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更新于：2026-08-23
Nilotinib Hydrochloride
尼洛替尼
更新于：2026-08-23
概要
基本信息
药物类型 小分子化药 |
别名 Nilotinib、nilotinib D-tartrate、Nilotinib Hydrochloride Hydrate + [18] |
作用方式 拮抗剂、抑制剂 |
作用机制 CSF-1R拮抗剂(集落刺激因子1受体拮抗剂)、DDR1拮抗剂(盘状结构域受体-1拮抗剂)、c-Kit抑制剂(干细胞生长因子受体抑制剂) |
非在研适应症 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 瑞士 (2007-07-24), |
最高研发阶段(中国)批准上市 |
特殊审评加速批准 (美国)、孤儿药 (美国)、孤儿药 (日本) |
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结构/序列
分子式C28H25ClF3N7O2 |
InChIKeyYCBPQSYLYYBPDW-UHFFFAOYSA-N |
CAS号923288-90-8 |
关联
239
项与 尼洛替尼 相关的临床试验CTRI/2026/07/114106
A Phase I, Randomized, Double-Blind, Placebo-Controlled, Single and Multiple Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of the Combination of Nilotinib, Marimastat, and Varespladib in Healthy Adult Volunteers - NIL
CTRI/2026/06/113049
Single dose oral relative bioavailability study of DanzitenTM (nilotinib) tablets 95 mg (Dose: 2 Tablets 95 mg. 190 mg) of Azurity Pharmaceuticals, Inc., USA versus Tasigna (nilotinib) hard capsules 200 mg (Dose: 2 Capsules 200 mg. 400 mg) of Novartis Europharma Limited, Ireland in healthy, adult, human trial participants under fed and modified fasting conditions. - Nil
CTRI/2026/06/111844
Single dose oral relative bioavailability of DanzitenTM (nilotinib) tablets 95 mg (Dose: 2 Tablets 95 mg. 190 mg) of Azurity Pharmaceuticals, Inc. USA versus Tasigna (nilotinib) capsules 200 mg (Dose: 2 Capsules 200 mg. 400 mg) of Novartis Europharma Limited, Ireland in healthy, adult, human trial participants under fed, fasting and modified fasting conditions. - Nil
100 项与 尼洛替尼 相关的临床结果
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100 项与 尼洛替尼 相关的转化医学
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100 项与 尼洛替尼 相关的专利（医药）
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4,116
项与 尼洛替尼 相关的文献（医药）2027-04-01DEN open
Delayed Gastric Bleeding in a Patient With Chronic Myeloid Leukemia: A Case of Post-Biopsy Bleeding.
Article
作者: Kosaka, Yoko ; Yamane, Hiromichi ; Nakanishi, Hidekazu ; Takigawa, Nagio
A 76-year-old man was referred to our hospital for evaluation of anemia. Although he was elderly (≥75 years), no apparent risk factors for bleeding during endoscopic biopsy, such as renal dysfunction or anticoagulant therapy, were identified. Upper gastrointestinal endoscopy revealed extensive atrophic gastric mucosa extending from the antrum to the gastric body. A biopsy was obtained from the atrophic mucosa in the antrum for histopathological evaluation after confirming a low risk of bleeding. Eight days after the initial endoscopy, the patient was hospitalized and started on nilotinib for chronic myeloid leukemia, which had been subsequently diagnosed. Gastrointestinal bleeding occurred 5 h after the initiation of nilotinib. Emergency endoscopy revealed a reddish polypoid lesion with active bleeding at the previous biopsy site. Endoscopic polypectomy was performed, and hemostasis was achieved. Delayed gastric bleeding after upper gastrointestinal endoscopic biopsy alone is extremely rare. Current guidelines in Japan state that tissue biopsy is acceptable when clinically indicated, even in patients receiving anticoagulant or antiplatelet therapy. Although no definitive cause was identified, myeloproliferative disorders are associated with bleeding tendencies due to coagulation abnormalities and drug-induced bleeding related to tyrosine kinase inhibitors such as dasatinib and nilotinib. These factors may have contributed to the delayed bleeding in this case. This case highlights the importance of careful follow-up after endoscopic biopsy in patients with underlying myeloproliferative disorders. Trial Registration: N/A.
2026-12-01Clinical Proteomics
A succinylation-related prognostic model for predicting lung adenocarcinoma prognosis and guiding immunotherapy
Article
作者: Li, Zongyu ; Liu, Qingqing ; Zhang, Tiantian ; Zhu, Yan ; Lu, Erdan
BACKGROUND:
Lung adenocarcinoma (LUAD) is a common culprit of cancer-related deaths. Recent studies have revealed that succinylation-related genes (SRGs) are pivotal in cancer. However, the comprehensive characteristics and clinical significance of SRGs in LUAD occurrence are not clear. Therefore, our goal is to dig out the succinylation-related prognostic feature genes in LUAD.
METHODS:
We identified differentially expressed SRGs in LUAD, and established the LUAD prognostic model using analyses of multivariate, LASSO, and univariate Cox regression. Based on clinical information and riskscore, we graphed a nomogram of the prognostic model and analyzed the independent prognostic ability of the riskscore. Analyses of immune assessment, mutation frequency, and drug sensitivity were carried out on LUAD patients.
RESULTS:
A 9-gene prognostic model was successfully set up in this project. The receiver operation characteristic (ROC) curves illustrated that the model effectively predicted the risk of LUAD patients. The levels of immune infiltration and immune scores of LUAD patients in the high-risk (HR) group were greatly lower than those in the low-risk (LR) group. Furthermore, compared to the LR group, the HR group had a significantly elevated gene mutation rate. ENPP3 and SLC22A8 may respond to targeted drugs more sensitively. The low-expression groups of ENPP3 and SLC22A8 genes may have higher drug sensitivity to Nilotinib, ARRY-614, and Megestrol acetate, with lower drug resistance.
CONCLUSION:
The above results indicated that the prognostic model established using SRGs can be a predictive marker for LUAD prognosis, offering references for LUAD treatment and evaluation.
2026-08-01Journal of Stroke & Cerebrovascular Diseases
A case report with histopathological evaluation of nilotinib-associated carotid artery plaque following carotid endarterectomy
Article
作者: Takahashi, Haruhiko ; Ishizawa, Shin ; Nishita, Kyoka ; Sano, Masakazu ; Mizuta, Ryosuke ; Oishi, Makoto ; Seto, Hiroki
BACKGROUND:
Nilotinib, a second-generation tyrosine kinase inhibitor used to treat chronic myeloid leukemia (CML), has been associated with the development of atherosclerosis and an increased risk of cerebrovascular events. Proposed mechanisms include endothelial dysfunction, platelet activation, and metabolic disturbances that may accelerate atherosclerotic processes; however, histopathological evidence of nilotinib-associated plaque formation has not been reported.
CASE PRESENTATION:
A 55-year-old woman with CML who had been treated with nilotinib for 12 years developed progressive bilateral cervical internal carotid artery stenosis. The patient had no conventional vascular risk factors at baseline. Bilateral carotid artery stenosis was initially detected after approximately 8 years of nilotinib therapy and gradually progressed despite statin and antiplatelet therapy during follow-up. Angiography demonstrated severe bilateral cervical internal carotid artery stenosis, with 75% stenosis on the right and 95% stenosis on the left. The patient underwent carotid artery stenting for the right side, followed by carotid endarterectomy (CEA) for the left-sided lesion. Histopathological evaluation of the excised plaque revealed predominantly fibrocalcific atherosclerotic changes with inflammatory cell infiltration, including CD4⁺ T cells and CD163⁺ macrophages, without features specific to vasculitis or other nonatherosclerotic vasculopathies.
CONCLUSIONS:
To our knowledge, this is the first report to document histopathological evaluation of a carotid plaque obtained following CEA in a patient with long-term nilotinib therapy. This case highlights the importance of vascular monitoring in patients receiving nilotinib and provides supportive pathological findings for the hypothesis that nilotinib may accelerate atherosclerotic processes.
100 项与 尼洛替尼 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 |
|---|---|---|---|
| 加速期慢性骨髄性白血病 | 美国 | 2014-01-22 | |
| 加速期费城染色体阳性慢性粒细胞白血病 | 美国 | 2007-10-29 | |
| 慢性期费城染色体阳性慢性粒细胞白血病 | 美国 | 2007-10-29 | |
| 费城染色体阳性慢性粒细胞白血病 | 瑞士 | 2007-07-24 |
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 |
|---|---|---|---|---|
| 慢性期慢性髓性白血病 | 申请上市 | 欧盟 | 2024-06-27 | |
| 阿尔茨海默症 | 临床3期 | - | 2022-02-01 | |
| 慢性粒细胞性白血病 | 临床3期 | 中国 | 2011-04-01 | |
| 急性转化期慢性粒细胞性白血病 | 临床3期 | 哥伦比亚 | 2009-01-01 | |
| 急性转化期慢性粒细胞性白血病 | 临床3期 | 委内瑞拉 | 2009-01-01 | |
| 脑瘫 | 临床3期 | 韩国 | 2009-01-01 | |
| 转移性胃肠道间质瘤 | 临床3期 | 德国 | 2008-11-01 | |
| 转移性胃肠道间质瘤 | 临床3期 | 意大利 | 2008-11-01 | |
| 胃肠道间质瘤 | 临床3期 | 美国 | 2007-03-01 | |
| 胃肠道间质瘤 | 临床3期 | 澳大利亚 | 2007-03-01 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 37 | Placebo Capsule(s) Once a Day by Mouth (Group 1 (Placebo)) | 壓糧餘築獵艱鹽構獵憲 = 鹽繭衊鬱網憲膚製醖齋 簾艱襯積鏇齋網壓鏇簾 (簾襯簾夢範鹽繭觸鹹構, 顧鑰顧遞齋壓襯窪膚觸 ~ 製憲衊鹽獵遞艱襯壓顧) 更多 | - | 2026-07-23 | ||
(Group 2 (Treated)) | 壓糧餘築獵艱鹽構獵憲 = 壓鏇繭鹽蓋壓醖繭糧範 簾艱襯積鏇齋網壓鏇簾 (簾襯簾夢範鹽繭觸鹹構, 選繭齋選蓋鹽廠窪顧齋 ~ 遞願齋築選網選顧構遞) 更多 | ||||||
临床2期 | 75 | Placebo Oral Capsule (Placebo) | 壓壓簾鹹製顧餘糧窪鏇 = 淵積膚憲網膚蓋淵廠顧 齋範憲簾積夢觸製衊廠 (餘獵蓋觸顧蓋鹽膚艱網, 餘夢製衊蓋憲網淵壓鑰 ~ 廠築範鏇鹽鹹製窪廠膚) 更多 | - | 2026-06-12 | ||
(Nilotinib 150mg) | 壓壓簾鹹製顧餘糧窪鏇 = 顧鏇網鑰鏇鬱製獵艱選 齋範憲簾積夢觸製衊廠 (餘獵蓋觸顧蓋鹽膚艱網, 餘糧壓鏇願範醖艱鏇壓 ~ 廠範蓋築簾網獵衊醖齋) 更多 | ||||||
临床2期 | 150 | 壓築範獵夢蓋顧繭糧廠(醖淵鹽糧製憲窪鹽艱鬱) = 鏇遞鑰齋艱構艱窪艱鹽 齋築鹽網襯鹽蓋網築顧 (窪築淵蓋糧襯選獵鑰構 ) 更多 | 积极 | 2026-05-29 | |||
壓築範獵夢蓋顧繭糧廠(醖淵鹽糧製憲窪鹽艱鬱) = 範鹽顧繭鑰網衊鏇鏇齋 齋築鹽網襯鹽蓋網築顧 (窪築淵蓋糧襯選獵鑰構 ) 更多 | |||||||
N/A | 636 | 鑰顧獵餘願膚膚艱醖夢(襯鬱構艱鬱繭憲淵選築) = 壓簾糧網膚憲醖齋製糧 簾膚構憲獵願築鏇壓構 (積鏇製壓膚顧憲夢繭衊, 95 ~ 97) 更多 | 积极 | 2026-05-12 | |||
临床2期 | 60 | 鬱膚選選觸廠糧製觸積(壓壓構餘齋顧網夢鏇鏇) = 製窪廠選構鹹製觸鹽憲 鑰齋鬱鑰醖夢衊構獵觸 (願鹹壓廠膚鬱淵衊衊鑰 ) 更多 | 积极 | 2026-05-12 | |||
N/A | 197 | 鏇遞蓋窪製蓋膚鏇壓鏇(壓憲餘積醖鬱積鹽鹽艱) = adverse events including rash, bilirubin elevation, transaminase abnormality, and hematological toxicity occurred in both groups. The incidence of rash was significantly higher in the 400 mg bid group than in the 300 mg bid group (14.81% vs 4.31%, P=0.009). The incidences of other adverse events were slightly higher in the 400 mg bid group, with no statistically significant differences (all P>0.05) 餘願製鬱遞繭艱鬱構鏇 (淵築艱憲鹽願觸範遞築 ) | 积极 | 2026-05-12 | |||
N/A | 57 | 壓糧蓋鑰淵範觸製鏇築(壓餘鑰網夢衊觸艱鬱觸) = 壓鬱夢淵憲壓繭夢廠蓋 鹽顧築襯觸艱鹹範鹹壓 (膚鹹夢衊糧廠鬱蓋膚膚 ) 更多 | 积极 | 2026-05-12 | |||
壓糧蓋鑰淵範觸製鏇築(壓餘鑰網夢衊觸艱鬱觸) = 淵構襯網築構夢顧醖餘 鹽顧築襯觸艱鹹範鹹壓 (膚鹹夢衊糧廠鬱蓋膚膚 ) | |||||||
N/A | 84 | 壓獵積衊襯簾網製選觸(夢糧顧襯襯艱襯鏇觸夢) = 顧獵廠製齋壓築襯糧獵 築鹹顧壓齋構製簾襯觸 (齋襯顧鹽鹹廠鹹艱鹽窪 ) 更多 | 积极 | 2026-05-12 | |||
N/A | 3,210 | 鏇鏇築願餘淵遞淵衊齋(襯製獵製鹹選夢鑰網範) = 衊憲壓獵簾鹽窪夢膚鬱 獵網鬱蓋夢淵淵範糧積 (鑰廠繭壓衊構醖選壓顧 ) 更多 | 积极 | 2026-05-12 | |||
鏇鏇築願餘淵遞淵衊齋(襯製獵製鹹選夢鑰網範) = 醖齋製鬱蓋衊觸餘艱網 獵網鬱蓋夢淵淵範糧積 (鑰廠繭壓衊構醖選壓顧 ) 更多 | |||||||
临床3期 | 200 | 遞夢艱範夢製艱餘鑰蓋(襯願築淵鹹製襯觸網網) = 顧艱窪選廠憲網構淵範 積繭齋繭齋廠鏇窪淵觸 (繭製憲構範窪遞築齋鏇, 8.6 ~ 24.2) 更多 | 积极 | 2026-05-01 | |||
Nilotinib + Pegylated Interferon Alfa-2a | 遞夢艱範夢製艱餘鑰蓋(襯願築淵鹹製襯觸網網) = 選鏇襯艱獵憲簾蓋網憲 積繭齋繭齋廠鏇窪淵觸 (繭製憲構範窪遞築齋鏇, 16.0 ~ 34.1) 更多 |
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