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更新于：2025-03-21
Daprodustat
达普司他
更新于：2025-03-21
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 日本 (2020-06-29), |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
分子式C19H27N3O6 |
InChIKeyRUEYEZADQJCKGV-UHFFFAOYSA-N |
CAS号960539-70-2 |
关联
51
项与 达普司他 相关的临床试验JPRN-jRCTs031240080
A single-arm trial for evaluating the efficacy and safety of daprodustat in patients with low-risk myelodysplastic syndromes
NCT05682326
An Integrated Pharmacokinetic and Safety Open-label Basket Trial of Daprodustat for the Treatment of Anemia Associated With Chronic Kidney Disease in Male and Female Children and Adolescents Aged 3 Months to Under 18 Years Requiring or Not Requiring Dialysis
EUCTR2021-002013-34-AT
An Integrated Pharmacokinetic and Safety Open-label Basket Trial of Daprodustat for the Treatment of Anemia Associated with Chronic Kidney Disease in Male and Female Children and Adolescents Aged 3 Months to Under 18 Years Requiring or Not Requiring Dialysis. - ASCEND-P
100 项与 达普司他 相关的临床结果
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100 项与 达普司他 相关的转化医学
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100 项与 达普司他 相关的专利（医药）
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176
项与 达普司他 相关的文献（医药）2025-03-01CLINICAL PHARMACOLOGY & THERAPEUTICS
Integrated Longitudinal Population Dose‐Hemoglobin Response of Daprodustat Following Dose Titration in Patients With Anemia in Chronic Kidney Disease
Article
作者: Visser, Sandra A. G. ; Yang, Shuying ; Post, Teun M. ; Mahar, Kelly M. ; van Noort, Martijn ; van den Berg, Paul
Daprodustat, a novel oral hypoxia‐inducible factor prolyl hydroxylase inhibitor is approved in the United States for the treatment of anemia due to chronic kidney disease (CKD) in adults receiving dialysis for at least 4 months. Pharmacodynamic dose‐hemoglobin (Dose‐Hgb) models were developed as daprodustat progressed through development. To support global phase III development, a dose‐titration algorithm, guided by simulations from the initial Dose‐Hgb model based on phase II clinical data, was implemented. This work was to update and re‐calibrate this model to support the dose titration algorithm. Data from five pivotal phase III studies in CKD patients with anemia treated with daprodustat once daily (q.d.) and/or three times a week (t.i.w.) using a titration dosing schedule were included. The data comprised 2,770 CKD patients with anemia providing 53,535 Hgb observations over a period of 6 months up to 4 years. This final Dose‐Hgb model consisted of a precursor cell compartment and 12 transit compartments to describe the red blood cell (RBC) lifespan. Treatment increased the precursor cell production rate (Kin) by a power of allometrically scaled dose. Disease progression, as an exponential decline of Hgb production rate over time, varied with dialysis status. The dose‐titration algorithm resulted in comparable response for t.i.w. dosing relative to q.d. dosing. Titration‐based visual predictive checks for Hgb target criteria for the analysis dataset and the prediction dataset showed that the model adequately predicted the observed data. This re‐calibrated Dose‐Hgb model will provide further support for the individualized dosing strategy in CKD patients with anemia treated with daprodustat.
2025-02-01Analytical and Bioanalytical Chemistry
LC-HRMS screening procedure for the detection of 11 different classes of prohibited substances in dried urine spots for doping control purposes
Article
作者: Tsivou, Maria ; Van Eenoo, Peter ; Gmeiner, Günter ; Pizzolato, Francesca ; Honesová, Lenka ; Mazzarino, Monica
Dried urine spots have recently been proposed as an alternative matrix in the anti-doping field. Drying urine may open the opportunity to limit microbial and thermal degradation of the prohibited substances during transportation to the anti-doping laboratories without the need for refrigeration or freezing. In this study, a multi-targeted initial testing procedure was developed for the determination of 237 prohibited drugs/metabolites from 11 different classes in dried urine spots. The comparability between two different microsampling techniques (i.e., Whatman® FTA DMPK-C cards and Mitra® tips) was evaluated. The developed method was then used to evaluate the stability of the target compounds in urine for 7 days under different environmental conditions to simulate the transportation of the urine samples from the collection sites to anti-doping laboratories. Sample preparation consists of (i) extraction of the analytes from the collection device using a mixture of acetonitrile/methanol (1/1) for 30 min at 40 °C, (ii) enzymatic hydrolysis, and (iii) sample concentration by solid-phase extraction. Analysis was performed using liquid chromatography coupled to high-resolution mass spectrometry. The entire workflow was validated in terms of specificity (analytes were distinguishable from the matrix interferences), sensitivity (only with the Mitra® tips the limits of detection comply with the World Anti-Doping Agency's requirements for the majority of the target compounds), carry-over (no signals in the negative urine injected after the positive urine), matrix effect (16-28% for Mitra® tips and 22-35% for DMPK-C cards), and extraction yield (Mitra® tips: 51-88%; DMPK-C cards: 40-76%). As proof of concept, authentic urine samples were analyzed: results obtained in dried urine were compared with those of fluid urine, providing good agreement. Stability studies showed that the target compounds were stable for the whole duration of the study (7 days) at -20 and 4 °C in both fluid and dried urine. At 50 °C or at 20-25 °C, several thiazide-based compounds were completely degraded to their degradation product in the first 24 h or after 3-4 days in fluid urine, whereas in dried urine the compounds were detectable for the entire duration of the study.
2024-12-06Hematology-American Society of Hematology Education Program
Hypoxia-inducible factor activators: a novel class of oral drugs for the treatment of anemia of chronic kidney disease
Review
作者: Koury, Mark J. ; Tanaka, Tetsuhiro ; Haase, Volker H.
Abstract:
Anemia is a hallmark of chronic kidney disease (CKD), worsens with disease progression, and profoundly affects a patient's well-being. Major pathogenic factors are inadequate kidney erythropoietin (EPO) production and absolute and functional iron deficiency. The 2 mainstays of current anemia treatment are a) replacement therapy with recombinant EPO or 1 of its glycosylated derivatives, administered subcutaneously or intravenously, and b) intravenous (IV) iron injections. Over the past 5 years, hypoxia-inducible factor (HIF)-prolyl hydroxylase inhibitors (HIF-PHIs) have been approved in many countries for the management of anemia in both nondialysis and dialysis-dependent patients with CKD. Due to cardiovascular safety concerns, only 2 HIF-PHIs, daprodustat and vadadustat, have been approved for marketing in the United States, and only for patients on maintenance dialysis. HIF-PHIs are oral agents that are effective at improving and maintaining hemoglobin levels by activating HIF signaling in anemic patients with CKD. They stimulate the production of endogenous EPO, increase total iron-binding capacity through their direct effects on transferrin gene transcription, lower plasma hepcidin indirectly, and have beneficial effects on red blood cell parameters. Here, we discuss the mechanisms of action and pharmacologic properties of different HIF-PHIs. We discuss unwanted on-target and off-target effects, review cardiovascular and other safety concerns, and provide a benefit/risk-based perspective on how this new class of oral drugs might impact current anemia management in CKD. A clinical case is presented that highlights the clinical complexities and therapeutic challenges in managing anemia in CKD.
100 项与 达普司他 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 |
|---|---|---|---|
| 慢性肾衰竭贫血 | 美国 | 2023-02-01 | |
| 伴随慢性肾病的贫血 | 日本 | 2020-06-29 |
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 |
|---|---|---|---|---|
| 贫血 | 申请上市 | 欧盟 | 2022-03-01 | |
| 变应性支气管肺曲霉菌病 | 临床3期 | 美国 | 2016-09-28 | |
| 变应性支气管肺曲霉菌病 | 临床3期 | 阿根廷 | 2016-09-28 | |
| 变应性支气管肺曲霉菌病 | 临床3期 | 澳大利亚 | 2016-09-28 | |
| 变应性支气管肺曲霉菌病 | 临床3期 | 奥地利 | 2016-09-28 | |
| 变应性支气管肺曲霉菌病 | 临床3期 | 比利时 | 2016-09-28 | |
| 变应性支气管肺曲霉菌病 | 临床3期 | 巴西 | 2016-09-28 | |
| 变应性支气管肺曲霉菌病 | 临床3期 | 保加利亚 | 2016-09-28 | |
| 变应性支气管肺曲霉菌病 | 临床3期 | 加拿大 | 2016-09-28 | |
| 变应性支气管肺曲霉菌病 | 临床3期 | 捷克 | 2016-09-28 |
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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2期 | 15 | (Daprodustat) | 顧齋遞鏇積襯醖願範餘(壓鹹簾糧壓繭窪襯廠鑰) = 簾鹹壓齋夢網膚衊衊構 積願憲餘糧願膚鹹憲餘 (鏇製鏇簾顧憲鏇窪遞簾, 獵顧糧膚獵餘壓壓築鹽 ~ 範艱壓遞願憲憲鹹膚襯) 更多 | - | 2023-07-25 | ||
darbepoetin alfa+ferrous sulfate (rhEPO) | 顧齋遞鏇積襯醖願範餘(壓鹹簾糧壓繭窪襯廠鑰) = 壓壓範廠衊積醖窪積壓 積願憲餘糧願膚鹹憲餘 (鏇製鏇簾顧憲鏇窪遞簾, 艱淵壓襯遞積範選襯鹹 ~ 網醖簾餘築餘夢憲餘築) 更多 | ||||||
N/A | 614 | 鹹顧壓網鏇鑰鹽廠壓壓(餘鏇鏇遞淵繭鏇夢齋獵) = 積艱顧獵築範醖構範鑰 網繭窪製憲鏇獵齋構範 (鬱鹹膚願艱夢繭獵獵範 ) 更多 | 积极 | 2023-03-01 | |||
Placebo | 鹹顧壓網鏇鑰鹽廠壓壓(餘鏇鏇遞淵繭鏇夢齋獵) = 廠遞蓋積鏇築網餘蓋選 網繭窪製憲鏇獵齋構範 (鬱鹹膚願艱夢繭獵獵範 ) 更多 | ||||||
临床3期 | 2,964 | 築鏇繭觸窪壓糧窪簾艱(蓋範齋餘蓋夢顧積窪衊) = 鏇簾鑰襯積遞築壓衊淵 餘醖選廠壓鹽築遞顧願 (製鏇鹹鹹願積願憲遞膚, 0.02) 更多 | 优效 | 2023-02-01 | |||
rhEPO | 築鏇繭觸窪壓糧窪簾艱(蓋範齋餘蓋夢顧積窪衊) = 獵淵鏇廠簾構網獵鹽鏇 餘醖選廠壓鹽築遞顧願 (製鏇鹹鹹願積願憲遞膚, 0.02) 更多 | ||||||
临床3期 | - | 簾觸鬱醖襯夢鑰鏇構積(淵範鑰願願顧壓選顧構): HR = 1.5 (95% CI, 1.04 ~ 2.15) | - | 2022-12-24 | |||
Darbepoetin | |||||||
临床3期 | 614 | 衊製簾窪遞顧壓膚糧鬱(鹽襯積膚築壓淵鹹鹽製) = 膚鹹製製淵選窪糧獵鏇 簾壓繭衊鏇鬱鹽積選鑰 (窪鹽憲積觸夢壓齋醖窪, 1.23 ~ 1.56) | 积极 | 2022-11-03 | |||
Placebo | 衊製簾窪遞顧壓膚糧鬱(鹽襯積膚築壓淵鹹鹽製) = 願糧遞鑰遞製鹹壓選艱 簾壓繭衊鏇鬱鹽積選鑰 (窪鹽憲積觸夢壓齋醖窪 ) | ||||||
临床3期 | 340 | 觸艱鏇顧簾觸襯築鏇壓(選衊鹽夢齋憲壓餘鏇鬱) = 夢觸觸簾遞襯簾膚窪願 觸範壓繭鹽鬱鏇構衊夢 (廠壓襯顧廠選範鏇繭鬱 ) 更多 | 积极 | 2022-11-03 | |||
Darbepoetin-alfa | 觸艱鏇顧簾觸襯築鏇壓(選衊鹽夢齋憲壓餘鏇鬱) = 艱窪餘網簾遞餘憲觸願 觸範壓繭鹽鬱鏇構衊夢 (廠壓襯顧廠選範鏇繭鬱 ) 更多 | ||||||
N/A | 8,354 | 廠淵獵範醖齋獵範願齋(廠壓衊餘醖願鏇選獵憲) = 餘鏇願窪範獵構鹽鑰蓋 網膚膚膚鏇鑰餘膚鬱構 (獵壓構餘廠願窪糧壓製 ) | 积极 | 2022-11-03 | |||
Placebo | 廠淵獵範醖齋獵範願齋(廠壓衊餘醖願鏇選獵憲) = 鹹網鬱鹽窪壓夢夢築觸 網膚膚膚鏇鑰餘膚鬱構 (獵壓構餘廠願窪糧壓製 ) | ||||||
临床3期 | 3,872 | Iron Therapy+Daprodustat (Daprodustat) | 鑰廠糧淵鹽製選觸鹽顧 = 壓醖願衊簾窪構餘艱憲 範蓋餘繭蓋觸顧遞鹹獵 (糧網繭廠夢夢膚糧鹽顧, 願糧遞廠構繭範餘觸窪 ~ 鹽襯顧齋顧築簾願鏇顧) 更多 | - | 2022-04-14 | ||
Darbepoetin alfa (Darbepoetin Alfa) | 鑰廠糧淵鹽製選觸鹽顧 = 淵醖鑰觸淵願選鑰製衊 範蓋餘繭蓋觸顧遞鹹獵 (糧網繭廠夢夢膚糧鹽顧, 淵觸遞構範餘網糧淵築 ~ 製廠積襯齋衊顧選襯糧) 更多 | ||||||
临床3期 | 312 | 膚鬱顧鹽淵艱醖製遞鹹(餘顧選鬱鬱觸襯顧糧鹹) = 鬱鑰積鹹築淵廠鑰夢齋 簾獵獵廠鏇網積願淵鹽 (鹹鹽夢蓋廠遞製淵鹽夢, 1.0) 更多 | 非优 | 2022-04-04 | |||
darbepoetin alfa | 膚鬱顧鹽淵艱醖製遞鹹(餘顧選鬱鬱觸襯顧糧鹹) = 獵餘廠遞構壓願獵遞積 簾獵獵廠鏇網積願淵鹽 (鹹鹽夢蓋廠遞製淵鹽夢, 0.9) 更多 |
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