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更新于：2025-03-24
Tirabrutinib Hydrochloride
替拉鲁替尼
更新于：2025-03-24
概要
基本信息
药物类型 小分子化药 |
别名 Tirabrutinib、Tirabrutinib hydrochloride (JAN)、Tirabutinib hydrochloride + [7] |
靶点 |
作用方式 抑制剂 |
作用机制 BTK抑制剂(酪氨酸蛋白激酶BTK抑制剂) |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 日本 (2020-03-25), |
最高研发阶段(中国)- |
特殊审评孤儿药 (美国)、孤儿药 (韩国) |
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结构/序列
分子式C25H23ClN6O3 |
InChIKeyUQYDCIJFACDXSG-GMUIIQOCSA-N |
CAS号1439901-97-9 |
关联
21
项与 替拉鲁替尼 相关的临床试验NCT06541665
A Multicenter, Phase I, Open-label, Uncontrolled Study of ONO-4059 in Combination With Rituximab, Methotrexate, Procarbazine, and Vincristine (R-MPV) Therapy for Untreated Primary Central Nervous System Lymphoma (PCNSL)
JPRN-jRCT2071230119
ONO-4059-14: relative bioavailability comparative studyOpen-label, randomized, 4-group 4-period cross-over, single-dose study to evaluate the relative bioavailability of the new high content formulation compared with the approved drug in Japanese healthy adult male subjects
JPRN-jRCT2031230277
Tirabrutinib maintenance versus placebo in patients with primary central nervous system lymphoma in complete remission: a randomized phase II study (JCOG2104)
100 项与 替拉鲁替尼 相关的临床结果
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100 项与 替拉鲁替尼 相关的转化医学
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100 项与 替拉鲁替尼 相关的专利（医药）
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161
项与 替拉鲁替尼 相关的文献（医药）2025-01-16Modern Rheumatology Case Reports
Isolated central nervous system lymphomatoid granulomatosis in an older adult patient with systematic lupus erythematosus: A case report
Article
作者: Kinashi, Hiroshi ; Yamaguchi, Makoto ; Ishimoto, Takuji ; Kamiya, Keisuke ; Kambe, Takayuki ; Sugiyama, Hirokazu ; Katsuno, Takayuki ; Banno, Shogo ; Imai, Kentaro ; Ito, Yasuhiko
ABSTRACT:
Lymphomatoid granulomatosis (LYG) is a rare, T-cell-rich Epstein–Barr virus (EBV)-positive B-cell lymphoproliferative systemic disease. Only a few cases of LYG have been described in patients with autoimmune disorders, with only one case described in a patient with systemic lupus erythematosus (SLE). However, no cases of isolated central nervous system (CNS)–LYG have been reported in patients with autoimmune diseases. Since isolated CNS involvement is rare, its clinicopathological features remain incompletely understood. Herein, we report about an 85-year-old Japanese woman who was diagnosed with SLE 26 years ago and was stable and maintained on prednisone (5 mg/day) for 20 years. Twenty-six days before admission, she developed cognitive dysfunction. Brain magnetic resonance imaging (MRI) revealed multiple nodular lesions with ring-like enhancements seen on gadolinium-enhanced T1-weighted imaging. A brain biopsy was performed on the right frontal lobe lesion. Pathological findings revealed T-cell infiltration surrounding the blood vessels with fibrin deposition, a few multinucleated cells, and large atypical cells with prominent nucleoli. Large atypical cells positive for CD20 and EBV-encoded RNA were seen at a density of >100 cells per high-power field. Based on laboratory testing, imaging, and pathology findings, the patient was diagnosed with Grade III LYG. Treatment with tirabrutinib (480 mg once daily) was started. The patient achieved clinical response to treatment, as evidenced by improved mental status. In patients with SLE who present with multiple nodular or ring-like lesions on brain MRI, a brain biopsy with histological diagnosis is crucial for the exclusion of CNS–LYG.
2024-12-31NMC case report journal
Lack of Apparent Neurotoxicity in Older Patients with Primary Central Nervous System Lymphoma Receiving Long-term Tirabrutinib: Report of 2 Cases
Article
作者: TAGUCHI, Akira ; YONEZAWA, Ushio ; KHAIRUNNISA, Novita I ; YAMASAKI, Fumiyuki ; ONISHI, Shumpei ; HORIE, Nobutaka ; OZONO, Iori
Older patients represent a unique and vulnerable subgroup, requiring careful consideration when determining treatment options. Treatment-related leukoencephalopathy is commonly observed in older patients months to years after receiving radiotherapy and/or methotrexate for primary central nervous system lymphoma (PCNSL). Tirabrutinib is an orally available, highly selective, and potent second-generation Bruton's tyrosine kinase inhibitor (BTKi) approved for treating recurrent/refractory PCNSL in Japan. However, limited studies evaluate the imaging findings in patients receiving tirabrutinib. In this study, we reported 2 cases of older patients with PCNSL who did not develop treatment-related neurotoxicity or leukoencephalopathy after long-term administration of tirabrutinib.
2024-10-01Current medicinal chemistry
The Pharmacokinetic Interaction of Tirabrutinib with Voriconazole,
Itraconazole, and Fluconazole in SD Rats by UPLC-MS/MS
Article
作者: Xia, Mengming ; Liu, Ya-Nan ; Dai, Gexin ; Chen, Jie ; Xu, Ren-Ai
Background::
Tirabrutinib is an orally effective, approved, and highly selective
second-generation Bruton's tyrosine kinase (BTK) inhibitor for the treatment of recurrent
or refractory primary central nervous system lymphoma (PCNSL).
Objective::
This study aimed to develop an ultra-high performance liquid chromatography-
tandem mass spectrometry (UPLC-MS/MS) method for the determination of tirabrutinib
concentration in rat plasma, where zanubrutinib was used as an internal standard
(IS). This method was also applied to study whether tirabrutinib would interact with voriconazole,
itraconazole, and fluconazole in rats, providing a reference value for clinical
medication guidance.
Methods::
In the current study, the organic solvent protein precipitation method was
used to treat plasma samples, which is simple and reproducible. Tirabrutinib (m/z 455.32
→ 320.21) and zanubrutinib (m/z 472.13 → 455.04) were separated on a Waters Acquity
BEH C18 column (2.1 × 50 mm, 1.7 μm) and detected by multiple reaction monitoring
(MRM) in positive ionization mode.
Results::
The method showed good linearity in the range of 5−3000 ng/mL for tirabrutinib
with the lower limit of quantification (LLOQ) of 5 ng/mL. The recovery and matrix
effects were 85.7-91.0% and 102.0-113.3%, respectively. The accuracy, precision, stability,
and carry-over effect were also acceptable. The method could also be used for determining
the pharmacokinetic interaction of tirabrutinib in rats. The results showed
AUC0→∞ of tirabrutinib to be increased by 139.3% and 83.9% in the presence of voriconazole
and fluconazole, respectively, while itraconazole had little effect.
Conclusion::
It is necessary to monitor the concentration of tirabrutinib in patients when
it is combined with voriconazole and fluconazole to achieve a better therapeutic effect
and reduce the risk of adverse reaction. Further research should be conducted in the future.
57
项与 替拉鲁替尼 相关的新闻（医药）2025-03-22
·同写意
抗体药物偶联物蛋白降解靶向嵌合体临床3期引进/卖出
2025-03-10
临床3期专利到期上市批准引进/卖出免疫疗法
2024-12-19
·贝壳社
临床2期上市批准引进/卖出临床申请
100 项与 替拉鲁替尼 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 |
|---|---|---|---|
| 巨球蛋白血症 | 日本 | 2020-08-21 | |
| 原发性中枢神经系统淋巴瘤 | 日本 | 2020-03-25 |
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 |
|---|---|---|---|---|
| 天疱疮 | 临床3期 | 日本 | 2022-08-15 | |
| 难治性中枢神经系统淋巴瘤 | 临床2期 | 美国 | 2021-12-29 | |
| 慢性荨麻疹 | 临床2期 | - | 2021-07-01 | |
| 干燥综合征 | 临床2期 | 美国 | 2017-05-01 | |
| 干燥综合征 | 临床2期 | 波兰 | 2017-05-01 | |
| 干燥综合征 | 临床2期 | 西班牙 | 2017-05-01 | |
| 干燥综合征 | 临床2期 | 英国 | 2017-05-01 | |
| 慢性淋巴细胞白血病 | 临床2期 | 德国 | 2016-12-13 | |
| B细胞淋巴瘤 | 临床1期 | 美国 | 2015-06-16 | |
| B细胞淋巴瘤 | 临床1期 | 法国 | 2015-06-16 |
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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 | - | 簾鏇窪糧艱鹹襯範鏇鏇(襯夢顧構鬱製齋壓遞鹽) = 1 patient without antiviral agent prophylaxis 遞膚簾繭獵鏇構鹽觸夢 (繭憲憲選鹹築積蓋範網 ) 更多 | - | 2024-12-09 | |||
N/A | - | 糧範觸餘構願顧壓夢鹹(鏇鏇夢艱醖膚網遞淵顧) = TRAEs of any grade were observed in 92 (57.1%) patients 獵壓淵餘襯憲鑰鹽艱製 (廠鏇壓衊齋鬱鏇繭構遞 ) 更多 | - | 2024-12-08 | |||
N/A | - | (Recurrent PCNSL patients) | 鬱襯鹽鹽淵齋窪鏇糧顧(夢築遞艱鑰壓網選願鏇) = 選餘餘選製築獵構選獵 淵齋廠遞糧窪襯鑰願糧 (築襯餘壓構獵夢餘餘憲 ) 更多 | 积极 | 2024-11-11 | ||
(Refractory PCNSL patients) | 鬱襯鹽鹽淵齋窪鏇糧顧(夢築遞艱鑰壓網選願鏇) = 顧積選觸蓋壓範構醖顧 淵齋廠遞糧窪襯鑰願糧 (築襯餘壓構獵夢餘餘憲 ) 更多 | ||||||
临床1/2期 | 44 | 網鬱鹹網鬱鑰艱廠築壓(齋築膚選鬱鹽衊淵鑰壓) = 製餘願積鏇簾觸衊遞鏇 蓋鹽醖鑰鹽淵網鏇願鬱 (夢選鹹網顧衊膚鬱醖簾 ) 更多 | - | 2023-12-11 | |||
網鬱鹹網鬱鑰艱廠築壓(齋築膚選鬱鹽衊淵鑰壓) = 簾廠網夢膚齋選鹽醖繭 蓋鹽醖鑰鹽淵網鏇願鬱 (夢選鹹網顧衊膚鬱醖簾 ) 更多 | |||||||
临床1/2期 | 44 | (320 mg QD) | 鹽衊衊鹽艱顧鹽廠鹽鬱(鏇選淵齋蓋網衊構醖廠) = 積膚憲繭糧選窪憲餘構 願襯鑰觸鹹鹹壓觸餘憲 (構積衊糧製鏇鏇蓋鹽膚, 36.1 ~ 80.9) 更多 | 积极 | 2023-05-31 | ||
(480 mg QD) | 鹽衊衊鹽艱顧鹽廠鹽鬱(鏇選淵齋蓋網衊構醖廠) = 鬱餘壓願蓋簾範蓋獵選 願襯鑰觸鹹鹹壓觸餘憲 (構積衊糧製鏇鏇蓋鹽膚, 59.0 ~ 100.0) 更多 | ||||||
临床1/2期 | 复发性中枢神经系统淋巴瘤 Bruton’s tyrosine kinase (BTK) | - | 蓋憲簾繭淵廠齋鑰顧選(遞構築膚壓顧鬱積選鹽) = 膚遞願範襯觸積廠餘膚 鬱醖壓壓製襯憲範願廠 (鬱糧鑰製蓋夢繭網壓鑰 ) 更多 | 积极 | 2021-11-12 | ||
临床1期 | 42 | (Cohort 1, Part A: Tirabrutinib 20 mg QD) | 願窪齋簾齋製壓憲齋選 = 鹹餘顧網鏇壓鑰醖壓繭 夢構觸簾憲淵齋鑰築簾 (遞築餘廠選壓鏇窪廠餘, 願構蓋構夢夢願鏇鏇衊 ~ 範簾構製製淵獵遞窪鏇) 更多 | - | 2020-09-09 | ||
Placebo (Cohort 1, Part A: Placebo) | 願窪齋簾齋製壓憲齋選 = 觸鏇餘簾壓鏇齋齋願鬱 夢構觸簾憲淵齋鑰築簾 (遞築餘廠選壓鏇窪廠餘, 齋蓋糧醖築願鬱構襯蓋 ~ 襯醖夢窪選醖壓選鹽壓) 更多 | ||||||
临床2期 | 35 | (Tirabrutinib + Idelalisib) | 艱廠網範夢艱廠築廠夢 = 襯鹹網網淵鏇糧構獵糧 選餘簾繭範醖選襯憲遞 (壓餘艱廠鹽糧蓋製餘願, 鑰遞鑰餘範膚窪餘築憲 ~ 窪艱網鏇襯選鹽繭鹹壓) 更多 | - | 2020-07-01 | ||
(Tirabrutinib + Idelalisib + Obinutuzumab) | 艱廠網範夢艱廠築廠夢 = 艱願窪選繭壓夢淵鏇鬱 選餘簾繭範醖選襯憲遞 (壓餘艱廠鹽糧蓋製餘願, 襯鏇獵餘築蓋遞網簾壓 ~ 艱願膚觸網鑰鏇願觸簾) 更多 | ||||||
临床1期 | 53 | 夢鏇壓鹽築襯範範衊遞(鑰顧淵鹹鹹淵蓋餘夢觸) = 築築簾築顧鏇鹽繭繭鏇 獵繭積衊糧齋鏇醖糧鹹 (製積餘廠鹹鬱選壓積蓋 ) 更多 | - | 2020-06-15 | |||
夢鏇壓鹽築襯範範衊遞(鑰顧淵鹹鹹淵蓋餘夢觸) = 繭襯鹹憲蓋襯淵構淵糧 獵繭積衊糧齋鏇醖糧鹹 (製積餘廠鹹鬱選壓積蓋 ) 更多 | |||||||
临床2期 | 36 | (Tirabrutinib + Entospletinib) | 壓餘製襯鏇願簾淵蓋築 = 憲簾憲衊蓋壓糧遞觸鹹 選構鏇鹽糧蓋鬱鬱淵選 (衊壓艱艱選遞繭鑰鹹構, 範鹽簾壓鏇膚窪選鑰淵 ~ 齋遞築淵範艱艱願繭顧) 更多 | - | 2020-02-28 | ||
(Tirabrutinib + Entospletinib + Obinutuzumab) | 壓餘製襯鏇願簾淵蓋築 = 衊艱顧餘簾鑰鑰夢糧窪 選構鏇鹽糧蓋鬱鬱淵選 (衊壓艱艱選遞繭鑰鹹構, 窪鑰鹹鏇鑰繭繭蓋構繭 ~ 鏇顧餘襯願獵鹽鏇膚願) 更多 |
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