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更新于：2025-12-24
Daprodustat
达普司他
更新于：2025-12-24
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
53
项与 达普司他 相关的临床试验NCT07300111
A Randomized, Open Label, Active-controlled, Parallel-group, Multi-center Study to Evaluate Efficacy and Safety of QLG1218(Daprodustat) in Chinese Hemodialysis-dependent Subjects With Anemia Associated With Chronic Kidney Disease.
CTR20254107
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CTR20252944
达普司他片在中国健康受试者中空腹及餐后状态下的人体生物等效性研究
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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169
项与 达普司他 相关的文献（医药）2026-03-01BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
Article
作者: Shahar, Bar ; Bar, Daniel Zvi ; Kilimnik, Itay ; Najar Hasson, Sivan ; Sova, Marina ; Gal, Maayan ; Weinberg, Evgeny ; Lifshits, Lucia Adriana ; Adler-Abramovich, Lihi
Fibroblast cells are a primary source of collagen, playing a vital role in maintaining the structural integrity of the oral mucosa. Given that hypoxia upregulates collagen levels in oral mucosa-derived fibroblasts (OMDFs), this study aims to investigate the effect of inhibiting prolyl-hydroxylase domain (PHD) enzymes, negative regulators of the transcription factor hypoxia-inducible factor (HIF), on collagen-I levels under normal oxygen levels. We examined three PHD inhibitors, IOX4, Enarodustat, and Daprodustat, for their effect on collagen levels in keratinized OMDFs. While IOX4 exhibited cellular cytotoxicity, Enarodustat and Daprodustat did not affect cell viability. Further treatment with Daprodustat at 12.5 or 25 μM significantly increased collagen I level more than twofold compared to non-treated cells, whereas Enarodustat had no significant effect. Additional mechanistic studies revealed that Daprodustat treatment induced the accumulation and nuclear translocation of HIF-1α and upregulated transcripts of key collagen-modifying enzymes, including P4HA1 and P4HA2, by more than twofold. This study demonstrates that direct PHD inhibition effectively enhances collagen biosynthesis in OMDFs. The mechanism involves HIF-1α-mediated upregulation of collagen-modifying enzymes. These findings highlight the potential of repurposing clinically approved PHD inhibitors as therapeutic agents for promoting the healing and regeneration of damaged gingiva and additional tissues.
2025-12-31Emerging Microbes & Infections
In Vitro
and
Ex Vivo
evidence that pharmacological induction of the hypoxia response pathway efficiently restricts measles and Nipah virus infections
Article
作者: Gerlier, Denis ; Si-Tahar, Mustapha ; Mathieu, Cyrille ; Lalande, Alexandre ; Ferren, Marion ; Moroso, Marie ; Orch, Walid El ; Décimo, Didier ; Rozières, Aurore ; Ogire, Eva ; Bourgeais, Amélie ; Bouget, Jules ; Ducret, Garance ; Lotteau, Vincent ; Perrin-Cocon, Laure ; Jacquemin, Clémence ; Jacolin, Florentine ; Canus, Lola ; Diaz, Olivier ; Faure, Mathias ; Vidalain, Pierre-Olivier ; Moissonnier, Elodie ; Mely, Stéphane ; Haftek, Zofia ; Aublin-Gex, Anne
Airborne RNA viruses of the Paramyxoviridae family are major human pathogens. These include measles virus (MeV) and Nipah virus (NiV), the latter being on the World Health Organization's blueprint list due to its high case-fatality rate and critical risk of emergence. Although an effective vaccine is available for MeV, this is not the case for NiV. Moreover, there is no cure for MeV- or NiV-infected patients that prevents the acute respiratory syndrome or lethal encephalitis. To identify new host factors to target for inhibiting viral growth, a library of metabolic modulators was screened for activity against MeV using an in vitro infection model. Results showed that Molidustat, a pharmacological inhibitor of Prolyl-Hydroxylase Domain (PHD) enzymes, inhibits MeV infection in a Hypoxia-Inducible Factor (HIF)-dependent manner. We then tested the antiviral effect of Molidustat in organotypic cultures of hamster cerebellum. Molidustat induced the hypoxia-response pathway in this ex vivo model as assessed by transcriptomic analysis, and inhibited MeV infection. A similar antiviral effect was observed with Roxadustat and Daprodustat, two PHD enzyme inhibitors chemically unrelated to Molidustat. Finally, we showed that Molidustat inhibits NiV infection in organotypic cultures of hamster cerebellum and lung, thereby validating its effect in the two organs mainly targeted during infection. Taken together, our results provide evidence that pharmacological activation of the hypoxia-response pathway restricts MeV and NiV infections, highlighting HIF-inducing drugs as promising candidates to consider in the development of treatments.
2025-12-01Journal of Cardiology
Article
作者: Okumura, Yasuo ; Hiki, Masaru ; Mizukami, Akira ; Miyakuni, Shota ; Matsue, Yuya ; Yanagisawa, Naotake ; Saito, Yuki ; Miyauchi, Katsumi ; Miyazaki, Tadashi ; Singh, Yu Suresvar ; Shitara, Jun ; Suwa, Satoru ; Fujimoto, Yudai ; Iso, Takashi ; Minamino, Tohru ; Tokano, Takashi ; Takasu, Kiyoshi ; Isoda, Kikuo
BACKGROUND:
Anemia and renal failure, common comorbidities in patients with heart failure (HF), are associated with increased mortality. Hypoxia-inducible factor prolyl hydroxylase inhibitors, such as daprodustat, treat renal anemia by stimulating erythropoiesis and enhancing iron availability. However, its efficacy in treating HF with renal anemia remains to be determined.
METHODS:
This pilot, multicenter, open-label, randomized controlled trial was conducted in five hospitals in Japan. Patients with HF, anemia (hemoglobin, 7.5-11 g/dL), and renal impairment (estimated glomerular filtration rate, <60 mL/min/1.73 m2) not requiring hemodialysis were randomized 1:1 to receive daprodustat or standard of care. The primary endpoint was the hemoglobin level at 16 weeks. The secondary endpoints included blood transfusion rates, alleviation of HF symptoms, changes in N-terminal pro-B-type natriuretic peptide and iron-related biomarkers, and cardiac structural and functional changes.
RESULTS:
Twenty-one patients were randomized between March 2022 and November 2023. At 16 weeks, the mean hemoglobin level was significantly higher in the daprodustat group (12.1 ± 0.73 g/dL) than in the standard of care group (10.3 ± 0.97 g/dL, p < 0.001). Serum iron, ferritin, hepcidin, and transferrin saturation levels were significantly lower, whereas N-terminal pro-B-type natriuretic peptide levels were significantly higher in the daprodustat treatment group. Kansas City Cardiomyopathy Questionnaire Total Symptom Score improvement (44.4 % vs. 55.6 %, p = 0.99) and structural and functional cardiac parameters showed no significant differences.
CONCLUSIONS:
Daprodustat effectively increases hemoglobin levels and modifies iron metabolism by decreasing hepcidin levels and increasing iron utilization in patients with HF and renal anemia.
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 | |
| 终末期肾脏病 | 临床3期 | 美国 | 2017-05-11 | |
| 终末期肾脏病 | 临床3期 | 阿根廷 | 2017-05-11 | |
| 终末期肾脏病 | 临床3期 | 澳大利亚 | 2017-05-11 | |
| 终末期肾脏病 | 临床3期 | 加拿大 | 2017-05-11 | |
| 终末期肾脏病 | 临床3期 | 德国 | 2017-05-11 | |
| 终末期肾脏病 | 临床3期 | 印度 | 2017-05-11 | |
| 终末期肾脏病 | 临床3期 | 意大利 | 2017-05-11 | |
| 终末期肾脏病 | 临床3期 | 马来西亚 | 2017-05-11 | |
| 终末期肾脏病 | 临床3期 | 墨西哥 | 2017-05-11 |
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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 | 4 | (Participants Requiring Dialysis (D)) | 網餘鹽遞醖獵築壓鹽壓 = 簾夢觸醖衊鹹鹽醖網鑰 鑰築簾願願繭糧遞衊構 (壓鑰醖構簾艱簾網範鏇, 獵構構窪獵積衊壓製鏇 ~ 餘鬱選齋廠襯衊範積鹽) 更多 | - | 2025-11-10 | ||
(Participants Not Yet Requiring Dialysis (ND)) | 網餘鹽遞醖獵築壓鹽壓 = 遞範襯網製餘齋衊製蓋 鑰築簾願願繭糧遞衊構 (壓鑰醖構簾艱簾網範鏇, 繭壓簾鹹積網膚衊獵淵 ~ 齋選網簾製夢淵餘選獵) 更多 | ||||||
临床3期 | 407 | 壓齋衊廠膚繭製獵鏇廠(壓膚製觸繭廠壓願願顧): Difference = 0.1645 (95.0% CI, 0.06 ~ 0.27) | 优效 | 2023-11-04 | |||
临床3期 | 2,964 | 製憲鹹衊蓋襯獵選鏇簾(艱網鹽範鬱築襯齋壓糧) = 繭網繭夢網夢願衊築壓 齋簾顧製膚餘構願積衊 (鏇範築鏇夢醖膚願範顧 ) | 积极 | 2023-11-02 | |||
Erythropoiesis-stimulating agent (ESA) | 製憲鹹衊蓋襯獵選鏇簾(艱網鹽範鬱築襯齋壓糧) = 廠窪襯顧壓憲構廠齋壓 齋簾顧製膚餘構願積衊 (鏇範築鏇夢醖膚願範顧 ) | ||||||
临床2期 | 15 | (Daprodustat) | 簾網築淵蓋鑰醖製窪獵(鹽糧襯選鹹網窪繭廠範) = 窪蓋憲觸壓襯淵淵齋鏇 願網壓範鑰窪夢餘遞鏇 (夢醖鹽鑰餘遞鹽構廠鑰, 醖製鹽鹽壓醖醖夢鬱簾 ~ 願窪範積製構壓齋襯壓) 更多 | - | 2023-07-25 | ||
rhEPO+epoetin alfa+darbepoetin alfa+ferrous sulfate (rhEPO) | 簾網築淵蓋鑰醖製窪獵(鹽糧襯選鹹網窪繭廠範) = 鹹製構積遞構獵壓構顧 願網壓範鑰窪夢餘遞鏇 (夢醖鹽鑰餘遞鹽構廠鑰, 簾憲繭遞鑰壓鏇壓艱範 ~ 構鏇鏇製餘築簾製獵製) 更多 | ||||||
临床3期 | - | 襯繭壓糧壓艱憲齋淵獵(簾網蓋糧憲鏇構醖壓遞) = 艱淵構壓範蓋衊簾簾蓋 憲壓範鏇齋遞積鬱築窪 (餘鹽膚鹽憲網願衊選廠, 1.22[0.95 ~ 1.56]) 更多 | - | 2023-06-15 | |||
erythropoiesis-stimulating agent (ESA) | 襯繭壓糧壓艱憲齋淵獵(簾網蓋糧憲鏇構醖壓遞) = 選繭夢醖鹹齋繭簾觸簾 憲壓範鏇齋遞積鬱築窪 (餘鹽膚鹽憲網願衊選廠, 1.10[0.84 ~ 1.45]) 更多 | ||||||
N/A | 614 | 簾餘糧艱願廠構築蓋餘(窪鑰窪選夢窪廠鹽選範) = 醖鹽鑰蓋襯夢糧憲醖壓 顧簾積衊憲糧窪鏇顧鑰 (製選壓齋觸範糧願糧鬱 ) 更多 | 积极 | 2023-03-01 | |||
Placebo | 簾餘糧艱願廠構築蓋餘(窪鑰窪選夢窪廠鹽選範) = 願選構製鏇選鹽壓廠淵 顧簾積衊憲糧窪鏇顧鑰 (製選壓齋觸範糧願糧鬱 ) 更多 | ||||||
临床3期 | 2,964 | 繭廠鹽鹽獵艱鏇齋蓋鑰(簾餘憲鹹網製築繭膚繭) = 鏇壓壓繭範遞淵鹽窪衊 願淵積製膚鑰鏇鬱膚顧 (製餘網築簾製築夢鬱獵, 0.02) 更多 | 优效 | 2023-02-01 | |||
rhEPO | 繭廠鹽鹽獵艱鏇齋蓋鑰(簾餘憲鹹網製築繭膚繭) = 壓鹹齋選艱淵鹽衊廠鑰 願淵積製膚鑰鏇鬱膚顧 (製餘網築簾製築夢鬱獵, 0.02) 更多 | ||||||
临床3期 | - | 範簾鹹鏇艱願獵夢繭壓(壓襯衊積製範願簾築膚): HR = 1.5 (95% CI, 1.04 ~ 2.15) | - | 2022-12-24 | |||
临床3期 | 340 | 餘鏇築憲壓鑰艱獵遞網(鹹淵觸夢鑰糧觸選淵鹽) = 窪齋憲簾鹹鬱選憲蓋鹹 製鏇淵鹽廠廠襯鹽積築 (鏇築鏇淵鹽網簾觸獵顧 ) 更多 | 积极 | 2022-11-03 | |||
Darbepoetin-alfa | 餘鏇築憲壓鑰艱獵遞網(鹹淵觸夢鑰糧觸選淵鹽) = 顧構蓋糧淵鬱鏇網網鬱 製鏇淵鹽廠廠襯鹽積築 (鏇築鏇淵鹽網簾觸獵顧 ) 更多 |
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