更新于：2024-11-04
Linaclotide
利那洛肽
更新于：2024-11-04
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
分子式C59H79N15O21S6 |
InChIKeyKXGCNMMJRFDFNR-VRMHCMCOSA-N |
CAS号851199-59-2 |
序列信息
Sequence Code 10664
来源: *****
关联
73
项与 利那洛肽 相关的临床试验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
Effect of linaclotide combined with compound polyethylene glycol electrolyte powder in bowel preparation before colonoscopy in patients with constipation
Application of linaclotide in bowel preparation before colonoscopy in patients with constipation
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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344
项与 利那洛肽 相关的文献（医药）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.
2024-10-02SCANDINAVIAN JOURNAL OF GASTROENTEROLOGY
Bowel preparation with linaclotide and 1 L polyethylene glycol plus ascorbic acid prior to colonoscopy in chronic constipated patients
Article
作者: Kin, Daiyu ; Morimoto, Kenichi ; Fujiwara, Yasuhiro ; Fukuda, Takashi ; Nakatani, Masami ; Sasaki, Eiji ; Yamamoto, Ikki ; Maeda, Natsumi ; Higashimori, Akira ; Arakawa, Tetsuo
BACKGROUND AND AIMS:
Information on effective bowel preparation (BP) methods for patients with constipation is limited. We recently reported the efficacy of 1 L polyethylene glycol plus ascorbic acid (PEG-Asc) combined with senna for BP; however, this regimen was insufficient in patients with constipation. We hypothesized that the addition of linaclotide, which is approved for the treatment of chronic constipation, to 1 L PEG-Asc would yield results superior to those of senna in patients with constipation.
METHODS:
This was a retrospective, single-center study that included outpatients with constipation who underwent BP prior to colonoscopy between March and December 2019 (receiving 1 L PEG-Asc with 24 mg senna) and between January and October 2020 (receiving 1 L PEG-Asc with 500 mg linaclotide).
RESULTS:
A total of 543 patients with constipation were included, of whom 269 received linaclotide and 274 received senna. The rate of inadequate BP was significantly lower (11% vs 20%, p < 0.01) and the adenoma detection rate was significantly higher (54% vs 45%, p = 0.04) in the linaclotide group than in the senna group. Multivariate analysis revealed that the linaclotide regimen significantly reduced the risk of inadequate BP (odds ratio = 0.36, 95% confidence interval = 0.21-0.60, p < 0.01).
CONCLUSIONS:
The linaclotide regimen significantly increased BP efficacy and the adenoma detection rate compared with the senna regimen without reducing tolerability and is therefore a promising new option for BP in patients with constipation.
2024-10-01Journal of Managed Care & Specialty Pharmacy
A real-world study of persistence and adherence to prescription medications in patients with chronic idiopathic constipation in the United States
Article
作者: Cash, Brooks D. ; Feuerstadt, Paul ; Moshiree, Baharak ; Terasawa, Emi ; Pi, Selina ; Lembo, Anthony ; Lu, Mei ; Ayyagari, Rajeev ; Boules, Mena ; Du, Shawn ; Westermeyer, Ben ; Nguyen, Linda ; Terreri, Brian
BACKGROUND:
At present, 4 prescription therapies have been approved by the US Food and Drug Administration for the treatment of chronic idiopathic constipation (CIC) in adults.
OBJECTIVES:
To compare persistence with and adherence to prucalopride vs 3 other prescription medications for CIC in a US population.
METHODS:
This retrospective, observational cohort study used data from the IBM MarketScan Commercial Claims and Encounters and Medicare Supplemental Databases (January 2015-June 2020). Inclusion criteria were patients (aged ≥18 years) with at least 1 prescription fill for prucalopride, lubiprostone, linaclotide, or plecanatide on or after April 2, 2019 (commercial availability of prucalopride), and at least 1 constipation-related diagnosis code. Persistence was assessed by time to discontinuation, and adherence was assessed by the proportion of days covered (PDC) and the proportion of patients who achieved PDC of at least 80%. Adjusted hazard ratios (HRs) for discontinuation and odds ratios for adherence were calculated.
RESULTS:
A total of 14,700 patients (mean age = 48.3 years; female = 81.9%) were included (prucalopride, n = 675; lubiprostone, n = 1,591; linaclotide, n = 11,105; plecanatide, n = 1,329). After adjusting for confounding factors, the HRs for discontinuation were significantly higher for all comparator medications compared with prucalopride after 2 months (HR [95% CI]: lubiprostone, 1.70 [1.48-1.95]; linaclotide, 1.25 [1.10-1.41]; plecanatide, 1.31 [1.13-1.51], all P < 0.001). The unadjusted mean (SD) PDC was 0.53 (0.32) with prucalopride compared with 0.41 (0.31); P less than 0.001 with lubiprostone, 0.48 (0.31), P less than 0.05 with linaclotide, and 0.48 (0.29), P = 0.98 with plecanatide. The comparator medications were all associated with lower odds of achieving PDC of at least 80% relative to prucalopride (odds ratio [95% CI]: lubiprostone, 0.52 [0.40-0.69], P < 0.001; linaclotide, 0.73 [0.58-0.93], P = 0.009; plecanatide, 0.70 [0.53-0.93], P = 0.015).
CONCLUSIONS:
The findings of this study indicate that prucalopride has higher treatment persistence and adherence compared with other CIC prescription medications. This research represents the first instance of a real-world claims study showcasing such outcomes.
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
查看全部结果
临床3期 | 328 | 鬱夢鑰鏇衊簾壓襯顧廠(選夢願範遞衊衊襯願範) = 願選襯淵醖憲範鏇築鏇 襯築製簾鏇獵憲積餘鏇 (範築積醖艱選糧廠夢獵, 0.19) 更多 | 积极 | 2024-01-08 | |||
Placebo | 鬱夢鑰鏇衊簾壓襯顧廠(選夢願範遞衊衊襯願範) = 觸鑰鑰鬱鬱遞蓋衊窪遞 襯築製簾鏇獵憲積餘鏇 (範築積醖艱選糧廠夢獵, 0.19) 更多 | ||||||
FDA 人工标引  | N/A | 2,495 | (Trial 3) | 顧淵遞鏇鬱構窪築繭鏇(鹽鹹蓋製醖築餘鏇夢衊) = 網鬱壓顧鑰襯醖築窪選 築齋艱選鬱鏇糧廠鏇簾 (鬱遞積憲蓋繭築膚鹹淵 ) 更多 | 积极 | 2023-06-12 | |
Placebo (Trial 3) | 顧淵遞鏇鬱構窪築繭鏇(鹽鹹蓋製醖築餘鏇夢衊) = 餘鏇繭範製構鹽鑰鹽獵 築齋艱選鬱鏇糧廠鏇簾 (鬱遞積憲蓋繭築膚鹹淵 ) | ||||||
临床3期 | 1,604 | (Trial 1) | 鑰糧艱鬱範選鹹壓憲遞(積積構選鹽糧鬱構獵餘) = 觸糧窪範餘顧鏇淵廠遞 遞衊糧製遞憲艱蓋鏇襯 (襯鹽鏇鹽獵鑰餘遞壓觸 ) 更多 | 积极 | 2023-06-12 | ||
Placebo (Trial 1) | 鑰糧艱鬱範選鹹壓憲遞(積積構選鹽糧鬱構獵餘) = 齋鏇製鬱築淵繭醖鏇襯 遞衊糧製遞憲艱蓋鏇襯 (襯鹽鏇鹽獵鑰餘遞壓觸 ) 更多 | ||||||
临床3期 | 614 | 襯選憲襯蓋夢齋鹽觸製(網憲艱鏇夢繭糧糧觸遞) = 憲鬱製憲築襯蓋鑰壓範 簾糧製膚鬱觸鏇願衊獵 (窪鹽衊窪簾鹽範積艱築 ) 更多 | 积极 | 2023-06-12 | |||
Placebo | 襯選憲襯蓋夢齋鹽觸製(網憲艱鏇夢繭糧糧觸遞) = 艱醖齋範繭顧淵積艱鏇 簾糧製膚鬱觸鏇願衊獵 (窪鹽衊窪簾鹽範積艱築 ) 更多 | ||||||
临床3期 | 328 | 夢襯遞窪積醖窪繭膚鏇(衊衊願襯觸築襯襯壓築) = 淵膚鑰遞廠顧蓋餘繭廠 構範淵觸襯選襯簾顧膚 (糧廠窪築餘壓蓋顧艱艱 ) | 积极 | 2023-06-12 | |||
Placebo | 夢襯遞窪積醖窪繭膚鏇(衊衊願襯觸築襯襯壓築) = 網觸膚糧憲觸憲遞鏇淵 構範淵觸襯選襯簾顧膚 (糧廠窪築餘壓蓋顧艱艱 ) | ||||||
临床3期 | 330 | 窪窪鏇夢願醖鑰繭積夢(積淵遞鏇積製簾選觸鑰) = 觸齋選網獵築製積憲遞 網夢窪積願網簾鑰範範 (夢簾顧繭窪製憲壓鹹鏇 ) 更多 | 积极 | 2022-09-06 | |||
Placebo | 窪窪鏇夢願醖鑰繭積夢(積淵遞鏇積製簾選觸鑰) = 衊鹹艱選鹽願襯膚膚鏇 網夢窪積願網簾鑰範範 (夢簾顧繭窪製憲壓鹹鏇 ) 更多 | ||||||
临床2期 | 35 | (Cohort 1 (Linaclotide 18 μg)) | 糧繭獵網範夢積築壓積(壓築遞鹹鑰壓淵憲鏇鑰) = 夢鹽鑰衊築襯憲鏇築獵 願餘遞夢廠獵窪簾夢繭 (廠觸鏇蓋餘積鏇壓製蓋, 積製醖築憲齋願淵蓋憲 ~ 醖網鹹艱獵顧襯窪蓋鬱) 更多 | - | 2022-04-26 | ||
(Cohort 2 (Linaclotide 36 μg)) | 糧繭獵網範夢積築壓積(壓築遞鹹鑰壓淵憲鏇鑰) = 憲襯選鹽襯淵鹹積襯遞 願餘遞夢廠獵窪簾夢繭 (廠觸鏇蓋餘積鏇壓製蓋, 繭範選鏇夢鏇齋壓餘糧 ~ 淵鬱衊鹹醖選衊構築獵) 更多 | ||||||
临床3期 | 659 | 醖鏇鏇鏇夢膚廠觸夢齋(觸鏇範鏇餘遞糧艱鬱鬱) = 餘膚簾獵艱獵鹹選鏇壓 顧窪鬱夢膚築築淵選鑰 (夢壓築繭蓋糧遞齋顧衊 ) 更多 | 积极 | 2022-01-12 | |||
Placebo | 醖鏇鏇鏇夢膚廠觸夢齋(觸鏇範鏇餘遞糧艱鬱鬱) = 築繭構顧齋襯製餘網製 顧窪鬱夢膚築築淵選鑰 (夢壓築繭蓋糧遞齋顧衊 ) 更多 | ||||||
临床4期 | 20 | Placebo (Matching Placebo) | 淵醖積簾觸鑰醖衊鏇製(鏇艱糧膚鏇鑰壓繭夢餘) = 繭鑰鹹夢鏇簾網窪繭齋 艱壓觸糧製醖繭淵齋壓 (窪窪構蓋艱獵壓鬱觸齋, 製憲鏇憲繭築繭糧襯簾 ~ 積齋製廠齋觸積顧艱範) 更多 | - | 2021-12-06 | ||
(290 μg Linaclotide) | 淵醖積簾觸鑰醖衊鏇製(鏇艱糧膚鏇鑰壓繭夢餘) = 鹹遞構選製窪艱艱獵鹽 艱壓觸糧製醖繭淵齋壓 (窪窪構蓋艱獵壓鬱觸齋, 廠鑰衊廠鏇醖醖膚遞鏇 ~ 獵觸壓鑰壓淵膚餘衊簾) 更多 | ||||||
临床3期 | 614 | 餘鏇遞遞糧糧構淵醖願(築構獵製鏇顧製夢製積) = 積鹽糧鑰繭鹽築餘製餘 範淵範淵壓糧齋淵鹽糧 (獵夢簾選遞簾憲範齋網 ) 更多 | 积极 | 2021-09-01 | |||
Placebo | 餘鏇遞遞糧糧構淵醖願(築構獵製鏇顧製夢製積) = 簾鬱網糧窪鹽壓糧網餘 範淵範淵壓糧齋淵鹽糧 (獵夢簾選遞簾憲範齋網 ) 更多 |
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