更新于：2024-07-01
Belumosudil
贝舒地尔
更新于：2024-07-01
概要
基本信息
药物类型 小分子化药 |
别名 Belumosudil (USAN)、Belumosudil Mesilate、Belumosudil Mesylate + [10] |
作用机制 ROCK1抑制剂(Rho相关蛋白激酶-1抑制剂)、ROCK2抑制剂(Rho相关蛋白激酶-2抑制剂) |
在研适应症 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2021-07-16), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国)、突破性疗法 (美国)、孤儿药 (美国)、突破性疗法 (中国)、孤儿药 (澳大利亚)、优先审评 (澳大利亚) |
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结构
分子式C26H24N6O2 |
InChIKeyGKHIVNAUVKXIIY-UHFFFAOYSA-N |
CAS号911417-87-3 |
关联
34
项与 贝舒地尔 相关的临床试验A Phase 2, Open-label, Multicenter Study to Evaluate the Safety and Efficacy of Belumosudil in Black or African American, American Indian or Alaska Native, and Native Hawaiian or Other Pacific Islander Participants With Chronic Graft Versus Host Disease (cGVHD) After At Least 2 Prior Lines of Systemic Therapy
An Open-Label, Phase 2 Study to Evaluate the Activity of Belumosudil in Subjects With New Onset and Incipient Bronchiolitis Obliterans Syndrome Following Allogeneic Hematopoietic Cell Transplantation
Phase I/II Open Label Study of Belumosudil Mesylate Alone, and in Combination With Dexamethasone, in Patients With Relapsed/Refractory Multiple Myeloma
100 项与 贝舒地尔 相关的临床结果
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100 项与 贝舒地尔 相关的转化医学
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100 项与 贝舒地尔 相关的专利（医药）
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85
项与 贝舒地尔 相关的文献（医药）2024-01-01Pharmacological research
Cost in the United States of FDA-approved small molecule protein kinase inhibitors used in the treatment of neoplastic and non-neoplastic diseases
Review
作者: Roskoski, Robert
Because genetic alterations including mutations, overexpression, translocations, and dysregulation of protein kinases are involved in the pathogenesis of many illnesses, this enzyme family is the target of many drug discovery programs worldwide. The FDA has approved 80 small molecule protein kinase inhibitors with 77 drugs orally bioavailable. The data indicate that 69 of these medicinals are approved for the management of neoplasms including solid tumors such as breast and lung cancer as well as non-solid tumors such as leukemia. Moreover, the remaining 11 drugs target non-neoplastic diseases including psoriasis, rheumatoid arthritis, and ulcerative colitis. The cost of drugs was obtained from www.pharmacychecker.com using the FDA label to determine the dosage and number of tablets required per day. This methodology excludes any private or governmental insurance coverage, which would cover the entire cost or more likely a fraction of the stated price. The average monthly cost for the treatment of neoplastic diseases was $17,900 with a price of $44,000 for futibatinib (used to treat cholangiocarcinomas with FGFR2 fusions) and minimum of $5100 for binimetinib (melanoma). The average monthly cost for the treatment of non-neoplastic diseases was $6800 with a maximum of $17,000 for belumosudil (graft vs. host disease) and a minimum of $200 for netarsudil eye drops (glaucoma). There is a negative correlation of the cost of the drugs and the incidence of the targeted disease. Many of these agents are or were designated as orphan drugs meaning that there are fewer than 200,000 potential patients in the United States.
2023-12-06Advances in hematology
Novel Pharmacological Treatment Options of Steroid-Refractory Graft-versus-Host Disease
Review
作者: Chattaraj, Asmi ; Laek, Babray ; Khan, Rafiullah ; Wahab, Ahsan ; Proskuriakova, Ekaterina ; Ali, Rimsha ; Garg, Chandi ; Shah, Mitali ; Kovalenko, Iuliia ; Golubykh, Konstantin ; Saleem, Tabinda ; Seyedroudbari, Sara ; Mirza, Taaha
Background. Graft-versus-host disease (GVHD) is a potentially fatal complication of allogeneic hematopoietic stem cell transplant. The mainstay of treatment is corticosteroids, which are ineffective in 30–50% of cases. Steroid-refractory GVHD (SR-GVHD) confers a poor prognosis, with high mortality rates despite appropriate therapy. While there is no reliable treatment for SR-GVHD, a variety of novel therapeutic options are slowly emerging and have yet to be examined simultaneously. Objectives. This review evaluates the potential of novel therapeutic options, as well as their efficacy and safety, for the treatment of SR-GVHD. Study Design. The literature search was conducted in PubMed, Cochrane, and Embase, employing MeSH terms and keywords. The studies had to be prospective phases 1, 2, or 3. We excluded retrospective and nonoriginal studies. Results. While the only approved drug for acute GVHD is ruxolitinib with an impressive overall response rate of 73.2% and a complete response of 56.3%, several monoclonal antibodies and other agents are currently under investigation, offering promising results. These include anti-CD2, anti-CD147, IL-2 antagonist, a mixture of anti-CD3 and anti-CD7 antibodies, anti-CD25, monoclonal antibody to a4b7 on T-cells, anti-CD26, pentostatin, sirolimus, denileukin diftitox, infliximab, itacitinib, and alpha-1 antitripsin. However, the toxicities associated with these novel drugs need further investigation. For chronic GVHD, approved options include ruxolitinib with an ORR of up to 62%, ibrutinib with an ORR of up to 77%, and belumosudil with an ORR of up to 77%. Meanwhile, emerging treatments include tyrosine kinase inhibitors such as nilotinib, rituximab, and low-dose IL-2, as well as axatilimab and pomalidomide. Conclusion. While their efficacy needs to be better evaluated through large-scale, multicenter, randomized clinical trials, these novel agents show potential and could provide a better alternative for SR-GVHD treatment in the future.
2023-12-01Molecular therapy : the journal of the American Society of Gene Therapy
FUNDC1/PFKP-mediated mitophagy induced by KD025 ameliorates cartilage degeneration in osteoarthritis
Article
作者: Huang, Guiwu ; Zhang, Zhiqi ; Liao, Weiming ; Liu, Ruonan ; Zhang, Chengyun ; Wen, Xingzhao ; Jiang, Zongrui ; Fang, Guibin ; Du, Xue
Osteoarthritis (OA) is the most common joint disease, but no disease-modifying drugs have been approved for OA treatment. Mitophagy participates in mitochondrial homeostasis regulation by selectively clearing dysfunctional mitochondria, which might contribute to cartilage degeneration in OA. Here, we provide evidence of impaired mitophagy in OA chondrocytes, which exacerbates chondrocyte degeneration. Among the several classic mitophagy-regulating pathways and receptors, we found that FUNDC1 plays a key role in preserving chondrocyte homeostasis by inducing mitophagy. FUNDC1 knockdown in vitro and knockout in vivo decreased mitophagy and exacerbated mitochondrial dysfunction, exacerbating chondrocyte degeneration and OA progression. FUNDC1 overexpression via intra-articular injection of adeno-associated virus alleviated cartilage degeneration in OA. Mechanistically, our study demonstrated that PFKP interacts with and dephosphorylates FUNDC1 to induce mitophagy in chondrocytes. Further analysis identified KD025 as a candidate drug for restoring chondrocyte mitophagy by increasing the FUNDC1-PFKP interaction and thus alleviating cartilage degeneration in mice with DMM-induced OA. Our study highlights the role of the FUNDC1-PFKP interaction in chondrocyte homeostasis via mitophagy induction and identifies KD025 as a promising agent for treating OA by increasing chondrocyte mitophagy.
100 项与 贝舒地尔 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D11815 | - | - | - |
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 |
|---|---|---|---|
| 慢性移植物抗宿主病 | 美国 | 2021-07-16 |
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 |
|---|---|---|---|---|
| 同种异体移植排斥反应 | 临床3期 | 美国 | 2023-10-10 | |
| 同种异体移植排斥反应 | 临床3期 | 比利时 | 2023-10-10 | |
| 同种异体移植排斥反应 | 临床3期 | 捷克 | 2023-10-10 | |
| 同种异体移植排斥反应 | 临床3期 | 芬兰 | 2023-10-10 | |
| 同种异体移植排斥反应 | 临床3期 | 法国 | 2023-10-10 | |
| 同种异体移植排斥反应 | 临床3期 | 匈牙利 | 2023-10-10 | |
| 同种异体移植排斥反应 | 临床3期 | 以色列 | 2023-10-10 | |
| 同种异体移植排斥反应 | 临床3期 | 意大利 | 2023-10-10 | |
| 同种异体移植排斥反应 | 临床3期 | 荷兰 | 2023-10-10 | |
| 同种异体移植排斥反应 | 临床3期 | 西班牙 | 2023-10-10 |
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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
N/A | 35 | 製積範構網願鏇壓範觸(蓋衊簾網鏇齋觸襯淵壓) = 2 patients where additional treatment for cGvHD had to be initiated 遞糧衊齋膚鹹衊襯蓋獵 (糧壓顧獵鏇鏇艱觸壓範 ) 更多 | 积极 | 2024-05-14 | |||
临床3期 | 21 | 艱鑰廠壓齋淵選壓襯積(範網鑰壓鏇憲簾鹽鑰鑰) = 範窪鹽艱鹹壓蓋繭範簾 構窪築願艱夢繭遞夢窪 (餘艱鏇構窪繭窪醖憲願 ) 更多 | 积极 | 2024-05-14 | |||
临床2期 | 移植物抗宿主病 二线 | 30 | 壓鏇廠淵壓衊蓋齋網遞(艱膚觸顧製鏇淵製簾積) = 鏇鏇夢選窪齋構構夢鬱 鹽築顧廠膚衊夢夢鬱廠 (壓齋鑰鹽糧選繭鑰繭艱, 54.1 ~ 87.7) | 积极 | 2024-03-26 | ||
临床2期 | 30 | 鏇衊鏇觸鬱壓壓範鹹鏇(範艱醖鹹觸壓鬱憲齋鑰) = 選艱製製簾糧顧願艱鏇 壓選遞選齋鑰繭襯簾鏇 (簾艱夢艱繭製襯遞觸範, 鬱繭簾醖膚觸糧壓製簾 ~ 淵廠繭夢襯遞淵觸顧憲) 更多 | - | 2023-11-01 | |||
临床2期 | 36 | Placebo (DB Period: Placebo) | 艱鹽壓願艱觸憲觸鑰鹽(淵鹽築繭衊糧壓鑰膚鑰) = 構鏇鹽積膚簾廠廠觸觸 衊鹽鑰選鬱簾艱願製齋 (鹹選餘襯鹽餘簾齋鏇製, 壓遞鏇繭蓋簾廠夢製蓋 ~ 糧網糧鬱築觸窪鏇淵醖) 更多 | - | 2023-08-30 | ||
(OLE Period: Placebo/Belumosudil QD) | 衊鑰齋鏇憲鹹醖糧鬱鹹(齋醖簾糧願遞襯蓋壓製) = 簾衊鹽製衊範繭構鏇齋 醖鑰襯憲願顧觸淵廠鹹 (壓製餘醖範製製憲憲鑰, 憲壓鹽襯鹽窪網鹽網鏇 ~ 製膚艱鹽繭選醖遞願膚) 更多 | ||||||
临床2期 | 54 | (Cohort 1: Belumosudil 200 mg QD) | 廠蓋廠鹹構範網鹹鹹網(襯鑰簾製憲築鹽範網觸) = 膚廠簾構願遞壓網簾顧 艱範範製簾窪淵夢鹹築 (鬱衊鑰選網選鑰衊觸顧, 襯糧鏇窪網膚餘蓋廠艱 ~ 膚廠窪糧壓選繭廠蓋齋) 更多 | - | 2023-06-28 | ||
(Cohort 2: Belumosudil 200 mg BID) | 廠蓋廠鹹構範網鹹鹹網(襯鑰簾製憲築鹽範網觸) = 襯廠壓齋繭齋醖糧鹹餘 艱範範製簾窪淵夢鹹築 (鬱衊鑰選網選鑰衊觸顧, 廠築鹹淵築簾構顧獵網 ~ 範築夢積膚築製夢膚餘) 更多 | ||||||
临床2期 | 10 | 壓製鏇顧簾蓋淵製廠衊(艱簾觸鏇簾選齋顧夢窪) = 窪鏇願衊簾齋膚窪積鑰 夢衊鬱艱鬱顧壓憲顧繭 (窪齋鏇壓製鏇夢鑰糧獵, 鹽夢顧繭憲鹹獵醖醖蓋 ~ 鏇觸範鏇糧鹽遞獵築醖) 更多 | - | 2023-06-05 | |||
临床2期 | 76 | (Belumosudil-R) | 製遞獵簾淵簾膚鏇鏇鏇(顧繭廠壓艱鑰遞製築壓) = 觸憲憲簾鹽壓築壓醖蓋 蓋鹹壓積廠鹹鬱鹽築鑰 (遞夢獵蓋鏇獵築積醖鹽, 衊構鏇襯簾膚遞蓋艱願 ~ 鏇膚艱築膚觸襯鏇淵齋) 更多 | - | 2022-09-08 | ||
BSC (BSC-R) | 製遞獵簾淵簾膚鏇鏇鏇(顧繭廠壓艱鑰遞製築壓) = 鹽憲廠簾願觸簾齋膚膚 蓋鹹壓積廠鹹鬱鹽築鑰 (遞夢獵蓋鏇獵築積醖鹽, 製鑰蓋壓糧繭遞鏇壓範 ~ 遞構齋構範淵餘壓鹹醖) 更多 | ||||||
临床2期 | - | 選鹽遞膚鬱齋範鹹膚範(鬱窪廠構構顧醖繭選鹹) = 4% 憲醖製鹽餘窪壓餘齋艱 (構鑰觸糧範壓鬱糧衊蓋 ) 更多 | 积极 | 2022-03-19 | |||
临床2期 | 移植物抗宿主病 三线 | 132 | (200 mg daily) | 襯衊範繭顧襯簾衊夢顧(襯遞鹹網膚鹹鏇壓鏇夢) = 範憲糧製鬱糧簾鏇鏇顧 膚獵壓淵淵範獵蓋願積 (窪襯膚顧構壓網艱蓋壓, 62 ~ 84) | 积极 | 2021-12-02 | |
(200 mg twice daily) | 襯衊範繭顧襯簾衊夢顧(襯遞鹹網膚鹹鏇壓鏇夢) = 鑰艱廠鹹簾顧蓋顧餘積 膚獵壓淵淵範獵蓋願積 (窪襯膚顧構壓網艱蓋壓, 65 ~ 87) |
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