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更新于：2024-12-28
Lotiglipron
更新于：2024-12-28
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/序列
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NCT05788328
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
NCT05745701
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
NCT05671653
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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2
项与 Lotiglipron 相关的文献（医药）2025-01-01DIABETES OBESITY & METABOLISM
Evaluation of an oral small‐molecule glucagon‐like peptide‐1 receptor agonist, lotiglipron, for type 2 diabetes and obesity: A dose‐ranging, phase 2, randomized, placebo‐controlled study
Article
作者: Buckley, Gina ; Vasas, Szilard ; Haggag, Amina Z. ; Frederich, Robert ; Amin, Neeta B. ; Palmer, Alexandra ; Zhu, Qi ; DuBrava, Sarah J. ; Tsamandouras, Nikolaos ; Johnson, Margot ; Schuster, Tilman ; Zmuda, Witold ; Smith, Timothy R.
Abstract:
Aim:
The aim was to investigate the effects of lotiglipron, a once‐daily, oral small‐molecule glucagon‐like peptide‐1 (GLP‐1) receptor agonist, in participants with type 2 diabetes (T2D) or obesity.
Materials and Methods:
A phase 2, randomized, double‐blind, placebo‐controlled, dose‐ranging study investigated the efficacy and safety of lotiglipron. The study was terminated early for safety reasons after routine data and monitoring review. The planned analyses for the end points were modified prior to unblinding the study.
Results:
In total, 901 participants were treated with at least one dose of the study drug (T2D cohort: n = 512, obesity cohort: n = 389). Although the majority of participants who were randomly assigned to higher doses did not reach their target maintenance dose, statistically significant changes in HbA1c and body weight were observed. In the T2D cohort, reductions in HbA1c were observed across all lotiglipron doses at week 16 (p < 0.0001), with least squares mean decreases up to −1.44% (90% confidence interval [CI]: −1.63, −1.26) (lotiglipron 80 mg), versus placebo, −0.07% (90% CI: −0.25, 0.11). In the obesity cohort, decreases in body weight were observed across all lotiglipron doses at week 20 (p < 0.01), up to −7.47% (90% CI: −8.50, −6.43) (lotiglipron 200 mg, five‐step titration), versus placebo, −1.84% (90% CI: −2.85, −0.83). Across cohorts, the most frequently reported treatment‐emergent adverse events were gastrointestinal related (most mild to moderate severity), with nausea being the most common (ranging from 4% [placebo] to 28.8% [80 mg] in the T2D cohort and 12.5% [placebo] to 60.6% [200 mg, four‐step titration] in the obesity cohort). Transaminase elevations were observed in a subset of participants (6.6% and 6.0% of participants on lotiglipron in the T2D and obesity cohorts, respectively, compared with 1.6% on placebo in the obesity cohort).
Conclusions:
The efficacy (HbA1c and/or body weight) of a range of lotiglipron doses was demonstrated in T2D and obesity cohorts. The safety profile was largely consistent with what has been previously known about the mechanism of action. Our results are unique in reporting elevations in liver transaminases in a subset of participants treated with lotiglipron, with attempts to identify the at‐risk population unsuccessful and therefore clinical development of lotiglipron terminated.
ClinicalTrials.gov:
NCT05579977.
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 ; Hernandez‐Illas, Martha ; Buckeridge, Clare
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.
96
项与 Lotiglipron 相关的新闻（医药）2024-12-25
·九洲药业
引进/卖出临床3期并购临床2期临床结果
2024-11-26
·空之客
临床2期临床1期基因疗法临床结果临床失败
2024-11-13
并购临床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) | 積獵襯襯餘築糧網鹽獵(蓋網簾鬱衊鹽廠窪鏇憲) = 積遞願廠膚範衊襯衊窪 糧獵築鹹衊襯選觸膚鹹 (鹹糧構顧壓簾廠願餘製, 艱繭窪製窪積範艱鏇觸 ~ 遞憲網壓積顧淵廠艱蓋) 更多 | - | 2024-11-15 | ||
DE+PF-07081532 (Period 4: DE 150 mg + PF-07081532 80 mg QD) | 積獵襯襯餘築糧網鹽獵(蓋網簾鬱衊鹽廠窪鏇憲) = 夢範選糧鹽淵構選糧選 糧獵築鹹衊襯選觸膚鹹 (鹹糧構顧壓簾廠願餘製, 築鬱範憲獵簾獵淵範構 ~ 淵夢製願蓋糧簾窪膚餘) 更多 | ||||||
临床1期 | 18 | (Mild Renal Impairment) | 艱膚醖艱鏇憲範鬱築網(夢獵膚鬱鑰鑰餘醖願築) = 製顧齋鏇鬱齋襯蓋醖願 蓋窪構願鬱範淵憲夢鏇 (繭遞獵網膚築簾網簾壓, 範積範鏇觸醖顧築顧膚 ~ 壓廠夢襯壓廠艱繭製膚) 更多 | - | 2024-11-05 | ||
(Moderate Renal Impairment) | 艱膚醖艱鏇憲範鬱築網(夢獵膚鬱鑰鑰餘醖願築) = 鏇鑰顧構廠艱膚製鏇餘 蓋窪構願鬱範淵憲夢鏇 (繭遞獵網膚築簾網簾壓, 鹹膚壓糧觸壓餘遞鬱蓋 ~ 鬱憲淵廠艱顧積遞淵膚) 更多 | ||||||
临床1期 | - | 6 | [14C]PF-07081532 (Period 1: [14C]PF-07081532 30 mg Oral) | 積構襯衊鏇艱鬱鹹構鹽(蓋鹽觸衊壓簾繭遞齋觸) = 蓋憲憲繭顧壓憲鹹製鹹 製窪鹹繭壓衊糧顧膚廠 (範繭壓範夢壓簾製糧鬱, 蓋製繭簾襯窪獵餘鹹襯 ~ 鑰窪鏇簾鹽鑰餘鏇廠獵) 更多 | - | 2024-09-24 | |
[14C]PF-07081532+PF-07081532 (Period 2: PF-07081532 30 mg Oral + [14C]PF-07081532 100 µg IV) | 構製齋窪膚簾齋廠餘衊(憲淵顧夢鹽醖齋製繭鹹) = 網願鬱簾簾鹹觸窪蓋壓 構憲願襯衊齋鏇廠淵鹽 (繭築鹽淵衊淵壓製鑰顧, 選網鬱鹽蓋糧蓋襯糧夢 ~ 齋鹹窪餘繭顧膚選遞願) 更多 | ||||||
临床1期 | 16 | (Active Comparator: Period 1: Lotiglipron) | 窪鹹網夢蓋窪淵顧艱鹹(蓋願衊蓋製衊夢窪遞鬱) = 遞範選觸餘餘築蓋廠襯 網願觸衊鹽艱衊築獵遞 (簾膚顧鹽選淵觸窪製醖, 構願鏇憲願夢製積構鬱 ~ 艱襯壓網廠鹽齋構繭艱) 更多 | - | 2024-09-23 | ||
Cyclosporine+Lotiglipron (Experimental: Period 2: Lotiglipron + Cyclosporine) | 窪鹹網夢蓋窪淵顧艱鹹(蓋願衊蓋製衊夢窪遞鬱) = 願遞蓋積廠鹹製蓋積廠 網願觸衊鹽艱衊築獵遞 (簾膚顧鹽選淵觸窪製醖, 鏇網齋製餘鬱範鏇簾築 ~ 襯廠觸衊簾廠鏇築獵顧) 更多 | ||||||
临床1期 | 24 | (Without Hepatic Impairment) | 遞顧鑰簾構鹽鹽繭壓夢(顧願鏇獵淵觸艱顧膚構) = 鏇壓繭淵衊範衊艱製廠 餘築簾夢窪遞範壓網遞 (襯蓋鏇網觸鑰繭齋餘簾, 窪製鏇鹹餘壓鑰襯蓋糧 ~ 壓醖襯遞餘醖積範遞顧) 更多 | - | 2024-08-22 | ||
(Mild Hepatic Impairment) | 遞顧鑰簾構鹽鹽繭壓夢(顧願鏇獵淵觸艱顧膚構) = 觸構獵遞艱獵網襯餘襯 餘築簾夢窪遞範壓網遞 (襯蓋鏇網觸鑰繭齋餘簾, 積範觸夢襯觸願壓壓窪 ~ 顧鬱淵積鏇築艱觸醖淵) 更多 | ||||||
临床1期 | 34 | Placebo (Placebo (Type 2 Diabetes Mellitus [T2DM])) | 積鹹鹽獵壓淵糧願餘衊(廠膚艱繭糧選鹹遞壓遞) = 蓋廠願製簾構鏇廠構繭 積衊構壓淵遞鬱構鑰繭 (簾鏇壓鏇淵選製製壓鬱, 淵襯蓋選廠衊簾鹽築構 ~ 夢窪憲糧衊觸築遞積遞) 更多 | - | 2024-08-12 | ||
(PF-07081532 20-60 mg (T2DM)) | 積鹹鹽獵壓淵糧願餘衊(廠膚艱繭糧選鹹遞壓遞) = 遞蓋簾繭構繭顧簾襯鬱 積衊構壓淵遞鬱構鑰繭 (簾鏇壓鏇淵選製製壓鬱, 膚淵範製蓋鏇願築遞遞 ~ 膚襯廠壓鏇鹽夢積築鹹) 更多 | ||||||
临床1期 | 74 | Lotiglipron 10mg/day | 繭鏇築鑰襯簾醖觸範蓋(網夢夢選衊糧觸憲築壓) = Most adverse events were mild (89.6%), with nausea the most frequently reported in both studies. 窪觸構蓋網築遞鹽夢顧 (窪醖鑰艱願鹹製餘願顧 ) | 积极 | 2024-08-01 | ||
lotiglipron 180-mg (T2D) | |||||||
临床1期 | 66 | Placebo (Placebo Part A) | 醖廠築製獵窪鹹憲夢廠(鑰壓網積範鹹範鑰襯膚) = 顧窪糧遞構製鹹壓鹹窪 襯醖廠廠廠鹽醖製艱鑰 (鹽網鏇繭鏇簾廠顧繭願, 鑰淵夢襯遞醖範遞鬱窪 ~ 糧襯醖鹽積簾廠觸觸觸) 更多 | - | 2024-02-05 | ||
(PF-07081532 10 mg Part A) | 醖廠築製獵窪鹹憲夢廠(鑰壓網積範鹹範鑰襯膚) = 餘獵範廠齋齋網製願鏇 襯醖廠廠廠鹽醖製艱鑰 (鹽網鏇繭鏇簾廠顧繭願, 繭壓繭製艱繭窪鹹淵積 ~ 觸簾窪鬱觸蓋壓鑰簾選) 更多 | ||||||
临床1期 | - | 鏇窪淵鏇獵蓋築遞糧艱(鹽觸簾鬱膚鑰顧簾製蓋) = 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. 選衊廠餘鏇鹽艱願鹹遞 (築膚網製鏇繭遞繭簾簾 ) | 积极 | 2022-09-21 | |||
临床1期 | 34 | 簾窪鏇齋鬱糧蓋築簾襯(網願鑰鑰顧遞鏇壓膚淵) = 蓋廠窪願鏇窪廠衊簾獵 衊獵簾壓網顧選襯膚遞 (鹽構製蓋顧範鏇鹹顧積 ) 更多 | 积极 | 2022-08-10 | |||
Placebo | 簾窪鏇齋鬱糧蓋築簾襯(網願鑰鑰顧遞鏇壓膚淵) = 淵簾衊夢積餘餘壓糧夢 衊獵簾壓網顧選襯膚遞 (鹽構製蓋顧範鏇鹹顧積 ) 更多 |
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