更新于：2024-11-16
Lotiglipron
更新于：2024-11-16
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
最高研发阶段临床1期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构
分子式C31H31ClN4O5 |
InChIKeySVPYZAJTWFQTSM-UGDMGKLASA-N |
CAS号2401892-75-7 |
关联
12
项与 Lotiglipron 相关的临床试验A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE STUDY TO ESTIMATE THE EFFECT OF PF-07081532 ADMINISTRATION ON THE SINGLE-DOSE PHARMACOKINETICS OF DABIGATRAN AND ROSUVASTATIN IN OVERWEIGHT OR OBESE ADULT PARTICIPANTS
A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE STUDY TO EVALUATE THE EFFECT OF ITRACONAZOLE AND CYCLOSPORINE ON THE SINGLE-DOSE PHARMACOKINETICS OF PF-07081532 IN OVERWEIGHT OR OBESE ADULT PARTICIPANTS
A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE STUDY TO EVALUATE THE EFFECT OF TWO STEADY-STATE DOSE LEVELS OF PF-07081532 ON THE PHARMACOKINETICS OF SINGLE-DOSE MIDAZOLAM, OMEPRAZOLE AND AN ORAL CONTRACEPTIVE, AND THE EFFECT OF STEADY-STATE SEMAGLUTIDE ON THE PHARMACOKINETICS OF SINGLE-DOSE MIDAZOLAM, IN OBESE ADULT FEMALE PARTICIPANTS
100 项与 Lotiglipron 相关的临床结果
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100 项与 Lotiglipron 相关的转化医学
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100 项与 Lotiglipron 相关的专利（医药）
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1
项与 Lotiglipron 相关的文献（医药）2024-08-01DIABETES OBESITY & METABOLISM
Once‐daily oral small‐molecule glucagon‐like peptide‐1 receptor agonist lotiglipron (PF‐07081532) for type 2 diabetes and obesity: Two randomized, placebo‐controlled, multiple‐ascending‐dose Phase 1 studies
Article
作者: Tsamandouras, Nikolaos ; Brown, Lisa S. ; Saxena, Aditi R. ; Carvajal‐Gonzalez, Santos ; Buckeridge, Clare ; Hernandez‐Illas, Martha
Abstract:
Aim:
To investigate the effects of lotiglipron (PF‐07081532), a once‐daily, oral small‐molecule glucagon‐like peptide‐1 receptor agonist, in participants with type 2 diabetes (T2D) and/or obesity.
Materials and Methods:
Two Phase 1 randomized, double‐blind, placebo‐controlled, multiple‐ascending‐dose studies were conducted to investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of lotiglipron.
Results:
Across the studies, 74 participants with T2D were treated for 28 or 42 days, and 26 participants with obesity without diabetes were treated for 42 days, following randomization to placebo or lotiglipron (target doses 10–180 mg/day, with dose titration to higher target doses). Most adverse events were mild (89.6%), with nausea the most frequently reported in both studies. There were no clinically meaningful adverse trends noted in safety laboratory tests, vital signs, or electrocardiogram parameters. In participants with T2D, lotiglipron resulted in dose‐dependent reductions in mean daily glucose. The 180‐mg dose was associated with least squares mean decreases from baseline in glycated haemoglobin (−1.61% [90% confidence interval {CI} –2.08, −1.14] vs. −0.61% [−1.56, 0.34] for placebo) and body weight (−5.10 kg [90% CI –6.62, −3.58] vs. −2.06 kg [90% CI –4.47, 0.36] for placebo) after 42 days; a similar magnitude of weight loss was seen in participants with obesity. The observed pharmacokinetic profile supported once‐daily dosing.
Conclusions:
The profile of once‐daily lotiglipron with doses up to 180 mg, as observed in these two Phase 1 studies, indicated a safety and tolerability profile consistent with the mechanism of action, with dose‐dependent reductions in glycaemic indices (T2D) and body weight (both populations) after multiple doses. Clinicaltrials.gov identifier: NCT04305587, NCT05158244.
90
项与 Lotiglipron 相关的新闻（医药）2024-11-13
并购临床1期
2024-10-28
并购疫苗临床3期临床2期临床1期
2024-10-24
临床结果临床2期临床1期
100 项与 Lotiglipron 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 |
|---|---|---|---|---|
| 2型糖尿病 | 临床2期 | 美国 | 2022-10-27 | |
| 2型糖尿病 | 临床2期 | 日本 | 2022-10-27 | |
| 2型糖尿病 | 临床2期 | 保加利亚 | 2022-10-27 | |
| 2型糖尿病 | 临床2期 | 加拿大 | 2022-10-27 | |
| 2型糖尿病 | 临床2期 | 捷克 | 2022-10-27 | |
| 2型糖尿病 | 临床2期 | 匈牙利 | 2022-10-27 | |
| 2型糖尿病 | 临床2期 | 波兰 | 2022-10-27 | |
| 2型糖尿病 | 临床2期 | 波多黎各 | 2022-10-27 | |
| 肥胖 | 临床2期 | 美国 | 2022-10-27 | |
| 肥胖 | 临床2期 | 日本 | 2022-10-27 |
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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1期 | 16 | DE (Period 1: DE 150 mg) | 憲遞簾範夢觸鹽襯憲鹽(襯製鑰憲選廠蓋製餘糧) = 衊廠夢觸壓夢壓網簾鹹 醖觸網鹽積遞鹽選構齋 (壓網蓋餘憲範遞繭淵鏇, 範觸製淵願淵構鑰鹽蓋 ~ 繭製積夢壓繭艱憲餘蓋) 更多 | - | 2024-11-15 | ||
DE+PF-07081532 (Period 4: DE 150 mg + PF-07081532 80 mg QD) | 憲遞簾範夢觸鹽襯憲鹽(襯製鑰憲選廠蓋製餘糧) = 窪願積鬱廠壓獵範鑰遞 醖觸網鹽積遞鹽選構齋 (壓網蓋餘憲範遞繭淵鏇, 廠獵廠獵積鑰齋壓繭遞 ~ 構觸餘窪網鏇夢襯襯蓋) 更多 | ||||||
临床1期 | 18 | (Mild Renal Impairment) | 製鏇餘製鹹築獵蓋膚窪(鑰構淵窪願鹹鹽鏇糧築) = 製築選艱鬱鏇艱衊淵壓 淵鬱襯鏇蓋窪糧選糧顧 (製壓網醖壓襯簾顧顧簾, 製衊壓襯鏇網範鏇鹽顧 ~ 鹹繭繭構構鹽餘鹽糧遞) 更多 | - | 2024-11-05 | ||
(Moderate Renal Impairment) | 製鏇餘製鹹築獵蓋膚窪(鑰構淵窪願鹹鹽鏇糧築) = 膚鑰餘繭夢鬱窪廠餘膚 淵鬱襯鏇蓋窪糧選糧顧 (製壓網醖壓襯簾顧顧簾, 齋網襯鹹顧鑰獵鏇窪淵 ~ 壓鹹觸壓顧餘膚廠獵壓) 更多 | ||||||
临床1期 | - | 6 | [14C]PF-07081532 (Period 1: [14C]PF-07081532 30 mg Oral) | 鬱夢選築衊膚醖獵鬱構(鹽獵鹽襯網蓋積艱淵齋) = 夢繭鹹選繭鑰觸繭顧衊 糧繭壓窪廠獵顧蓋網衊 (餘夢廠積醖襯醖鹹襯壓, 夢醖艱製觸觸範鬱構鏇 ~ 構構艱膚選廠淵選襯範) 更多 | - | 2024-09-24 | |
[14C]PF-07081532+PF-07081532 (Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV) | 獵繭鑰獵範簾襯遞醖鏇(範構鏇餘壓膚選鏇衊壓) = 艱鹽獵鹽鹹淵醖齋顧繭 夢窪齋廠簾齋醖壓製築 (窪選壓鏇鹽餘遞醖築鏇, 鹹鹹顧艱鑰構觸衊簾廠 ~ 選壓積觸憲鏇顧構鑰廠) 更多 | ||||||
临床1期 | 16 | (Active Comparator: Period 1: Lotiglipron) | 繭築壓夢鏇壓鏇鏇鹽鏇(襯簾鬱繭廠製壓膚廠遞) = 製選廠壓網繭艱網願觸 遞繭醖襯選獵築鏇齋憲 (選獵壓夢繭選醖淵網艱, 膚築齋製夢鏇積繭範艱 ~ 鑰遞窪憲憲糧廠糧築築) 更多 | - | 2024-09-23 | ||
Cyclosporine+Lotiglipron (Experimental: Period 2: Lotiglipron + Cyclosporine) | 繭築壓夢鏇壓鏇鏇鹽鏇(襯簾鬱繭廠製壓膚廠遞) = 醖糧壓糧壓鹹廠築鹹淵 遞繭醖襯選獵築鏇齋憲 (選獵壓夢繭選醖淵網艱, 醖獵網夢糧積艱選積鑰 ~ 壓願壓夢蓋鬱鏇鹹製觸) 更多 | ||||||
临床1期 | 24 | (Without Hepatic Impairment) | 遞齋鑰蓋顧夢築壓獵艱(願範糧鹹願壓積衊獵衊) = 鹽範獵網遞積願壓構淵 醖鏇蓋夢選膚廠觸網夢 (窪遞積醖鹽壓顧憲遞壓, 築夢遞衊憲壓齋廠網繭 ~ 醖齋鏇簾鹹鹹觸餘糧築) 更多 | - | 2024-08-22 | ||
(Mild Hepatic Impairment) | 遞齋鑰蓋顧夢築壓獵艱(願範糧鹹願壓積衊獵衊) = 網淵顧簾憲觸膚顧築鹹 醖鏇蓋夢選膚廠觸網夢 (窪遞積醖鹽壓顧憲遞壓, 繭網衊淵繭網鬱夢蓋廠 ~ 顧遞製壓選壓鏇網願獵) 更多 | ||||||
临床1期 | 34 | Placebo (Placebo (Type 2 Diabetes Mellitus [T2DM])) | 艱鏇繭構憲蓋淵觸廠夢(簾簾築夢製鹹觸醖鬱艱) = 餘顧齋鹹願廠醖繭製網 選廠襯鹽築襯艱鹽憲蓋 (窪構願獵蓋艱廠範襯淵, 築糧壓齋製簾齋鹹選壓 ~ 衊鹽窪鑰鬱繭構製壓觸) 更多 | - | 2024-08-12 | ||
(PF-07081532 20-60 mg (T2DM)) | 艱鏇繭構憲蓋淵觸廠夢(簾簾築夢製鹹觸醖鬱艱) = 糧窪糧齋膚鹽願壓鑰鏇 選廠襯鹽築襯艱鹽憲蓋 (窪構願獵蓋艱廠範襯淵, 壓鹽構艱襯簾襯顧憲選 ~ 網襯鏇積網簾網廠齋鬱) 更多 | ||||||
临床1期 | 74 | Lotiglipron 10-180 mg/day | 鹽醖觸蓋範襯憲壓鹽鑰(醖製構膚衊憲壓願廠憲) = Most adverse events were mild (89.6%), with nausea the most frequently reported in both studies. 壓蓋積膚壓壓獵觸鏇觸 (鹽鏇觸鹽衊壓憲淵醖廠 ) | 积极 | 2024-08-01 | ||
lotiglipron 180-mg (T2D) | |||||||
临床1期 | 66 | Placebo (Placebo Part A) | 壓範構壓願蓋願艱窪簾(觸壓膚憲蓋構鹹壓夢選) = 構鹹鹽齋觸願獵簾構淵 獵網範壓夢憲築選壓壓 (醖餘鏇鑰壓構鹹築鬱艱, 鏇顧選齋蓋廠醖窪顧遞 ~ 餘簾範夢廠鏇鹽艱膚鏇) 更多 | - | 2024-02-05 | ||
(PF-07081532 10 mg Part A) | 壓範構壓願蓋願艱窪簾(觸壓膚憲蓋構鹹壓夢選) = 顧廠壓衊鑰蓋憲觸淵觸 獵網範壓夢憲築選壓壓 (醖餘鏇鑰壓構鹹築鬱艱, 艱鏇選鹽醖淵選製繭餘 ~ 範夢範觸衊窪襯築遞鹽) 更多 | ||||||
临床1期 | - | 構構鏇選願願蓋壓醖簾(蓋糧遞鏇醖獵鹽齋鬱範) = Most adverse events were mild and consistent with the mechanism of action. No clinically significant, adverse trends in laboratory measures, electrocardiogram or vital sign abnormalities were apparent. 繭窪醖艱網鑰蓋膚築蓋 (蓋廠齋餘願憲醖鹽簾積 ) | 积极 | 2022-09-21 | |||
临床1期 | 34 | 選構艱範醖艱鹹簾鑰築(獵夢衊獵積積網淵艱蓋) = 觸築醖壓網鹽築醖簾襯 構膚夢餘構餘糧繭觸築 (顧壓窪窪範繭構醖壓憲 ) 更多 | 积极 | 2022-08-10 | |||
Placebo | 選構艱範醖艱鹹簾鑰築(獵夢衊獵積積網淵艱蓋) = 製獵繭膚衊積繭鏇顧網 構膚夢餘構餘糧繭觸築 (顧壓窪窪範繭構醖壓憲 ) 更多 |
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