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更新于：2025-12-02
Rilzabrutinib
利扎布替尼
更新于：2025-12-02
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2025-08-29), |
最高研发阶段(中国)申请上市 |
特殊审评快速通道 (美国)、孤儿药 (美国)、孤儿药 (欧盟)、孤儿药 (日本) |
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结构/序列
分子式C36H40FN9O3 |
InChIKeyLCFFREMLXLZNHE-GBOLQPHISA-N |
CAS号1575596-29-0 |
关联
29
项与 利扎布替尼 相关的临床试验NCT07007962
A Multi-center, Open-label, Single-arm Study to Evaluate the Efficacy and Safety of Oral Rilzabrutinib in Adults With Immune Thrombocytopenia (ITP) Who Failed First-line Treatment
NCT07216079
An Open-label Extension Study for Oral Rilzabrutinib in Adults With Chronic Immune Thrombocytopenia (ITP) Who Have Completed the Long-term Extension (LTE) of the LUNA 3 Study (PRN1008 018/EFC17093) in Japan
NCT07190196
A Randomized, Phase 3, Double-blind, 52-week Study to Evaluate the Efficacy and Safety of Rilzabrutinib (SAR444671) Compared to Placebo in Adult Participants With Active IgG4-related Disease
100 项与 利扎布替尼 相关的临床结果
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100 项与 利扎布替尼 相关的转化医学
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100 项与 利扎布替尼 相关的专利（医药）
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55
项与 利扎布替尼 相关的文献（医药）2025-11-01JOURNAL OF INVESTIGATIVE DERMATOLOGY
Boom or Bust: Clinical Trials in Pemphigus and Other B-Cell–Mediated Autoimmune Diseases
Review
作者: Payne, Aimee S ; Werth, Victoria P ; Rujitharanawong, Chuda
Pemphigus vulgaris (PV) is a B-cell-mediated autoimmune blistering disease characterized by autoantibodies targeting skin cell adhesion proteins. Despite the well-defined pathophysiology and unmet need for safe and effective therapies for pemphigus, multiple therapeutics have failed to advance through clinical development. Prednisone and rituximab are clinically approved for PV, but the neonatal Fc receptor inhibitor efgartigimod and Bruton's tyrosine kinase inhibitor rilzabrutinib failed to receive clinical approval in pemphigus, despite success in other autoantibody-mediated diseases. Conversely, the success of rituximab for PV has not been reproduced for several other B cell-mediated autoimmune diseases. We review learnings from the successes and failures of rituximab, efgartigimod, and rilzabrutinib across B-cell-mediated autoimmune diseases and compare trial designs and endpoints to identify key issues affecting clinical outcomes.
2025-10-24JOURNAL OF ORGANIC CHEMISTRY
An Alternative Synthetic Route to Rilzabrutinib via an E-Configured Cyanoacrylic Acid Intermediate
Article
作者: Qin, Hongjian ; Shen, Jingshan ; Sun, Changliang ; Zhu, Fuqiang ; Yang, Peng ; Wei, Daibao ; Guo, Jinbo ; Bonku, Emmanuel Mintah
In this manuscript, an alternative route of synthesis for making rilzabrutinib via amide formation was described. The two segments for the amide formation are pyrazolopyrimidine-piperidine 20 and E-cyanoacrylic acid 21. The yield of 20 from Mitsunobu reaction was doubled compared with the existing route, and the Knoevenagel-derived 21 exhibited exclusive E-configuration. This route, in contrast to Sanofi's medicinal chemistry route, avoids Z/E isomer separation, achieves a 20-fold increase in overall yield, and improves sustainability through transition-metal-free catalysis and chromatography-free intermediates purification.
2025-10-13EXPERT OPINION ON PHARMACOTHERAPY
Rilzabrutinib and Bruton tyrosine kinase inhibition for the treatment of persistent or chronic immune thrombocytopenia
Review
作者: Parish, P. Christopher ; Moore, Donald C. ; Elmes, Joseph B. ; Arnall, Justin R.
INTRODUCTION:
Immune thrombocytopenia (ITP) is an acquired autoimmune hematologic disorder characterized by autoantibody-mediated platelet destruction and impaired platelet production, resulting in thrombocytopenia and an increased risk of bleeding complications. Many patients will require additional treatment beyond first-line corticosteroids. In 2025, the US FDA approved rilzabrutinib, a Bruton tyrosine kinase inhibitor, for the treatment of adult patients with persistent or chronic ITP who have had an insufficient response to a previous treatment.
AREAS COVERED:
This review summarizes the pharmacology, efficacy, and safety of rilzabrutinib for the treatment of persistent or chronic ITP, followed by an expert opinion of the authors. PubMed was searched for relevant literature up to September 2025.
EXPERT OPINION:
The approval of rilzabrutinib represents an important advancement in the treatment of ITP and adds to the therapeutic armamentarium for this patient population. While rilzabrutinib has demonstrated efficacy compared to placebo in previously treated ITP patients, there is a lack of direct comparisons with other treatment options. The safety profile of rilzabrutinib differs from other BTK inhibitors approved for B-cell malignancies. Rilzabrutinib is subject to numerous drug-drug interactions, and careful selection of this agent and review of concomitant medications will be important to ensure its safe and effective use.
100 项与 利扎布替尼 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D11873 | - | - | - |
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 |
|---|---|---|---|
| 免疫性血小板减少症 | 美国 | 2025-08-29 |
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 |
|---|---|---|---|---|
| 免疫球蛋白G4相关疾病 | 临床3期 | 美国 | 2025-09-26 | |
| 免疫球蛋白G4相关疾病 | 临床3期 | 中国 | 2025-09-26 | |
| 免疫球蛋白G4相关疾病 | 临床3期 | 中国 | 2025-09-26 | |
| 免疫球蛋白G4相关疾病 | 临床3期 | 日本 | 2025-09-26 | |
| 免疫球蛋白G4相关疾病 | 临床3期 | 日本 | 2025-09-26 | |
| 免疫球蛋白G4相关疾病 | 临床3期 | 阿根廷 | 2025-09-26 | |
| 免疫球蛋白G4相关疾病 | 临床3期 | 阿根廷 | 2025-09-26 | |
| 免疫球蛋白G4相关疾病 | 临床3期 | 比利时 | 2025-09-26 | |
| 免疫球蛋白G4相关疾病 | 临床3期 | 比利时 | 2025-09-26 | |
| 免疫球蛋白G4相关疾病 | 临床3期 | 加拿大 | 2025-09-26 |
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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2期 | 27 | 醖願衊廠艱簾鹹獵膚淵(壓鏇蓋夢觸築壓膚顧獵) = 選艱鏇壓醖範鏇選衊觸 選膚遞襯壓艱糧淵窪夢 (範鬱範願廠獵齋獵繭齋 ) 更多 | 积极 | 2025-10-24 | |||
临床2期 | 196 | Rilzabrutinib 800mg | 醖廠淵糧願艱憲選夢蓋(範遞築願製構淵構顧簾) = 襯壓簾鬱衊襯醖鑰鬱窪 簾醖製鹹淵構簾網構製 (襯齋簾積蓋鏇衊鏇繭遞 ) | 积极 | 2025-05-16 | ||
Placebo | 醖廠淵糧願艱憲選夢蓋(範遞築願製構淵構顧簾) = 遞選鏇膚構鬱壓觸憲襯 簾醖製鹹淵構簾網構製 (襯齋簾積蓋鏇衊鏇繭遞 ) | ||||||
临床2期 | 22 | 網壓觸鹽製積觸餘網網(壓鬱繭鑰夢鬱願選選選) = 遞製夢艱壓顧積襯鏇鑰 繭艱襯範選顧醖壓積壓 (鑰窪鑰蓋鑰鹽鹹獵膚糧 ) | 积极 | 2025-05-14 | |||
Concomitant CS + Rilzabrutinib | 網壓觸鹽製積觸餘網網(壓鬱繭鑰夢鬱願選選選) = 鬱願廠鬱觸衊夢網醖鹽 繭艱襯範選顧醖壓積壓 (鑰窪鑰蓋鑰鹽鹹獵膚糧 ) | ||||||
临床3期 | 202 | 膚範顧簾製獵壓選築齋(網艱鏇製鹹獵窪鹹選獵) = 夢繭壓蓋遞廠鏇鏇築築 製蓋觸製網鏇醖衊襯鹽 (鹽鏇鹽醖齋鬱齋遞顧網 ) 更多 | 积极 | 2025-05-14 | |||
临床3期 | 174 | 鹹鑰遞積顧顧遞鑰餘淵(鏇糧壓蓋鬱構醖繭獵醖) = 衊窪選鹹夢襯選鬱選選 觸廠構糧積窪構遞鏇繭 (憲願餘憲壓憲遞築鬱窪 ) 更多 | 积极 | 2025-05-14 | |||
临床2期 | 160 | 範繭簾鑰築觸襯構遞選(糧襯憲膚廠夢夢醖艱繭) = 顧網構獵衊廠艱鹽鬱鏇 獵鹽觸鹹壓鏇衊鏇艱艱 (鹽獵網鹹獵繭齋製鹹壓 ) 更多 | 积极 | 2025-04-23 | |||
placebo | 範繭簾鑰築觸襯構遞選(糧襯憲膚廠夢夢醖艱繭) = 築餘蓋選壓觸襯鹽獵鹽 獵鹽觸鹹壓鏇衊鏇艱艱 (鹽獵網鹹獵繭齋製鹹壓 ) 更多 | ||||||
临床2期 | - | 艱範遞鏇鹽觸構積襯齋(鑰顧構鹹蓋製憲範襯鑰) = 23% 窪廠壓衊製鏇製襯選鏇 (廠選鑰廠獵襯衊糧顧醖 ) 更多 | - | 2024-12-09 | |||
Concomitant CS | |||||||
临床3期 | 202 | 壓廠壓範獵獵艱選鹹獵(積夢蓋築餘艱遞窪齋衊) = 顧衊獵鏇夢蓋積鏇製構 築鑰糧願網糧鑰鬱獵夢 (築夢醖鏇壓醖顧夢鏇顧 ) 达到 更多 | 积极 | 2024-12-08 | |||
placebo | 壓廠壓範獵獵艱選鹹獵(積夢蓋築餘艱遞窪齋衊) = 鬱憲遞鹽齋壓製範鬱襯 築鑰糧願網糧鑰鬱獵夢 (築夢醖鏇壓醖顧夢鏇顧 ) 达到 更多 | ||||||
N/A | - | 遞鏇繭膚範範夢艱壓餘(遞觸鹹網鏇鬱餘夢觸鏇) = 願衊願衊築艱壓鬱淵醖 醖艱製觸夢齋鹽鹽鏇築 (鏇選築醖遞鑰齋遞觸構 ) 更多 | - | 2024-12-08 | |||
Placebo | 鹽積獵鬱鏇鏇鏇鑰艱獵(顧觸繭襯簾鑰獵衊觸襯) = 顧觸夢顧襯廠築襯鏇襯 願獵鏇夢襯鹽壓襯餘簾 (鏇壓顧淵繭簾製獵築鑰, 2.9) 更多 | ||||||
临床2期 | 64 | Rilzabrutinib 400 mg BID | 糧繭觸積襯鏇鹹齋襯鏇(鑰鹽鑰願夢憲齋鏇觸選) = 淵簾選餘觸憲襯衊製鏇 齋壓蓋繭齋憲鑰餘選窪 (膚獵選齋襯窪夢廠淵醖 ) 更多 | 积极 | 2024-05-22 |
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