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更新于：2026-05-07
Olverembatinib
奥雷巴替尼
更新于：2026-05-07
概要
基本信息
药物类型 小分子化药 |
别名 Orebatinib、Oribatinib、奥瑞巴替尼 + [15] |
作用方式 抑制剂 |
作用机制 Bcr-Abl T315I抑制剂(bcr-abl酪氨酸激酶T315I抑制剂)、c-Kit抑制剂(干细胞生长因子受体抑制剂) |
在研适应症 |
非在研适应症- |
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 中国 (2021-11-24), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟)、优先审评 (中国)、突破性疗法 (中国)、附条件批准 (中国)、快速通道 (美国) |
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结构/序列
分子式C31H35F3N6O7S2 |
InChIKeyLEVIGHXVOVROGW-UHFFFAOYSA-N |
CAS号1421783-64-3 |
关联
47
项与 奥雷巴替尼 相关的临床试验NCT07178912
Phase II Study of the Combination of Subcutaneous Blinatumomab and Olverembatinib in Patients With Philadelphia Chromosome (ph)-Positive and/or BCR::ABL1 Positive Acute Lymphoblastic Leukemia (ALL)
NCT07454226
An Open-Label, Single-Arm, Phase II Exploratory Study of ABL and JAK Kinase Inhibitors With Chemotherapy and Venetoclax in Adult Patients With Ph-like ALL
NCT07493161
Low-intensity Chemotherapy Combined With Targeted-Immunotherapy for Newly Diagnosed Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia: A Prospective Clinical Cohort Study
100 项与 奥雷巴替尼 相关的临床结果
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100 项与 奥雷巴替尼 相关的转化医学
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100 项与 奥雷巴替尼 相关的专利（医药）
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104
项与 奥雷巴替尼 相关的文献（医药）2026-06-01TRANSPLANT IMMUNOLOGY
T315I-mutated chronic myeloid leukemia with blast crisis relapse 10 years after allo-HSCT: A case report of second transplantation combined with olverembatinib maintenance therapy
Article
作者: Ji, JiaJuan ; Fan, ShengJin ; Zhu, YuTing ; Zhao, YanQiu ; Ding, PeiWen ; Luo, Dan ; Guo, Dan ; Liu, Jie
Chronic myeloid leukemia (CML) is a myeloproliferative neoplasm characterized by the presence of the Philadelphia chromosome and the resulting fusion proteins with abnormal tyrosine kinase activity. The treatment of CML includes allogeneic hematopoietic stem cell transplantation (allo-HSCT) and TKI drug therapy. The BCR::ABL1 T315I mutation in CML leads to resistance to first- and second-generation tyrosine kinase inhibitors (TKIs), but is sensitive to two third-generation TKIs, olverembatinib and ponatinib. Olverembatinib, an oral third-generation BCR::ABL1 TKI, has preclinical activity against T315I-mutated CML. Here, we present a case of a CML patient with the T315I mutation who experienced late relapse with blast crisis 10 years after allo-HSCT. Following hematologic recovery and achievement of major molecular response (MMR) through induction therapy, the patient underwent a second allo-HSCT from his haploidentical sister. After successful engraftment, the patient received regular consolidation maintenance therapy with olverembatinib.
2026-04-01JOURNAL OF BIOLOGICAL CHEMISTRY
Pharmacological targeting of the mycothiol cysteine ligase MshC in Mycobacterium abscessus
Article
作者: Liu, Yi ; Giannini, Greta Carola ; Nguyen, Thanh Quang ; Larrouy-Maumus, Gerald ; Kremer, Laurent ; Hamela, Claire ; Boeck, Lucas ; Pang, Luping
The prevalence of pulmonary diseases caused by Mycobacterium abscessus is on the rise and surpasses tuberculosis in many countries. However, intrinsic resistance of this pathogen to antibiotics profoundly limits our therapeutic arsenal, and new chemotherapeutic agents and targets are urgently needed. Mycothiol (MSH), the major thiol in mycobacteria, plays an important role in resistance to oxidative stress. Previous work in Mycobacterium smegmatis and Mycobacterium tuberculosis indicates that the ATP-dependent cysteine ligase MshC catalyzes the penultimate step in MSH biogenesis. Here, we investigated whether MshC represents a potent drug target in M. abscessus. CRISPRi was used to demonstrate that mshC is essential in vitro and during infection in zebrafish larvae. Subsequently, in silico drug screening identified three potential MshC-binding molecules, namely rebastinib, olverembatinib and SB-224289, significantly inhibiting M. abscessus growth and MSH production. Spontaneous missense mutations in MshC generated cross-resistance to all three compounds. Mapping the mutations conferring resistance on a MshC three-dimensional homology model defined the enzyme catalytic site as the potential drug binding cavity. Additionally, overexpression of mshC in a susceptible M. abscessus strain increased resistance levels to rebastinib, olverembatinib and SB-224289, but not to rifabutin. Conversely, reduced mshC expression levels in the CRISPRi mutant increased susceptibility to the inhibitors. Systematic assessment of olverembatinib and SB-224289 in combination with 18 additional drugs revealed distinct synergistic and antagonistic interactions. These results emphasize a yet unexploited chemical structure classes against M. abscessus and highlights the potential of targeting the MSH pathway for future translational developments against M. abscessus lung diseases.
2026-02-01EXPERIMENTAL CELL RESEARCH
Overcoming multidrug resistance in cancer cells targeting ABC transporter ABCB1 with tyrosine kinase inhibitor: Olverembatinib
Article
作者: Bo, Letao ; Dong, Xingduo ; Wang, Shanzhi ; Li, Yidong ; Chen, Xiang ; Chou, Brian ; Patel, Harsh ; Zhang, Bohan ; Chen, Zhe-Sheng
The overexpression of ATP-binding cassette subfamily B member 1 (ABCB1) remains a primary challenge in overcoming multidrug resistance (MDR) in cancer cells. This study investigates the potential of olverembatinib, a third-generation tyrosine kinase inhibitor (TKI), to reverse ABCB1-mediated MDR and enhance the efficacy of chemotherapeutic drugs. Non-cytotoxic concentrations of olverembatinib significantly increased the sensitivity of ABCB1-overexpressing cells to paclitaxel and vincristine. Mechanistic analyses revealed that olverembatinib did not alter the expression or localization of ABCB1 but inhibited its drug efflux function, resulting in increased intracellular drug retention. Additionally, olverembatinib activated the ATPase activity of ABCB1 in a concentration-dependent manner and exhibited potent binding affinity to ABCB1 in docking simulations. These findings suggest that olverembatinib holds promise as a potent reversal agent for MDR, paving the way for its integration into novel combination chemotherapy regimens to improve cancer treatment outcomes.
100 项与 奥雷巴替尼 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
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 |
|---|---|---|---|
| 加速期慢性骨髄性白血病 | 中国 | 2021-11-24 | |
| 慢性期慢性髓性白血病 | 中国 | 2021-11-24 |
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 |
|---|---|---|---|---|
| 琥珀酸脱氢酶缺陷型胃肠道间质瘤 | 临床3期 | 中国 | 2024-11-11 | |
| 琥珀酸脱氢酶缺陷型胃肠道间质瘤 | 临床3期 | 中国 | 2024-11-11 | |
| 费城染色体阳性慢性粒细胞白血病 | 临床3期 | 美国 | 2024-02-05 | |
| 费城染色体阳性成人前体急性淋巴细胞白血病 | 临床3期 | 美国 | 2023-08-31 | |
| 费城染色体阳性成人前体急性淋巴细胞白血病 | 临床3期 | 中国 | 2023-08-31 | |
| 费城染色体阳性成人前体急性淋巴细胞白血病 | 临床3期 | 澳大利亚 | 2023-08-31 | |
| 费城染色体阳性成人前体急性淋巴细胞白血病 | 临床3期 | 捷克 | 2023-08-31 | |
| 费城染色体阳性成人前体急性淋巴细胞白血病 | 临床3期 | 法国 | 2023-08-31 | |
| 费城染色体阳性成人前体急性淋巴细胞白血病 | 临床3期 | 意大利 | 2023-08-31 | |
| 费城染色体阳性成人前体急性淋巴细胞白血病 | 临床3期 | 罗马尼亚 | 2023-08-31 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 63 | 膚製獵壓淵獵鏇製淵範(窪糧廠遞壓蓋窪範膚構) = 窪鑰網餘餘憲衊積鑰衊 構鏇醖艱鑰壓鏇製淵糧 (窪襯衊醖憲觸餘襯襯餘 ) 更多 | 积极 | 2025-12-06 | |||
original TKI therapy | 膚製獵壓淵獵鏇製淵範(窪糧廠遞壓蓋窪範膚構) = 顧構製壓積鹽構蓋範夢 構鏇醖艱鑰壓鏇製淵糧 (窪襯衊醖憲觸餘襯襯餘 ) 更多 | ||||||
N/A | 64 | 鑰醖衊膚簾艱繭蓋糧鑰(鏇艱獵簾觸鹽觸願簾網) = Treatment-related adverse events in olverembatinib cohort 52.4% (11/21) of patients. Six (28.6%) developed grade 3/4 neutropenia. Cardiovascular Events were observed in two patients, including deep vein thrombosis (n=1) and pericardial effusion (n=1). 齋襯簾衊醖膚鏇糧鏇襯 (鹽網願襯網醖淵築齋觸 ) 更多 | 积极 | 2025-12-06 | |||
1/2G-TKI | |||||||
N/A | 167 | Olverembatinib therapy | 鏇糧觸壓鹽醖積齋鬱壓(窪網襯鬱糧積齋顧顧鏇) = 鏇憲製襯襯繭獵廠鏇構 簾鬱餘鬱製淵壓構醖糧 (繭餘餘鬱繭鏇憲蓋艱繭 ) 更多 | 积极 | 2025-12-06 | ||
临床1期 | 琥珀酸脱氢酶缺陷型胃肠道间质瘤 SDH deficient | 66 | (TKI-failed, evaluable) | 膚選顧積醖窪鑰構網餘(膚衊簾膚遞鹹醖鹹齋醖) = 構鹹觸簾鏇糧壓壓繭蓋 選願鑰簾鹹鑰憲餘餘築 (網衊鏇襯簾衊餘夢範範, 9 ~ 43.7) 更多 | 积极 | 2025-11-04 | |
临床2期 | 79 | 糧糧衊鹹遞積淵鏇鏇構(鑰壓糧範願顧鏇網選艱) = 糧繭衊窪襯範鏇願壓廠 鏇製鬱觸製憲繭構構獵 (鑰鹹獵積範範觸鏇鏇艱 ) 更多 | 积极 | 2025-08-01 | |||
PS1367 (EHA2025) 人工标引  | N/A | 24 | olverembatinib(40mg once every other day) in combination with blinatumomabolverembatinib(40mg once every other day) in combination with blinatumomab | 網製鹽餘膚餘築餘築獵(齋餘遞廠艱淵糧構築築) = achieved in 17 patients who adhered to the treatment within the first 3 months of the treatment course 製壓衊製簾淵觸簾壓鑰 (選積積鏇蓋夢夢顧顧齋 ) | 积极 | 2025-06-14 | |
临床2期 | 13 | (chronic-phase) | 鑰願構艱鏇鑰網窪艱膚(廠廠製範鹹遞顧築鏇構) = 餘淵鏇積鏇繭鹽鹹構鏇 鑰簾選艱顧選廠憲夢醖 (糧艱觸簾鹽繭製襯鑰壓 ) | 积极 | 2025-06-13 | ||
(blast-phase) | 蓋憲簾夢壓鏇夢餘獵齋(憲齋製選壓範鹽膚鏇壓) = 淵齋淵夢網簾廠積鬱觸 糧鏇獵廠壓簾鏇獵鏇齋 (願蓋夢積獵艱獵糧鑰鹽 ) | ||||||
NEWS | Pubmed 人工标引 | N/A | 282 | 壓鹽廠積鏇鑰膚範艱壓(選齋鑰淵簾夢蓋鏇窪願) = 两个起始剂量组在CHR(血液学反应)、PCyR/CCyR(细胞遗传学反应)、MMR/MR4(分子学反应)，以及PFS(无进展生存)和OS(总生存)方面均无显著差异(p值均>0.2)。 艱壓鏇網憲鑰簾繭餘齋 (構憲壓廠網範膚艱廠糧 ) 更多 | 积极 | 2025-05-18 | ||
临床2期 | 17 | 製衊鬱鹹襯醖構製鏇醖(觸膚築蓋選製積衊鑰鏇) = 蓋選襯齋顧觸膚膚窪壓 簾築網遞網顧艱鑰衊製 (艱觸構齋繭網鬱遞糧構 ) | 积极 | 2025-05-14 | |||
N/A | 30 | 窪積範衊顧鏇構鏇築餘(構鑰艱鹽構繭壓範鑰膚) = 獵鹽襯鏇鑰願繭選廠窪 鹹廠醖鹽範鹽蓋蓋願蓋 (夢製範憲範艱積繭壓醖 ) 更多 | 积极 | 2025-05-14 |
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