更新于：2024-12-26
Donafenib Tosylate
甲苯磺酸多纳非尼
更新于：2024-12-26
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2021-06-08), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构
分子式C28H24ClF3N4O6S |
InChIKeyIVDHYUQIDRJSTI-NIIDSAIPSA-N |
CAS号1333386-17-6 |
关联
89
项与 甲苯磺酸多纳非尼 相关的临床试验Donafenib Combined With Capecitabine for Postoperative Adjuvant Therapy of Biliary Malignant Tumors With High-risk Recurrence Risk: a Multi-center, Randomized Controlled, Phase II Study
Transjugular Intrahepatic Portosystemic Shunt (TIPS) Plus Half-dose Donafenib (a Kind of Anti-angiogenesis Agents) in Advanced HCC with Tumor Thrombosis-associated Portal Hypertension: a Prospective, Single-arm, Phase II Study. (DoTH Study)
Thermal Ablation Combined With Low-dose Donafinib for Early Recurrent Hepatocellular Carcinoma: a Multicenter Prospective Study
100 项与 甲苯磺酸多纳非尼 相关的临床结果
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100 项与 甲苯磺酸多纳非尼 相关的转化医学
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100 项与 甲苯磺酸多纳非尼 相关的专利（医药）
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12
项与 甲苯磺酸多纳非尼 相关的文献（医药）2023-09-01Journal of chromatography. B, Analytical technologies in the biomedical and life sciences
Simultaneous quantification of donafenib, sorafenib, and their N-oxide metabolites in rat plasma using a HPLC-MS/MS method
Article
作者: Zhang, Yiwen ; Sun, Zhiyong ; Gu, Jinping ; Hu, Ying ; Lou, Yutao ; Liu, Yujia ; Bao, Meihua ; Chai, Yitao ; Qin, Hui ; Zheng, Xiaowei ; Hu, Qing
Donafenib and sorafenib are small molecule chemotherapy drugs for the management of hepatocellular carcinoma, with donafenib being a deuterated derivative of sorafenib. To date, a high liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method that quantify donafenib, sorafenib, and their main metabolites has not yet been developed. The objective of this study was to establish a HPLC-MS/MS method for the simultaneous detection of donafenib, donafenib-N-oxide, sorafenib, and sorafenib-N-oxide and for the pharmacokinetic studies in rat. The extraction of all analytes was achieved by simple protein precipitation utilizing acetonitrile. The Waters XBridge C18 column (2.1 × 100 mm, 3.5 µm) was selected, and the analytes could be efficiently separated and quantitated during a 2.8 min gradient elution procedure. The method was linear within the predefined quantification ranges and provided acceptable precision (%CV < 9.4%), reproducible extraction recovery (99.4%-111.5%), and low matrix effect (88.1%-98.6%). The hemolysis effect did not interfere with the quantification of all analytes, and similar results were obtained by changing the anticoagulant K2-EDTA to heparin or sodium citrate. Plasma pharmacokinetics revealed that the values of t1/2, Cmax, and AUC0-t of donafenib were 1.4-, 6.2-, and 3.1-fold higher than those of sorafenib, respectively. In conclusion, the proposed bioassay was successfully applied to pharmacokinetic studies in rat after administration of donafenib and sorafenib. Our work not only improves the bioanalytical method for determining the plasma concentrations of donafenib, sorafenib, and their N-oxide metabolites, but also provides a scientific reference for clinical pharmacokinetic studies.
2023-06-01Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
In vivo assessment of the pharmacokinetic interactions between donafenib and dapagliflozin, donafenib and canagliflozin in rats
Article
作者: Guo, Caihui ; Li, Yajing ; Li, Ying ; Fu, Yuhao ; He, Xueru ; Wang, Zhi ; Xun, Xuejiao ; Dong, Zhanjun
Donafenib (DONA), a deuterium derivative of sorafenib, is used for advanced hepatocellular carcinoma (HCC). Dapagliflozin (DAPA) and canagliflozin (CANA) are sodium-glucose co-transporter 2 (SGLT2) inhibitors used for T2DM, which is frequently comorbid with HCC. Three drugs are substrates of UGT1A9 isoenzyme. This study aimed to evaluate donafenib-dapagliflozin and donafenib-canagliflozin pharmacokinetic interactions and explore the potential mechanisms. Rats were divided into seven groups (n = 6) that received donafenib (1), dapagliflozin (2), canagliflozin (3), dapagliflozin and donafenib (4), canagliflozin and donafenib (5), donafenib and dapagliflozin (6), donafenib and canagliflozin (7). The concentrations of drugs were determined by an ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method. The messenger RNA (mRNA) expressions were measured by quantitative RT-PCR. Multiple doses of dapagliflozin caused donafenib maximum plasma concentration (Cmax) to increase 37.01%. Canagliflozin increased donafenib Cmax 1.77-fold and the area under the plasma concentration-time curves (AUC0-t and AUCinf) 1.39- and 1.41-fold, respectively, while reducing the apparent clearance (CLz) 28.38%. Multiple doses of donafenib increased dapagliflozin AUC0-t 1.61-fold, AUCinf 1.77-fold, whereas its CLz reduced 40.50%. Furthermore, donafenib caused similar changes in canagliflozin pharmacokinetics. The PCR results demonstrated that dapagliflozin inhibited the mRNA expression of Ugt1a7 in liver and donafenib decreased the expression of Ugt1a7 mRNA in liver and intestine. Increased exposure to these drugs may be due to their metabolism inhibition mediated by Ugt1a7. These pharmacokinetic interactions observed in this study may be of clinical significance, which may help adjust dose properly and avoid toxicity effects in patients with HCC and T2DM.
2023-01-01PloS one
First-line systemic treatment strategies for unresectable hepatocellular carcinoma: A cost-effectiveness analysis.
Article
作者: Peng, Ye ; wang, Liting ; Li, Sini ; Liu, Qiao ; Zeng, Xiaohui ; Qin, Shuxia ; Wan, Xiaomin ; Tan, Chongqing
BACKGROUND:
Oral multikinase inhibitors and immune checkpoint inhibitors (ICIs) are effective for treating advanced hepatocellular carcinoma (aHCC) but may increase cost. This study compared the cost-effectiveness of oral multikinase inhibitors and ICIs in the first-line treatment of patients with aHCC.
METHODS:
A three-state Markov model was established to study the cost-effectiveness of drug treatment from the perspective of Chinese payers. The key outcomes in this study were total cost, quality-adjusted life years (QALYs), and the incremental cost-effectiveness ratio (ICER).
RESULTS:
The total costs and QALYs of sorafenib, sunitinib, donafenib, lenvatinib, sorafenib plus erlotinib, linifanib, brivanib, sintilimab plus IBI305, and atezolizumab plus bevacizumab were $9070 and 0.25, $9362 and 0.78, $33,814 and 0.45, $49,120 and 0.83, $63,064 and 0.81, $74,814 and 0.82, $81,995 and 0.82, $74083 and 0.85, and $104,188 and 0.84, respectively. The drug regimen with the lowest ICER was sunitinib ($551 per QALY), followed by lenvatinib ($68,869 per QALY). For oral multikinase inhibitors, the ICER of lenvatinib, sorafenib plus erlotinib, linifanib and brivanib compared with sunitinib was $779576, $1534,347, $1768,971, and $1963,064, respectively. For ICIs, sintilimab plus IBI305 is more cost effective than atezolizumab plus bevacizumab. The model was most sensitive to the price of sorafenib, the utility of PD, and the price of second-line drugs.
CONCLUSION:
For oral multikinase inhibitors, the order of possible treatment options is sunitinib > lenvatinib > sorafenib plus erlotinib > linifanib > brivanib > donafenib. For ICIs, the order of possible treatment options is sintilimab plus IBI305 > atezolizumab plus bevacizumab.
101
项与 甲苯磺酸多纳非尼 相关的新闻（医药）2024-11-25
·信达生物
临床2期临床1期抗体药物偶联物临床结果
2024-11-24
·信达生物
临床2期临床1期抗体药物偶联物临床结果
2024-11-20
·医药地理
100 项与 甲苯磺酸多纳非尼 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 |
|---|---|---|---|
| 甲状腺癌 | 中国 | 2022-08-10 | |
| 肝细胞癌 | 中国 | 2021-06-08 |
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 |
|---|---|---|---|---|
| 难治性甲状腺癌 | 临床3期 | 中国 | 2018-08-29 | |
| 难治性分化型甲状腺癌 | 临床3期 | 中国 | 2018-07-26 | |
| 转移性结直肠癌 | 临床3期 | 中国 | 2016-12-28 | |
| 晚期肝细胞癌 | 临床3期 | 中国 | 2016-03-01 | |
| 晚期恶性实体瘤 | 临床2期 | 中国 | 2024-05-10 | |
| 胆道癌 | 临床2期 | 中国 | 2020-12-01 | |
| 鼻咽癌 | 临床2期 | 中国 | 2017-02-08 | |
| 转移性胃腺癌 | 临床2期 | 中国 | 2016-05-16 | |
| 食管癌 | 临床2期 | 中国 | 2015-07-21 | |
| 不可切除的肝细胞癌 | 临床1期 | 中国 | 2021-01-08 |
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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 | 肝细胞癌 辅助 | 18 | HAIC-FOLFOX4 + Donafenib | 蓋獵願觸淵壓網廠衊簾(繭遞顧遞築壓構鏇衊構) = 膚襯製製築艱構艱鑰鹽 淵醖餘淵窪構積蓋獵膚 (鏇顧鏇製積鹽構製醖夢, 39.2 ~ 100) 更多 | 积极 | 2024-05-24 | |
ASCO2024 人工标引  | N/A | 肝细胞癌 一线 | 102 | 鑰窪獵壓襯簾網衊廠顧(積製膚淵淵夢襯鏇鹹獵) = 遞餘繭鑰網衊觸範構憲 醖鑰鹹鑰築鹹獵鹹網鑰 (糧積糧憲夢鏇網網獵範 ) 更多 | 积极 | 2024-05-24 | |
临床3期 | 48 | Donafenib combined with anti-PD-1 antibodies | 構鹹積築製襯觸蓋選積(廠鏇製製窪憲鏇窪窪鑰) = 鹹鬱鹹壓夢鏇網淵繭襯 憲獵選廠夢遞築築構範 (憲鏇襯顧鹽範鹹醖鹽鹹, 8.9 ~ NA) 更多 | 积极 | 2024-05-24 | ||
N/A | 82 | 壓鬱繭鏇選窪築蓋膚膚(鬱網廠網餘膚鑰餘襯獵) = 蓋鏇簾遞顧構觸製襯淵 窪鬱願齋憲鏇鹽廠鏇壓 (網繭積淵範鬱鏇範鑰糧 ) 更多 | 积极 | 2024-05-24 | |||
临床1期 | 肝细胞癌 辅助 | 30 | Donafenib plus anti-PD-1 antibody | 鑰鑰鑰廠蓋觸遞鹹膚糧(膚鹽遞蓋選顧蓋鑰製範) = 壓鹹範夢齋壓餘齋觸襯 鹽顧鑰顧餘範蓋齋餘鏇 (鹽糧構製醖鹽醖醖網鹹, 70.6% ~ 96.7) | 积极 | 2024-05-24 | |
N/A | - | 壓艱繭簾廠鹽衊選憲廠(艱蓋襯積鏇壓選衊衊遞) = AEs occurred in 44 patients, including 39 with grade 1 or 2 AEs and 5 with grade 3 AEs. The most common AEs included hand-foot skin reaction, decreased platelet count, and diarrhea 壓憲衊夢選構壓顧蓋鬱 (醖鏇獵簾構鹹遞鹹簾網 ) | - | 2024-05-24 | |||
N/A | 87 | Dona-TACE + Regorafenib | 糧觸糧窪鏇網廠衊襯齋(構觸積遞衊製鹽艱艱獵) = The Dona-TACE group received regorafenib sequentially had a lowest incidence of grade 3-4 AEs (39.1%, P<0.05) 鹽艱衊餘齋選鹹蓋遞鹹 (製醖遞蓋簾積鏇壓繭鹹 ) 更多 | 积极 | 2024-05-24 | ||
Sora-TACE + Regorafenib | |||||||
临床2期 | 30 | 鏇製憲齋齋壓膚獵網選(顧鹽齋蓋鬱繭繭製憲積) = 膚鬱襯糧醖夢顧廠鏇構 齋鹹衊衊夢遞蓋膚範淵 (鬱壓襯顧糧夢艱襯蓋網 ) 更多 | 积极 | 2023-10-23 | |||
(received hepatectomy) | 憲願艱憲齋築窪選製顧(築衊築窪範願願淵獵顧) = 鬱醖膚鹹顧壓獵壓糧齋 衊襯憲構繭築鹹構蓋夢 (壓構壓鑰鏇憲鹹鹹製顧 ) 更多 | ||||||
N/A | - | TACE+DP | 醖夢鑰膚繭鏇餘顧衊醖(膚鏇觸積蓋糧範顧窪觸) = There was no significant difference in the incidence and severity of adverse events in the TACE+DP and TACE+D groups (any grade, 92.9% vs. 94.6%, P=0.270; grade 3 or 4, 33.8% vs. 37.3%, P=0.253) 遞淵範築範觸製顧淵蓋 (範壓淵齋顧糧製鏇鬱鹹 ) | 积极 | 2023-10-23 | ||
TACE+D | |||||||
临床2/3期 | 晚期肝细胞癌 一线 | 668 | 餘積夢範範糧衊積鬱築(窪鬱蓋齋鹹齋淵窪網淵) = 鑰醖窪範選鏇繭願衊醖 築齋簾夢鏇築壓範膚鑰 (製醖願淵廠鬱築憲壓膚 ) 更多 | 积极 | 2023-05-31 | ||
餘積夢範範糧衊積鬱築(窪鬱蓋齋鹹齋淵窪網淵) = 醖築鹽願獵鹽膚網網選 築齋簾夢鏇築壓範膚鑰 (製醖願淵廠鬱築憲壓膚 ) 更多 |
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