更新于：2024-07-01
Roxadustat
罗沙司他
更新于：2024-07-01
概要
基本信息
原研机构 |
非在研机构- |
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
分子式C19H16N2O5 |
InChIKeyYOZBGTLTNGAVFU-UHFFFAOYSA-N |
CAS号808118-40-3 |
关联
148
项与 罗沙司他 相关的临床试验A Phase 3, Open-label, Uncontrolled Study to Evaluate the Activity, Safety, Pharmacokinetics and Pharmacodynamics of Roxadustat for the Treatment of Anemia in Pediatric Participants with Chronic Kidney Disease - -
Hypoxic Enhancement Before Major Surgery (HYPE): A pilot randomised controlled trial of preoperative Roxadustat vs placebo in patients undergoing major surgery, assessing safety, effectiveness and feasibility.
罗沙司他胶囊单中心、随机、开放、单剂量、两制剂、两周期、两序列交叉设计，空腹和餐后状态下的人体生物等效性研究。
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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369
项与 罗沙司他 相关的文献（医药）2024-04-01Environmental toxicology
Roxadustat ameliorates vascular calcification in CKD rats by regulating HIF ‐2α/HIF ‐1α
Article
作者: Xiao, Min ; Shi, Tianli ; Cai, Feng ; Zhou, Xiaoyan ; Huang, Denggao ; Tian, Shuhong ; Wang, Yujing ; Li, Yang
Abstract:
Vascular calcification (VC) is a common complication of chronic kidney disease (CKD). VC is a gene‐regulated process similar to osteogenic differentiation. There are still no convincing schemes to prevent and reduce the development of VC. It has been reported that hypoxia‐inducing factor 1α (HIF‐1α) and endothelin‐1(ET‐1) are related to VC. In this study, we found that the expression of ET‐1 and HIF‐1α was enhanced after VC, the interaction between HIF‐1α and ET‐1 was confirmed by CO‐IP and luciferase experiments. We found that ET‐1 was an upregulated differential gene of calcified vascular smooth muscle cells (VSMCs) through gene sequencing. However, hypoxia‐inducing factor 2α (HIF‐2α) and HIF‐1α have antagonistic effects on each other. HIF‐1α is a pro‐inflammatory cytokine, and HIF‐2α can improve inflammation and fibrosis. Roxadustat, as a selective PHD3 inhibitor, preferentially activates HIF‐2α. It is still unclear whether roxadustat improves VC in CKD by regulating the expression of HIF‐2α/HIF‐1α. Alizarin red staining and western blot as well as immunohistochemical results showed that roxadustat could significantly reduce the degree of vascular and VSMCs calcification in CKD rats. Serum HIF‐1α and ET‐1 were significantly decreased after roxadustat treatment. In addition, western blot results showed that roxadustat could decrease the expression of HIF‐1α and ET‐1 in vascular tissues and calcified VSMC, but HIF‐2α expression significantly increased. Interestingly, our study confirmed that activation of HIF‐1α or inhibition of HIF‐2α reversed the ameliorating effect of roxadustat on VC, proving that the effect mediated by roxadustat is HIF‐2α/HIF‐1α dependent. We have demonstrated for the first time that roxadustat improves VC in CKD rats by regulating HIF‐2α/HIF‐1α, thus providing a new idea for the application of roxadustat in VC of CKD.
2024-03-01Journal of hypertension
Hypoxia-inducible factor-prolyl hydroxylase inhibitor Roxadustat (FG-4592) reduces renal fibrosis in Dahl salt-sensitive rats
Article
作者: Naito, Yoshiro ; Masuyama, Tohru ; Yasumura, Seiki ; Tsujino, Takeshi ; Ishihara, Masaharu ; Okuno, Keisuke ; Asakura, Masanori
Objective::
Although hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitors have been developed for the treatment of renal anemia, their effects on cardiac and renal dysfunction remain unknown. We previously reported on Dahl salt-sensitive rats, in a rat model of salt-sensitive hypertension, that exhibited anemia and impaired expression of duodenal iron transporters after the development of hypertensive cardiac and renal dysfunction. Therefore, we investigated the effects of Roxadustat (FG-4592), an HIF-PH inhibitor, on anemia, iron regulation, and cardiac and renal dysfunction in Dahl salt-sensitive rats.
Methods::
Six-week-old male Dahl salt-sensitive rats were fed a normal or high-salt diet for 8 weeks. A further subset of Dahl salt-sensitive rats, that were fed a high-salt diet, was administered Roxadustat for 8 weeks.
Results::
Dahl salt-sensitive rats fed a high-salt diet developed hypertension, cardiac and renal dysfunction, and anemia after 8 weeks of feeding. Roxadustat increased hemoglobin and serum erythropoietin levels in Dahl salt-sensitive rats fed a high-salt diet. With regard to the iron-regulating system, Roxadustat lowered hepatic hepcidin gene expression and increased the gene expression of duodenal iron transporters, such as cytochrome b and divalent metal transporter 1, in Dahl salt-sensitive rats fed a high-salt diet. Roxadustat did not affect the development of hypertension and cardiac hypertrophy in Dahl salt-sensitive rats with a high-salt diet; however, Roxadustat treatment attenuated renal fibrosis in these rats.
Conclusions::
Roxadustat ameliorated anemia with affecting the gene expression of the iron-regulating system, and did not affect cardiac hypertrophy but attenuated renal fibrosis in Dahl salt-sensitive rats fed a high-salt diet.
International urology and nephrology
A clinical study on roxadustat for anemia in diabetic nephropathy: a 8-week study
Article
作者: Sun, Dong ; Raj, Ashok ; Jia, Ruoyu ; Xu, Yizhou ; Zheng, Zhifang ; Jiang, Luhua ; Zhang, Xuejie
PURPOSE:
The development of roxadustat is a standard treatment for renal anemia, and multiple clinical trials have proved its safety and efficacy. However, less information is available from trials of the population with diabetic nephropathy (DN). This study aimed to determine whether roxadustat is effective for treating DN.
METHODS:
This was a single-center, retrospective, institutional review board-approved cohort study. The patients with DN were chosen and given roxadustat or erythropoietin (EPO) for 8 weeks. The mean hemoglobin (Hb) level after 8 weeks of treatment served as the primary outcome. Alterations in the iron index and lipid levels were considered secondary objectives. Sub-group analysis was performed to observe the impact of inflammation and glycemic status on Hb.
RESULTS:
A total of 80 patients were enrolled, 40 in each group. After 8 weeks of treatment, the Hb levels in the roxadustat group were higher than those in the control group. The number of patients who achieved Hb response was higher in the roxadustat group than in the control group (77.5% versus 27.5%; P < 0.001). In addition to lowering total cholesterol and low-density lipoprotein cholesterol, roxadustat decreased ferritin and elevated total iron-binding capacity. Compared to the control group, roxadustat was more beneficial for patients with an inflammatory condition and poor glycemic control.
CONCLUSIONS:
Roxadustat treatment remarkably corrected anemia in patients with DN, and its effectiveness was unaffected by inflammation or glycemic control levels. In addition, roxadustat can also reduce a patient's blood lipid level and enhance the body's use of iron.
CLINICAL TRIAL REGISTRATION:
ChiCTR2200057232.
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 | 2017-09-07 | |
| 骨髓增生异常综合征 | 临床3期 | 澳大利亚 | 2017-09-07 | |
| 骨髓增生异常综合征 | 临床3期 | 比利时 | 2017-09-07 | |
| 骨髓增生异常综合征 | 临床3期 | 加拿大 | 2017-09-07 | |
| 骨髓增生异常综合征 | 临床3期 | 丹麦 | 2017-09-07 | |
| 骨髓增生异常综合征 | 临床3期 | 法国 | 2017-09-07 | |
| 骨髓增生异常综合征 | 临床3期 | 德国 | 2017-09-07 | |
| 骨髓增生异常综合征 | 临床3期 | 印度 | 2017-09-07 | |
| 骨髓增生异常综合征 | 临床3期 | 以色列 | 2017-09-07 | |
| 骨髓增生异常综合征 | 临床3期 | 意大利 | 2017-09-07 |
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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4期 | 25 | (Roxadustat) | 網襯願願顧夢願繭獵構(廠構憲憲顧構遞築襯繭) = 積獵蓋鹹夢觸鑰網壓簾 鏇膚膚鬱醖築膚鬱獵觸 (積願憲襯願夢憲憲鹹餘, 鹽夢鏇艱夢選繭淵願淵 ~ 鹹夢壓鏇觸簾夢衊艱網) 更多 | - | 2024-04-22 | ||
rHuEPO (rHuEPO) | 網襯願願顧夢願繭獵構(廠構憲憲顧構遞築襯繭) = 鹽醖積鹹艱製製鬱願遞 鏇膚膚鬱醖築膚鬱獵觸 (積願憲襯願夢憲憲鹹餘, 鑰遞餘獵鏇衊壓觸壓膚 ~ 願窪範鏇醖齋壓壓鬱鏇) 更多 | ||||||
临床3期 | 慢性肾病 hemoglobin level | transferrin saturation | 2,354 | 範願鏇獵夢齋艱選襯壓(鑰餘顧鏇鹹網壓獵繭窪) = 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 繭繭獵齋積夢獵獵簾製 (襯簾簾憲膚鏇夢鏇夢憲 ) 更多 | - | 2024-04-01 | ||
临床3期 | 62 | Roxadustat (higher transfusion burden) | 醖鹹繭齋夢觸鬱網醖襯(廠製憲繭鬱鑰糧窪鹽觸) = 鹹鹽鹽廠夢餘廠蓋鑰餘 襯選窪淵願網築範齋觸 (願選淵襯憲衊衊鏇壓窪, 20.8 ~ 53.8) 更多 | 积极 | 2023-12-09 | ||
placebo (higher transfusion burden) | 醖鹹繭齋夢觸鬱網醖襯(廠製憲繭鬱鑰糧窪鹽觸) = 鑰衊糧窪齋遞範廠壓憲 襯選窪淵願網築範齋觸 (願選淵襯憲衊衊鏇壓窪, 2.4 ~ 30.2) 更多 | ||||||
临床3期 | 140 | 選獵觸顧衊選顧壓艱選(夢獵壓衊鬱鬱餘獵醖觸) = percentages of pts with TEAEs leading to treatment discontinuation were similar across arms 膚艱簾醖顧衊遞淵製構 (糧獵鬱餘選壓衊衊鹽夢 ) 更多 | 积极 | 2023-12-09 | |||
Placebo | |||||||
ESMO2023 人工标引  | 临床3期 | 140 | 醖襯簾廠夢獵鑰鑰齋網(憲蓋選鬱壓蓋窪觸憲齋) = 鹹衊鏇獵鹹鑰鑰範襯窪 獵觸糧網糧憲廠襯觸繭 (蓋積積觸鹽餘衊獵醖淵, 13.58 ~ 20.71) | 非劣 | 2023-10-21 | ||
醖襯簾廠夢獵鑰鑰齋網(憲蓋選鬱壓蓋窪觸憲齋) = 觸鹽壓憲鬱襯製繭顧簾 獵觸糧網糧憲廠襯觸繭 (蓋積積觸鹽餘衊獵醖淵, 11.34 ~ 19.50) | |||||||
N/A | 93 | 蓋構廠糧鏇淵選廠構遞(齋鹹鬱繭夢廠艱獵鏇觸) = 獵齋艱廠淵鏇選繭構鏇 遞繭夢廠衊積壓範選醖 (築襯遞顧餘構齋夢壓餘 ) | - | 2023-06-15 | |||
临床3期 | - | 4,072 | 構遞齋衊憲鹽鬱衊餘範(淵淵網簾積窪壓鑰鬱淵) = 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. 糧糧壓鬱廠簾醖選糧憲 (觸糧遞鹽構餘鹹遞遞願 ) | 积极 | 2023-06-14 | ||
临床3期 | 2,142 | 鏇醖遞壓積簾選選遞蓋(鹽襯鹹製範選觸夢衊艱): HR = 0.79 (95% CI, 0.61 ~ 1.02) 更多 | 积极 | 2023-02-07 | |||
临床3期 | - | 蓋鬱淵糧獵鏇製範選醖(醖襯糧壓餘餘選築衊鏇) = 憲衊鹹繭網鏇鏇願獵鑰 繭繭壓憲夢鹹遞鹽選繭 (淵淵廠窪築繭餘製鹽醖, -4.37 ~ -2.59) 更多 | 积极 | 2022-11-03 | |||
N/A | - | 1,763 | 遞鹽糧構構鹽蓋膚選繭(觸淵觸憲鏇襯襯鬱獵構) = 鏇艱膚遞膚鏇窪選醖積 餘遞蓋觸願鏇廠蓋簾襯 (憲遞醖顧鹹網繭蓋鹽顧 ) 更多 | 积极 | 2022-11-03 | ||
遞鹽糧構構鹽蓋膚選繭(觸淵觸憲鏇襯襯鬱獵構) = 鑰範衊夢鏇範顧衊繭膚 餘遞蓋觸願鏇廠蓋簾襯 (憲遞醖顧鹹網繭蓋鹽顧 ) 更多 |
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