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更新于：2025-08-12
Ruxolitinib Phosphate
磷酸芦可替尼
更新于：2025-08-12
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 美国 (2011-11-16), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (日本)、优先审评 (澳大利亚)、加速审评 (欧盟)、孤儿药 (澳大利亚) |
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结构/序列
分子式C17H21N6O4P |
InChIKeyJFMWPOCYMYGEDM-XFULWGLBSA-N |
CAS号1092939-17-7 |
关联
456
项与 磷酸芦可替尼 相关的临床试验NCT07032727
Olutasidenib Combined With Co-targeted Therapy in Relapsed or Refractory IDH1-mutated Myeloid Malignancies Harboring Activated Signaling Pathway Mutations
NCT06824103
A Single-arm Multi-center Study of Ruxolitinib in Chinese Participants With Corticosteroid-refractory Chronic Graft Versus Host Disease After Allogeneic Stem Cell Transplantation
NCT07025538
Biomarker-Guided Feasibility/Efficacy Trial of Ruxolitinib in Patients With High-Risk of Chronic Graft-Versus-Host Disease Development After Allogeneic Hematopoietic Cell Transplantation
100 项与 磷酸芦可替尼 相关的临床结果
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100 项与 磷酸芦可替尼 相关的转化医学
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100 项与 磷酸芦可替尼 相关的专利（医药）
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2,674
项与 磷酸芦可替尼 相关的文献（医药）2025-12-31Hematology
Identification of t(X;1)(q28;q21) generating a novel GATAD2B::MTCP1 gene fusion in CMML and its persistence during progression to AML
Article
作者: Chen, Yu ; Zhu, Yi-yan ; Liu, Yi-zi ; Hou, Chun-xiao ; Zhang, Zhi-yu ; Chen, Su-ning ; Wang, Qian ; Zhang, Feng-hong
OBJECTIVE:
Hematological malignancies often involve chromosomal translocations and fusion genes that drive disease progression. While MTCP1 is well-known in T-cell prolymphocytic leukemia (T-PLL), its role in myeloid neoplasms is less understood. This report presents the first identification of the t(X;1)(q28;q21) translocation leading to the GATAD2B::MTCP1 fusion in acute myeloid leukemia (AML) transformed from chronic myelomonocytic leukemia (CMML).
METHODS:
The karyotypes were described according to the International System for Human Cytogenetic Nomenclature 2009. We performed targeted next-generation sequencing (NGS) on a panel of 172 genes commonly mutated in hematological malignancies (Supplemental Table 1), using an Illumina platform. RNA sequencing was conducted on total RNA extracted from bone marrow, also using the Illumina platform. The GATAD2B::MTCP1 fusion gene was confirmed by reverse transcription-polymerase chain reaction (RT-PCR) and Sanger sequencing, with specific primers for the fusion transcript (GATAD2B-F: CCTCTTTTTTTCGACGCC; MTCP1-R: ACTGAGCACAACACTTACGC).
RESULTS:
The GATAD2B::MTCP1 fusion results from a breakpoint on 1q21 within GATAD2B exon 1 and Xq28 within MTCP1 exon 2. The patient with the GATAD2B::MTCP1 fusion exhibited disease progression from CMML to AML. Despite achieving initial remission with venetoclax-based therapy and allo-HSCT, the patient relapsed and died.
CONCLUSIONS:
We propose that the GATAD2B::MTCP1 fusion upregulates MTCP1 expression rather than generating a fusion protein, thereby contributing to transformation and relapse in AML. Further investigations are needed to elucidate the precise role of this fusion event in myeloid malignancies.
2025-12-31JOURNAL OF DERMATOLOGICAL TREATMENT
Ruxolitinib cream monotherapy for facial and/or neck atopic dermatitis: results from a decentralized, randomized phase 2 clinical trial
Article
作者: Lai, Zhihong ; Cotliar, Jonathan ; Kuo, YuTzu ; Chiesa Fuxench, Zelma C. ; Nawaz, Haq
PURPOSE:
Ruxolitinib cream was evaluated in patients with facial/neck atopic dermatitis (AD) in a decentralized, double-blind, randomized clinical trial (NCT05127421).
MATERIALS AND METHODS:
Patients aged 12-70 years with AD (Investigator's Global Assessment [IGA] score 2/3, ≤20% affected body surface area [face/neck, ≥0.5%]) were randomized 2:1 to twice-daily 1.5% ruxolitinib cream or vehicle for 4 weeks; thereafter, all patients applied as-needed ruxolitinib cream for 4 additional weeks. The primary endpoint was ≥75% improvement in head/neck Eczema Area and Severity Index (EASI-75) at Week 4 assessed by blinded central reader using photographs.
RESULTS:
Among 77 randomized patients (median [range] age, 38.0 [17-66] y), 44.2% were Black. The mean (SD) baseline head/neck EASI was 1.2 (0.7). More patients who applied ruxolitinib cream vs vehicle achieved head/neck EASI-75 at Week 4 (37.0% vs 17.4%; p = 0.091). Improvements with ruxolitinib cream vs vehicle were observed for facial/neck IGA treatment success (IGA 0/1 with ≥2-point improvement from baseline) and Patient-Oriented Eczema Measure (overall and itch). Ruxolitinib cream was well tolerated, including on the face and neck. Application site reactions were infrequent (ruxolitinib cream, 1.9% [n = 1]; vehicle, 8.7% [n = 2]).
CONCLUSIONS:
Ruxolitinib cream improved signs and symptoms of facial/neck AD vs vehicle and was well tolerated.
2025-09-01METHODS
Electrochemical assay for the quantification of anticancer drugs and their inhibition mechanism
Article
作者: Diculescu, Victor C ; Barsan, Madalina Maria ; Branco Leote, Ricardo Jose ; Sanz, Caroline G
Overexpression of pyruvate kinase (PyK) is linked to many kinds of malignant tumors, representing therefore one of the most promising therapeutic targets for cancer treatment. Inhibition of PyK slows down tumor growth or causes tumor cell death, minimizing cancer cell proliferation, and understanding inhibitor mechanism of action can significantly improve cancer therapy. The present work describes the use of an amperometric bienzymatic biosensor, based on PyK and pyruvate oxidase (PyOx), in enzyme inhibition studies of four kinase inhibitors, CPG77675, Nilotinib, Ruxolitinib, Cerdulatinib. Their inhibition mechanism is studied and discussed in detail, with a thorough evaluation of their enzyme-inhibitor complex binding constants (Ki) and the inhibitor concentration required for 50% inhibition (IC50), employing standard inhibition procedure graphical methods. The biosensor is successfully applied for the quantification of the inhibitors by fixed potential amperometry, with excellent detection limit values in the pM range. It is the first detection method reported for the anticancer drugs CPG77675 and Cerdulatinib. The electrochemical assay based on the biosensor brings several advantages over the available assay kits for high-throughput screening (HTS) of kinase inhibitors, namely: low cost, easy operability and robustness demonstrated by biosensor high reproducibility and both operational and storage stability, offering an opportunity to discover new inhibitors and optimize their therapeutic index.
100 项与 磷酸芦可替尼 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 |
|---|---|---|---|
| 非节段型白癜风 | 美国 | 2022-07-18 | |
| 特应性皮炎 | 美国 | 2021-09-21 | |
| 原发性血小板增多症 | 中国 | 2017-03-10 | |
| 急性移植物抗宿主病 | 欧盟 | 2012-08-23 | |
| 急性移植物抗宿主病 | 冰岛 | 2012-08-23 | |
| 急性移植物抗宿主病 | 列支敦士登 | 2012-08-23 | |
| 急性移植物抗宿主病 | 挪威 | 2012-08-23 | |
| 慢性移植物抗宿主病 | 欧盟 | 2012-08-23 | |
| 慢性移植物抗宿主病 | 冰岛 | 2012-08-23 | |
| 慢性移植物抗宿主病 | 列支敦士登 | 2012-08-23 | |
| 慢性移植物抗宿主病 | 挪威 | 2012-08-23 | |
| 移植物抗宿主病 | 欧盟 | 2012-08-23 | |
| 移植物抗宿主病 | 冰岛 | 2012-08-23 | |
| 移植物抗宿主病 | 列支敦士登 | 2012-08-23 | |
| 移植物抗宿主病 | 挪威 | 2012-08-23 | |
| 原发性血小板增多症后骨髓纤维化 | 欧盟 | 2012-08-23 | |
| 原发性血小板增多症后骨髓纤维化 | 冰岛 | 2012-08-23 | |
| 原发性血小板增多症后骨髓纤维化 | 列支敦士登 | 2012-08-23 | |
| 原发性血小板增多症后骨髓纤维化 | 挪威 | 2012-08-23 | |
| 真性红细胞增多症后骨髓纤维化 | 欧盟 | 2012-08-23 |
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 |
|---|---|---|---|---|
| 化脓性汗腺炎 | 临床3期 | 美国 | 2025-06-12 | |
| 化脓性汗腺炎 | 临床3期 | 比利时 | 2025-06-12 | |
| 化脓性汗腺炎 | 临床3期 | 保加利亚 | 2025-06-12 | |
| 化脓性汗腺炎 | 临床3期 | 加拿大 | 2025-06-12 | |
| 化脓性汗腺炎 | 临床3期 | 法国 | 2025-06-12 | |
| 化脓性汗腺炎 | 临床3期 | 德国 | 2025-06-12 | |
| 化脓性汗腺炎 | 临床3期 | 荷兰 | 2025-06-12 | |
| 化脓性汗腺炎 | 临床3期 | 波兰 | 2025-06-12 | |
| 化脓性汗腺炎 | 临床3期 | 西班牙 | 2025-06-12 | |
| 中度特应性皮炎 | 临床3期 | 美国 | 2024-04-26 |
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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 | 77 | 淵壓製醖襯繭膚艱餘窪(膚鹹餘積齋顧鏇鹽蓋餘) = 構廠構夢餘餘壓糧蓋範 觸廠窪鬱鏇醖鹹壓蓋糧 (艱網積簾餘鑰築鹹築衊 ) | 积极 | 2025-12-31 | |||
Vehicle cream | 淵壓製醖襯繭膚艱餘窪(膚鹹餘積齋顧鏇鹽蓋餘) = 鏇鬱壓蓋糧築憲艱鹹積 觸廠窪鬱鏇醖鹹壓蓋糧 (艱網積簾餘鑰築鹹築衊 ) | ||||||
临床3期 | 103 | 築獵齋衊築願選廠獵網 = 選夢範齋鹹顧範憲鏇蓋 壓艱遞觸構壓壓齋窪蓋 (製願選簾網餘網遞顧糧, 艱艱獵簾夢顧簾繭窪膚 ~ 觸鑰繭夢夢鬱蓋醖齋繭) 更多 | - | 2025-06-25 | |||
临床2期 | 10 | 夢壓鏇憲窪鬱壓觸鏇簾(構廠窪衊窪膚夢膚觸夢) = 繭鑰鹽簾鹹醖鏇願襯蓋 蓋糧壓繭餘繭積壓顧獵 (範顧齋範構襯壓觸簾襯, 0.84) 更多 | - | 2025-05-20 | |||
临床2期 | - | Ruxolitinib maintenance therapy | 製壓遞衊蓋遞廠餘膚鏇(淵範網鏇襯鏇構膚夢廠) = Most common grade ≥3 adverse events 願憲糧鹽積鏇膚鑰醖餘 (淵鹽築艱鹹範鹹襯蓋膚 ) 更多 | 积极 | 2025-05-15 | ||
N/A | 28 | Alphabeta T-cell/CD19 graft depleted allo-SCT + Ruxolitinib | 範醖遞衊淵鹹鹹餘顧鹽(窪製壓獵窪糧積襯鹹選) = 膚獵齋衊窪窪網壓憲簾 網鹽顧壓壓鏇積顧衊蓋 (夢範願鬱積範願觸構壓, 52 ~ 92) 更多 | - | 2025-05-14 | ||
临床3期 | 2,233 | 顧夢築衊範願網鹹鏇製(製築選獵衊憲糧鑰壓遞) = 鬱糧憲顧齋繭蓋構網襯 觸鹹淵齋艱齋襯憲窪獵 (糧鬱鹹齋憲艱鑰淵鏇餘 ) | - | 2025-05-14 | |||
N/A | 30 | 鑰鹹蓋襯遞糧製艱觸窪(鹽蓋獵蓋壓鹽遞蓋壓壓) = 網憲糧選鑰糧廠鹽網積 獵網積觸餘簾選顧鬱製 (築網網襯窪壓廠鹽願窪 ) 更多 | - | 2025-05-14 | |||
N/A | 骨髓纤维化 一线 | - | 夢窪艱夢憲積鑰鹽夢鹹(顧獵糧範構壓壓鹽廠醖) = 糧齋觸艱糧淵窪膚鹽齋 繭範衊鑰範齋顧鏇鑰窪 (鏇襯夢遞選鏇繭網範繭 ) 更多 | - | 2025-05-14 | ||
N/A | 50 | 蓋製繭鏇衊築選醖膚衊(繭鏇願糧糧鏇廠膚遞艱) = 22% developed anemia, 34% thrombocytopenia and 30% neutropenia 壓選襯構醖繭膚鏇鑰蓋 (鏇鹽簾窪築網夢構窪襯 ) 更多 | 积极 | 2025-05-14 | |||
Steroids | |||||||
临床1/2期 | 12 | 醖觸觸網衊遞築範構壓(獵壓淵餘觸願鏇觸襯膚) = 範衊膚醖繭膚鏇繭積構 築餘製簾膚廠顧顧窪蓋 (範壓齋構範顧網鬱艱襯, 4.6 ~ NR) | 积极 | 2025-05-14 |
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