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更新于：2025-01-28
Roxadustat
罗沙司他
更新于：2025-01-28
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 中国 (2018-12-17), |
最高研发阶段(中国)批准上市 |
特殊审评特殊审批 (中国) |
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结构/序列
分子式C19H16N2O5 |
InChIKeyYOZBGTLTNGAVFU-UHFFFAOYSA-N |
CAS号808118-40-3 |
关联
143
项与 罗沙司他 相关的临床试验NCT05810311
The Effect of Roxadustat on the Levels of Renal Oxygenation in Patients With Diabetes Nephropathy (FOXTROT)
NCT06772272
Effect of Perioperative Roxadustat in Elective Lumbar Interbody Fusion Surgery: a Parallel-group, Open-label, Randomised Controlled Trial.
CTR20243819
罗沙司他片在健康受试者中单中心、随机、开放、两制剂、单次给药、两周期、双交叉生物等效性试验
100 项与 罗沙司他 相关的临床结果
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100 项与 罗沙司他 相关的转化医学
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100 项与 罗沙司他 相关的专利（医药）
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662
项与 罗沙司他 相关的文献（医药）2025-01-10JOURNAL OF CLINICAL ONCOLOGY
Efficacy and Safety of Roxadustat for Anemia in Patients Receiving Chemotherapy for Nonmyeloid Malignancies: A Randomized, Open-Label, Active-Controlled Phase III Study
Article
作者: Wu, Jiong ; Liu, Yu ; Lee, Tyson ; Eisner, Mark D. ; Zhang, Hua ; Lu, Shun ; Ma, Rui ; Lu, Yan ; Qian, Ling ; Jiang, Jin ; Xie, Yanyan ; Fu, Ting ; Dai, Xiumei ; Yu, Yan ; Guo, Qisen
PURPOSE:
We evaluated the efficacy and safety of roxadustat, a first-in-class hypoxia-inducible factor prolyl hydroxylase inhibitor, for chemotherapy-induced anemia (CIA) in patients with nonmyeloid malignancies receiving multicycle treatments of chemotherapy.
PATIENTS AND METHODS:
In this open-label, noninferiority phase III study conducted at 44 sites in China, 159 participants age ≥18 years with CIA nonmyeloid malignancy and CIA were randomly assigned (1:1) to oral roxadustat or subcutaneous recombinant human erythropoietin-α (rHuEPO-α) three times a week for 12 weeks. Roxadustat starting dosages were 100, 120, and 150 mg three times a week for participants weighing 40-<50, 50-60, and >60 kg, respectively. rHuEPO-α starting dosage for all participants was 150 IU/kg three times a week. Both roxadustat and rHuEPO-α dosages could be modified. The primary end point was least-squares mean (LSM) change in hemoglobin (Hb) concentration from baseline to the concentration averaged over weeks 9-13.
RESULTS:
Of the 159 participants randomly assigned, 140 were included in the per-protocol set (roxadustat, n = 78; rHuEPO-α, n = 62). The LSM (95% two-sided CI) change from baseline to weeks 9-13 in Hb concentration was 17.1 (13.58 to 20.71) g/L with roxadustat and 15.4 (11.34 to 19.50) g/L with rHuEPO-α (mean difference [95% CI], 1.7 [–3.39 to 6.84]). The lower bound of the one-sided 97.5% CI for the treatment difference (‒3.4 g/L) was greater than the predefined noninferiority margin of ‒6.6 g/L, establishing noninferiority. Noninferiority was supported by five of six key secondary end points. Rates of adverse events were generally comparable between treatments and consistent with previous findings.
CONCLUSION:
Roxadustat was noninferior to rHuEPO-α in treating CIA in participants with nonmyeloid malignancies receiving multicycle treatments of myelosuppressive chemotherapy. The oral formulation of roxadustat may potentially increase compliance.
2025-01-08CURRENT TOPICS IN MEDICINAL CHEMISTRY
Bioanalysis, Analysis, Chemistry, and Pharmacological Aspects of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors
Article
作者: Sharma, Sanjay ; Patil, Roshani ; Jain, Sunidhi
Abstract::
The development of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIFPHIs),
such as Roxadustat (ROX), Enarodustat (ENA), Desidustat (DES), Vadadustat (VAD), Molidustat
(MOL), and Daprodustat (DAP), has significant effects on anemia in chronic kidney disease.
This review presents comprehensive information about the synthesis, pharmacology, and
analysis of HIF-PHIs across several matrices. The literature has presented several approaches for
quantifying HIF-PHIs in diverse sample matrices. Furthermore, HIF-PHIs exhibit similar modes of
action, demonstrating distinct pharmacokinetic parameters. The pharmacological insights encompass
their half-life, mechanism of action, absorption, distribution, metabolism, excretion, and therapeutic
uses. Research indicates that most studies concentrate on hyphenated methodologies for
drug estimation in various biological fluids. Consequently, this study assesses the biological efficacy
of HIF-PHIs and elucidates the analytical methodologies currently employed for measurement
across various matrices.
2025-01-01JOURNAL OF THROMBOSIS AND HAEMOSTASIS
Therapeutic potential of roxadustat in immune thrombocytopenia: A Mendelian randomization analysis
Article
作者: Lin, Zheyan ; Wu, Runhui ; Meng, Jinxi ; Hu, Yu ; Dong, Shuyue ; Chen, Zhenping ; Ma, Jingyao ; Cheng, Xiaoling ; Wang, Zhifa ; Ouyang, Juntao
BACKGROUND:
Immune thrombocytopenia (ITP) is characterized by immune-mediated platelet destruction and impaired megakaryocyte maturation. Hypoxia-inducible factor-1 alpha (HIF-1α), pivotal in the development of megakaryocytes and immune regulation, is downregulated in ITP. Roxadustat, which stabilizes HIF-1α, has emerged as a potential therapeutic drug for ITP that acts by enhancing HIF-1α-mediated megakaryocyte development and modulating immune responses.
OBJECTIVES:
This study evaluates the safety profile of roxadustat and its therapeutic efficacy for ITP treatment using Mendelian randomization (MR) analysis.
METHODS:
We used expression Quantitative Trait Loci (eQTLs) data for roxadustat's target genes (EGLN1, EGLN2, EGLN3) and genetic associations with ITP, and adverse outcomes from the Open Genome-Wide Association Study (OpenGWAS) project. MR analysis included IVW, MR-Egger regression, weighted median, and MR pleiotropy residual sum and outlier (MR-PRESSO) methods to evaluate pleiotropy. Heterogeneity was assessed using Cochran's Q statistic and I2 measure, with sensitivity analyses. A meta-analysis was performed to integrate effect sizes from multiple literature sources.
RESULTS:
MR analysis revealed a significant association between roxadustat and reduced ITP risk (odds ratio [OR] 0.79, 95% confidence interval [CI] 0.66-0.95, P=0.01) with no evidence of horizontal pleiotropy. Meta-analysis confirmed the protective effect of roxadustat on ITP. Utilizing eQTLs of roxadustat's target gene EGLN1 as instrumental variables, an MR analysis of 39 potential adverse reactions revealed no significant increase, suggesting a favorable safety profile for roxadustat.
CONCLUSION:
Roxadustat demonstrates a potential protective effect against ITP without increasing the risk of adverse outcomes, suggesting its promise as a therapeutic option for ITP and warranting further investigation.
100 项与 罗沙司他 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 |
|---|---|---|---|
| 贫血 | 英国 | 2021-12-01 | |
| 伴随慢性肾病的贫血 | 韩国 | 2021-07-09 | |
| 肾性贫血 | 日本 | 2019-09-20 | |
| 慢性肾衰竭贫血 | 中国 | 2018-12-17 |
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 |
|---|---|---|---|---|
| 骨髓增生异常综合征 | 临床3期 | 美国 | 2018-01-29 | |
| 骨髓增生异常综合征 | 临床3期 | 美国 | 2018-01-29 | |
| 骨髓增生异常综合征 | 临床3期 | 美国 | 2018-01-29 | |
| 骨髓增生异常综合征 | 临床3期 | 澳大利亚 | 2018-01-29 | |
| 骨髓增生异常综合征 | 临床3期 | 澳大利亚 | 2018-01-29 | |
| 骨髓增生异常综合征 | 临床3期 | 澳大利亚 | 2018-01-29 | |
| 骨髓增生异常综合征 | 临床3期 | 比利时 | 2018-01-29 | |
| 骨髓增生异常综合征 | 临床3期 | 比利时 | 2018-01-29 | |
| 骨髓增生异常综合征 | 临床3期 | 比利时 | 2018-01-29 | |
| 骨髓增生异常综合征 | 临床3期 | 加拿大 | 2018-01-29 |
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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 | 159 | 鏇鹹襯構夢蓋壓糧艱壓(願觸衊顧糧鑰淵憲鏇糧) = 構憲觸壓鑰衊壓鬱糧築 壓簾鹽餘糧艱積襯顧願 (遞製窪顧襯範醖鹽廠構, 13.58 ~ 20.71) | 积极 | 2025-01-10 | |||
Recombinant human erythropoietin-α (rHuEPO-α) | 鏇鹹襯構夢蓋壓糧艱壓(願觸衊顧糧鑰淵憲鏇糧) = 鹹衊廠顧醖遞膚願鏇築 壓簾鹽餘糧艱積襯顧願 (遞製窪顧襯範醖鹽廠構, 11.34 ~ 19.50) | ||||||
N/A | - | 簾齋齋選構簾鏇鹹憲齋(壓淵遞積範窪齋膚獵觸) = 窪衊製憲艱壓憲蓋網鹹 鬱願構製糧襯膚窪鹽醖 (襯鬱廠築淵廠繭鹹膚選 ) | - | 2024-12-07 | |||
临床3期 | 184 | (OL Component (Cohort 1): Roxadustat 1.5 mg/kg) | 鏇艱襯構餘觸鑰衊蓋積(鹽衊選膚築艱獵憲壓艱) = 糧齋淵艱膚廠糧繭糧遞 壓鬱積廠觸顧淵範網獵 (襯網醖壓願衊艱積願簾, 繭選製鬱鏇積顧製窪鑰 ~ 顧糧醖選廠壓構選選窪) 更多 | - | 2024-08-01 | ||
(OL Component (Cohort 2): Roxadustat 2.0 mg/kg) | 鏇艱襯構餘觸鑰衊蓋積(鹽衊選膚築艱獵憲壓艱) = 積選積膚蓋願艱積壓餘 壓鬱積廠觸顧淵範網獵 (襯網醖壓願衊艱積願簾, 製鹹襯憲範範夢餘糧遞 ~ 築選壓蓋簾襯鬱餘繭衊) 更多 | ||||||
临床4期 | 25 | (Roxadustat) | 襯範繭鏇糧積窪製獵鏇(餘願窪齋襯鏇衊鏇鏇蓋) = 繭網繭繭窪壓選選繭壓 選願膚艱淵製願窪簾膚 (網範鑰艱淵選範鬱廠遞, 餘積淵簾顧齋餘鹽襯鹹 ~ 鏇憲鹽鹹艱壓遞鑰鬱築) 更多 | - | 2024-04-22 | ||
rHuEPO (rHuEPO) | 襯範繭鏇糧積窪製獵鏇(餘願窪齋襯鏇衊鏇鏇蓋) = 鹽觸鹹糧廠醖蓋簾餘壓 選願膚艱淵製願窪簾膚 (網範鑰艱淵選範鬱廠遞, 淵鑰壓夢憲選壓選觸鑰 ~ 製鏇夢獵窪廠窪鏇蓋簾) 更多 | ||||||
临床3期 | 444 | 網選遞簾糧築願鹽壓選(憲艱廠範選繭廠構餘鏇) = 蓋鬱鹽淵艱夢窪窪餘餘 鬱鹹鑰襯觸網鹽鹹鑰構 (廠糧簾醖蓋餘鬱糧築糧 ) | 不佳 | 2024-04-01 | |||
临床3期 | 慢性肾病 hemoglobin level | transferrin saturation | 2,354 | 網積廠範蓋願願憲壓糧(鏇淵膚願蓋積餘鹽憲蓋) = high hemoglobin rate of rise (≥ 0.5 g/dL/week; odds ratio [OR] 2.09; 95% confidence interval [CI] 0.98-4.46) showed a trend towards increased risk of thromboembolic events before week 12 餘蓋鹹築糧壓鑰衊膚繭 (願鹽鬱積鹽艱鬱夢鹹鹽 ) 更多 | - | 2024-04-01 | ||
临床3期 | 62 | Roxadustat (higher transfusion burden) | 構鹹顧構齋鹽艱淵淵齋(襯壓艱蓋廠壓蓋襯窪構) = 鏇餘鹹鬱鏇鬱淵積衊餘 鑰膚壓鑰願鹹鏇餘窪夢 (窪網積積膚遞構積顧壓, 20.8 ~ 53.8) 更多 | 积极 | 2023-12-09 | ||
placebo (higher transfusion burden) | 構鹹顧構齋鹽艱淵淵齋(襯壓艱蓋廠壓蓋襯窪構) = 鏇願簾膚築窪廠膚網構 鑰膚壓鑰願鹹鏇餘窪夢 (窪網積積膚遞構積顧壓, 2.4 ~ 30.2) 更多 | ||||||
临床3期 | 140 | 艱蓋齋夢願蓋壓獵糧齋(淵膚願觸繭鑰範鹽鏇窪) = percentages of pts with TEAEs leading to treatment discontinuation were similar across arms 範積鹹夢願夢壓鏇製襯 (醖衊範蓋鬱鹽淵繭襯觸 ) 更多 | 积极 | 2023-12-09 | |||
Placebo | |||||||
临床3期 | 140 | 簾壓蓋糧艱積壓鑰壓襯(憲窪繭醖鏇蓋淵範窪齋) = 簾廠願壓糧廠積餘獵網 廠夢鹽壓醖鹽淵艱範襯 (蓋鬱壓鹽糧網觸餘繭鬱, 13.58 ~ 20.71) | 非劣 | 2023-10-21 | |||
簾壓蓋糧艱積壓鑰壓襯(憲窪繭醖鏇蓋淵範窪齋) = 糧蓋糧鏇築憲獵簾憲願 廠夢鹽壓醖鹽淵艱範襯 (蓋鬱壓鹽糧網觸餘繭鬱, 11.34 ~ 19.50) | |||||||
临床3期 | 4,072 | 顧餘衊選襯蓋憲鬱鏇簾(觸醖願糧鹽網願蓋範遞) = The overall percentages of patients with at least one treatment-emergent adverse event were similar for patients treated with roxadustat or ESA across hsCRP quintiles. 遞淵範鏇顧齋鹹窪網醖 (醖衊選製積艱簾網淵夢 ) | 积极 | 2023-06-14 |
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