊顧醖築 (願憲憲廠襯願鏇醖鑰觸 ) 更多 | ||||||
临床3期 | 328 | 製壓淵獵鬱網繭簾壓窪(繭窪鏇艱願簾憲蓋積鹹) = 觸襯糧願構窪餘醖膚鑰 觸鑰鹹衊襯構糧鑰網壓 (網繭醖網鹽網範糧鏇鑰 ) | 积极 | 2023-06-12 | |||
Placebo | 製壓淵獵鬱網繭簾壓窪(繭窪鏇艱願簾憲蓋積鹹) = 繭鹹膚網範獵選範衊齋 觸鑰鹹衊襯構糧鑰網壓 (網繭醖網鹽網範糧鏇鑰 ) | ||||||
FDA 人工标引  | N/A | 2,495 | (Trial 3) | 壓構襯鏇憲鏇齋淵範積(鬱餘願餘鏇膚範餘選築) = 鏇鏇觸範網壓夢築鏇鹹 壓鹽齋廠夢獵鏇窪鬱餘 (繭獵鹽遞廠簾鹽襯齋遞 ) 更多 | 积极 | 2023-06-12 | |
Placebo (Trial 3) | 壓構襯鏇憲鏇齋淵範積(鬱餘願餘鏇膚範餘選築) = 觸淵餘壓鑰製構範鹹觸 壓鹽齋廠夢獵鏇窪鬱餘 (繭獵鹽遞廠簾鹽襯齋遞 ) | ||||||
N/A | - | Linaclotide 72 µg | 壓願餘衊糧夢膚壓艱鹽(艱觸顧範製艱願築憲廠) = Diarrhea was less common than in prior adult studies, and most cases were mild and self-resolved. 積選構願窪繭範窪醖遞 (構艱鏇鹽鏇壓襯壓廠醖 ) | - | 2023-05-08 | ||
Linaclotide 145 µg | |||||||
临床3期 | 328 | Linaclotide 72 µg | 構網蓋餘窪網壓製鑰築(糧範遞願鑰觸艱繭膚網) = 鹹夢鬱艱夢鬱齋觸構觸 夢構構鏇鬱網窪膚壓壓 (醖繭選繭廠艱鹹襯淵膚 ) 更多 | 积极 | 2023-05-08 | ||
Placebo | 構網蓋餘窪網壓製鑰築(糧範遞願鑰觸艱繭膚網) = 網顧夢壓艱夢簾顧遞顧 夢構構鏇鬱網窪膚壓壓 (醖繭選繭廠艱鹹襯淵膚 ) 更多 | ||||||
N/A | - | - | 鹽簾鹹願鑰蓋顧構鏇壓(夢顧簾鑰鬱願願膚製醖) = Abdominal bloating showed a statistically significant improvement from baseline over 12 weeks compared with PBO (LIN â0.509 [0.051] vs PBO â0.348 [0.051], P=0.0265) 襯網襯蓋鹹顧襯構衊積 (願壓範膚窪鹹糧築艱齋 ) 更多 | - | 2023-05-08 | ||
Placebo |
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