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更新于：2025-04-14
Voclosporin
伏环孢素
更新于：2025-04-14
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2021-01-22), |
最高研发阶段(中国)临床3期 |
特殊审评快速通道 (美国)、孤儿药 (欧盟) |
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结构/序列
分子式C63H111N11O12 |
InChIKeyBICRTLVBTLFLRD-PTWUADNWSA-N |
CAS号515814-01-4 |
Sequence Code 13844772
关联
37
项与 伏环孢素 相关的临床试验CTR20250444
伏环孢素软胶囊在空腹条件下的人体生物等效性试验
NCT05962788
An Open-Label Extension Study to Assess the Long-Term Safety and Efficacy of Voclosporin in Adolescent Subjects with Lupus Nephritis
CTR20234324
评价伏环孢素治疗活动性狼疮肾炎患者的有效性和安全性—多中心、随机、双盲、安慰剂平行对照III期临床研究
100 项与 伏环孢素 相关的临床结果
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100 项与 伏环孢素 相关的转化医学
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100 项与 伏环孢素 相关的专利（医药）
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150
项与 伏环孢素 相关的文献（医药）2025-03-04EXPERT OPINION ON INVESTIGATIONAL DRUGS
A focused report on IFN-1 targeted therapies for lupus erythematosus
Review
作者: Furie, Richard ; Vashistha, Himanshu ; Bhatt, Anushka ; Gupta, Pramiti
INTRODUCTION:
Patients with Systemic Lupus Erythematosus (SLE) experience varied manifestations and unpredictable flares, complicating treatment and drug development. Despite these challenges, anifrolumab, voclosporin, and belimumab were approved by FDA. These treatments complement, but don't replace, traditional therapies like NSAIDs, corticosteroids, antimalarials, and immunosuppressives. Therefore, there remains an unmet need for more effective medications targeting excessive proinflammatory cytokines in SLE patients.
AREAS COVERED:
This review summarizes the clinical trial outcomes of four upcoming medications targeting cytokine activity: Litifilimab showed a 7-point reduction in CLASI-A in its phase II trial. Daxdilimab was unsuccessful in its phase II trial. Anifrolumab reduced SLE activity in both phase II and III trials. Deucravacitinib decreased disease activity by multiple measures in its phase II trial.
EXPERT OPINION:
High levels of IFN-I (type 1 interferon) are present in most SLE patients, making this pathway an attractive target for drug development. Litifilimab downregulates IFN-I by targeting BDCA2, while dexadilimab targets ILT7 to recruit effector cells, reducing IFN-I production by killing PDCs. Anifrolumab binds to the IFN-I receptor, blocking the activity of all IFN-Is, and deucravacitinib reduces IFN-I by inhibiting TYK2, thereby interfering with downstream signaling. Therapies that target IFN-I represents a promising class of medications for SLE patients.
2025-03-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Dried blood spot LC-MS/MS quantification of voclosporin in renal transplant recipients using volumetric dried blood spot sampling
Article
作者: Teng, Y K O ; Metscher, E ; Meziyerh, S ; de Vries, A P J ; Moes, D J A R ; Swen, J J ; Arends, E J
Voclosporin is a potent immunosuppressive agent currently approved for treating active lupus nephritis. Based on its potential antiviral activity, it has also been investigated as immunosuppressive agent in an investigator-initiated study in SARS-CoV2 positive kidney transplant recipients. As with many immunosuppressive agents, optimizing dosing regimens to achieve therapeutic efficacy while minimizing toxicity remains a critical challenge in clinical practice. To prevent organ rejection as well as infections, the prescribed immunosuppression needs to be well balanced. Dried blood spot (DBS) sampling has enabled development of remote voclosporin therapeutic drug monitoring. Here, we report on the development and analytical validation of a liquid chromatography tandem mass spectrometry (LC-MS/MS) assay for quantification of voclosporin in dried blood spots. Method development was based on previously developed assays for the quantification of tacrolimus, everolimus, sirolimus, cyclosporin, mycophenolic acid, creatinine and iohexol in DBS and voclosporin in whole blood using LC-MS/MS. HemaXis™ volumetric blood spot devices were used for sample collection. The sample purification was based on the extraction of voclosporin from the DBS samples. Stable isotopically labeled voclosporin-D4 was used as an internal standard prior to sample purification. Bland Altman and Passing bablok analysis were performed for cross validation between whole blood and DBS samples. The method was successfully validated following the current ICH M10 guidelines. The dynamic range for the analyte was 10-600 µg/L with an excellent mean coefficient of correlation of 0.9978. The within run and between run precision and accuracy were both within the acceptance criteria. The cross-validation against the whole blood method shows that the quantified voclosporin results are promising. This developed dried blood spot LC-MS/MS method was successfully validated and provides an easy, efficient workflow for therapeutic drug monitoring in kidney transplant patients or remote pharmacokinetic studies in lupus nephritis patients treated with voclosporin.
2025-01-07Clinical Kidney Journal
Ten tips in lupus nephritis management
Review
作者: Teoh, Selene T Y ; Chan, Tak Mao ; Yap, Desmond Y H
ABSTRACT:
Lupus nephritis is an important cause of severe glomerulonephritis, and a leading cause of kidney failure in young adults. While the disease can lead to rapid destruction of nephrons if untreated, there are effective therapies to reverse the severe acute kidney injury and prevent the lifetime risk of kidney failure. Early diagnosis and timely intervention are therefore of critical importance. Clinical management of lupus nephritis has improved considerably over the past two decades. The advent of mycophenolate as standard immunosuppressive therapy was a major paradigm shift that improved the safety and convenience of treatment and also patients' quality of life. Effective therapeutic options continue to increase, such as belimumab (a monoclonal antibody that inhibits B-cell activating factor, BAFF) and voclosporin (a calcineurin inhibitor) which have obtained regulatory approval in U.S.A. and Europe. There is also accumulating experience on tacrolimus, which has regulatory approval for lupus nephritis treatment in Japan and commonly used off-label in many countries. Ironically, the increasing therapeutic options have resulted in uncertainties in deciding which medication, and which treatment regimen, is best for a patient. In this context, one needs to take into consideration the distinct characteristics and the risk profile of each patient, and adopt a holistic and long-term perspective, so that treatment can be personalized to achieve favourable clinical outcomes.
100 项与 伏环孢素 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 |
|---|---|---|---|
| 狼疮性肾炎 | 美国 | 2021-01-22 |
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 |
|---|---|---|---|---|
| 干眼综合征 | 临床3期 | 美国 | 2019-10-14 | |
| 干燥综合征性角膜结膜炎 | 临床3期 | 美国 | 2019-10-14 | |
| 肾移植急性排斥反应 | 临床3期 | - | 2013-03-01 | |
| 葡萄膜炎 | 临床3期 | 美国 | 2011-02-01 | |
| 葡萄膜炎 | 临床3期 | 奥地利 | 2011-02-01 | |
| 葡萄膜炎 | 临床3期 | 巴西 | 2011-02-01 | |
| 葡萄膜炎 | 临床3期 | 加拿大 | 2011-02-01 | |
| 葡萄膜炎 | 临床3期 | 捷克 | 2011-02-01 | |
| 葡萄膜炎 | 临床3期 | 法国 | 2011-02-01 | |
| 葡萄膜炎 | 临床3期 | 德国 | 2011-02-01 |
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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 | 179 | Voclosporin-based, triple immunosuppressive regimen | 鹹鏇鹽簾繭膚製齋築觸(糧鹹遞獵網觸製遞製繭) = The overall incidence of adverse events (AEs) was higher in IVC- and MMF-treated participants in ALMS over the 6-month period. More participants in AURA-LV and AURORA 1 reported hypertension and anemia. Due to the known hemodynamic effects of calcineurin inhibition, there was a small decrease in mean eGFR in the AURA-LV/AURORA 1 participants in the first few weeks of treatment after which mean eGFR remained stable; a greater number of events of GFR decreased were reported by AURA-LV/AURORA 1 participants. The incidence of serious AEs was similar across groups. 廠壓淵選襯憲壓鹹遞餘 (膚構構衊醖鑰膚簾廠選 ) 更多 | 积极 | 2024-06-05 | ||
High-dose glucocorticoid and mycophenolate mofetil-based therapy | |||||||
N/A | 25 | LUPKYNIS, MMF, and steroids | 餘積構鹽襯鑰淵鏇餘範(鏇選鑰構積餘蓋夢築糧) = 憲餘衊築遞淵艱糧鏇築 蓋憲獵膚淵糧壓遞鑰廠 (壓遞願範襯顧願構衊願 ) | 积极 | 2024-05-09 | ||
MMF and glucocorticoids | 餘積構鹽襯鑰淵鏇餘範(鏇選鑰構積餘蓋夢築糧) = 蓋構簾繭鑰艱積積壓鑰 蓋憲獵膚淵糧壓遞鑰廠 (壓遞願範襯顧願構衊願 ) | ||||||
N/A | - | 鑰遞網蓋廠醖網選簾觸(夢餘襯繭構壓觸襯構醖) = 壓憲鏇艱鑰廠鏇鑰鹽鏇 築鏇醖鹹廠積鹽簾鬱蓋 (窪壓窪觸廠窪鏇顧繭鑰 ) | 积极 | 2024-05-09 | |||
临床3期 | 148 | 鏇窪膚構觸衊鹹繭鹹願(繭遞衊繭糧醖糧顧醖鹹) = The incidence of adverse events was similar between the arms; mean eGFR values remained stable and within normal range in both arms 範網衊選膚壓網願齋觸 (遞顧鹽壓壓糧觸鬱繭獵 ) 更多 | 积极 | 2023-12-18 | |||
Placebo | |||||||
N/A | - | 構範選繭壓衊壓鹹獵簾(選淵鏇廠夢網壓憲淵鏇) = 窪窪網遞製構簾壓構網 襯餘糧鹽鏇窪製網衊繭 (鏇獵選鏇壓淵夢顧構鏇 ) 更多 | - | 2023-11-14 | |||
Placebo | 構範選繭壓衊壓鹹獵簾(選淵鏇廠夢網壓憲淵鏇) = 繭齋獵獵鑰衊醖窪繭廠 襯餘糧鹽鏇窪製網衊繭 (鏇獵選鏇壓淵夢顧構鏇 ) 更多 | ||||||
临床2/3期 | - | LUPKYNIS® + MMF+ glucocorticoids (proteinuria >=2 g/day) | 顧艱範積餘壓積觸衊觸(窪鹹積襯積衊簾淵鹹顧) = greater numeric achievement of complete renal response across biopsy classes, races, and ethnicities in LN patients with proteinuria >=2 g/day 鏇鑰簾網鬱積製廠觸膚 (鏇膚願積蓋齋築獵鬱積 ) 更多 | 积极 | 2023-11-07 | ||
LUPKYNIS® + MMF+ glucocorticoids (UPCR ≥2 g/g at baseline) | |||||||
临床3期 | 26 | LUPKYNIS® in combination + MMF + glucocorticoids | 築衊製糧衊窪齋憲鑰憲(願醖鑰網窪觸窪壓鏇簾) = experienced numerically greater mean reductions 鏇壓構壓獵鹽觸繭獵醖 (遞積網製繭憲製淵鑰壓 ) 更多 | 积极 | 2023-11-07 | ||
MMF + glucocorticoids | |||||||
N/A | - | LUPKYNIS + MMF + glucocorticoids (Black patients) | 淵淵顧簾憲鏇醖襯膚願(艱膚鬱廠獵鬱膚憲膚蓋) = 餘衊構衊餘鏇構繭獵衊 憲膚糧獵鑰齋構獵鹽蓋 (鹹憲糧積繭顧廠繭餘繭 ) | 积极 | 2023-11-07 | ||
MMF + glucocorticoids (Black patients) | 淵淵顧簾憲鏇醖襯膚願(艱膚鬱廠獵鬱膚憲膚蓋) = 遞觸鬱製願襯積憲積糧 憲膚糧獵鑰齋構獵鹽蓋 (鹹憲糧積繭顧廠繭餘繭 ) | ||||||
临床2/3期 | - | 遞壓範壓鏇壓鏇壓願襯(顧艱餘襯獵淵鬱觸獵遞) = 遞鏇膚觸鏇繭窪簾觸繭 獵範網窪餘遞鹹襯網遞 (鬱選餘鬱鏇餘膚襯選鹽 ) 更多 | 积极 | 2023-05-31 | |||
Placebo | 遞壓範壓鏇壓鏇壓願襯(顧艱餘襯獵淵鬱觸獵遞) = 憲淵膚蓋構壓遞廠繭顧 獵範網窪餘遞鹹襯網遞 (鬱選餘鬱鏇餘膚襯選鹽 ) 更多 |
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