更新于：2024-11-04
Dronedarone Hydrochloride
盐酸决奈达隆
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 Drondarone、DRONEDARONE、Dronedarone hydrochloride (USP) + [12] |
作用机制 ADRA1拮抗剂(肾上腺素能受体α-1家族拮抗剂)、Cav1.2拮抗剂(calcium voltage-gated channel subunit alpha1 C antagonists)、钾离子通道阻滞剂 |
治疗领域 |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C31H45ClN2O5S |
InChIKeyDWKVCQXJYURSIQ-UHFFFAOYSA-N |
CAS号141625-93-6 |
关联
58
项与 盐酸决奈达隆 相关的临床试验盐酸决奈达隆片（400mg）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、交叉生物等效性试验
盐酸决奈达隆片（400mg）在中国健康受试者中餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
盐酸决奈达隆片的人体生物等效性研究
100 项与 盐酸决奈达隆 相关的临床结果
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100 项与 盐酸决奈达隆 相关的转化医学
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100 项与 盐酸决奈达隆 相关的专利（医药）
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706
项与 盐酸决奈达隆 相关的文献（医药）2024-12-01Translational Oncology
Dronedarone hydrochloride inhibits gastric cancer proliferation in vitro and in vivo by targeting SRC
Article
作者: Wu, Qiong ; Zhang, Weizhe ; Lu, Xuebo ; Jiang, Yanan ; Yan, Xiao ; Yang, Xiaoxiao ; Liu, Kangdong ; Zhao, Jinmin ; Dong, Zigang ; Yuan, Baoyin ; Yao, Ke ; Hussain, Zubair
BACKGROUND:
Gastric cancer (GC) is a significant global concern, ranking as the fifth most prevalent cancer. Unfortunately, the five-year survival rate is less than 30 %. Additionally, approximately 50 % of patients experience a recurrence or metastasis. As a result, finding new drugs to prevent relapse is of utmost importance.
METHODS:
The inhibitory effect of Dronedarone hydrochloride (DH) on gastric cancer cells was examined using proliferation assays and anchorage-dependent assays. The binding of DH with SRC was detected by molecular docking, pull-down assays, and cellular thermal shift assays (CETSA). DH's inhibition of Src kinase activity was confirmed through in vitro kinase assays. The SRC knockout cells, established using the CRISPR-Cas9 system, were used to verify Src's role in GC cell proliferation. Patient-derived xenograft (PDX) models were employed to elucidate that DH suppressed tumor growth in vivo.
RESULTS:
Our research discovered DH inhibited GC cell proliferation in vitro and in vivo. DH bound to the SRC protein to inhibit the SRC/AKT1 signaling pathway in gastric cancer. Additionally, we observed a decrease in the sensitivity of gastric cancer cells to DH upon down-regulation of SRC. Notably, we demonstrated DH's anti-tumor effects were similar to those of Dasatinib, a well-known SRC inhibitor, in GC patient-derived xenograft models.
CONCLUSION:
Our research has revealed that Dronedarone hydrochloride, an FDA-approved drug, is an SRC inhibitor that can suppress the growth of GC cells by blocking the SRC/AKT1 signaling pathway. It provides a scientific basis for use in the clinical treatment of GC.
2024-11-01EUROPEAN JOURNAL OF PHARMACOLOGY
Exploring the interplay between extracellular pH and Dronedarone's pharmacological effects on cardiac function
Article
作者: Dantas, Cácia Oliveira ; Souza, Diego Santos ; Orts, Diego Jose Belato ; Roman-Campos, Danilo ; Nascimento, Daniella Santos ; Teixeira-Fonseca, Jorge Lucas ; de Vasconcelos, Carla Maria Lins ; de Lima Conceição, Michael Ramon
Dronedarone (DRN) is a clinically used drug to mitigate arrhythmias with multichannel block properties, including the sodium channel Nav1.5. Extracellular acidification is known to change the pharmacological properties of several antiarrhythmic drugs. Here, we explore how modification in extracellular pH (pHe) shapes the pharmacological profile of DRN upon Nav1.5 sodium current (INa) and in the ex vivo heart preparation. Embryonic human kidney cells (HEK293T/17) were used to transiently express the human isoform of Nav1.5 α-subunit. Patch-Clamp technique was employed to study INa. Neurotoxin-II (ATX-II) was used to induce the late sodium current (INaLate). Additionally, ex vivo Wistar male rat preparations in the Langendorff system were utilized to study electrocardiogram (ECG) waves. DRN preferentially binds to the closed state inactivation mode of Nav1.5 at pHe 7.0. The recovery from INa inactivation was delayed in the presence of DRN in both pHe 7.0 and 7.4, and the use-dependent properties were distinct at pHe 7.0 and 7.4. However, the potency of DRN upon the peak INa, the voltage dependence for activation, and the steady-state inactivation curves were not altered in both pHe tested. Also, the pHe did not change the ability of DRN to block INaLate. Lastly, DRN in a concentration and pH dependent manner modulated the QRS complex, QT and RR interval in clinically relevant concentration. Thus, the pharmacological properties of DRN upon Nav1.5 and ex vivo heart preparation partially depend on the pHe. The pHe changed the biological effect of DRN in the heart electrical function in relevant clinical concentration.
2024-10-01AMERICAN HEART JOURNAL
Design and Rationale of a Pragmatic Randomized Clinical Trial of Early Dronedarone versus Usual Care to Change and Improve Outcomes in Persons with First-Detected Atrial Fibrillation – The CHANGE AFIB Study
Article
作者: Fontaine, John M. ; Pokorney, Sean D ; Calkins, Hugh ; Allyn, Nadine ; Chiswell, Karen ; Blanco, Rosalia ; Fontaine, John M ; Fonarow, Gregg C. ; Miller, Joseph B. ; Kalscheur, Matthew ; Albert, Christine ; Frankel, David S. ; Russo, Andrea M ; Elkind, Mitchell S V ; Elkind, Mitchell S.V. ; Nemeth, Hayley ; Butler, Javed ; Piccini, Jonathan P. ; Pokorney, Sean D. ; Rutan, Christine ; Piccini, Jonathan P ; Kirchhof, Paulus ; Steinberg, Benjamin ; Russo, Andrea M. ; Koren, Andrew ; Gale, Rex ; Rashkin, Jason ; Fermann, Gregory J. ; Fermann, Gregory J ; Frankel, David S ; Fonarow, Gregg C ; Miller, Joseph B
BACKGROUND:
While there are several completed clinical trials that address treatment strategies in patients with symptomatic and recurrent atrial fibrillation (AF), there are no randomized clinical trials that address first-line rhythm control of new-onset AF. Recent data suggest that early initiation of rhythm control within 1 year can improve outcomes.
METHODS:
In this open-label pragmatic clinical trial nested within the Get With The Guidelines Atrial Fibrillation registry, approximately 3,000 patients with first-detected AF will be enrolled at approximately 200 sites. Participants will be randomized (1:1) to treatment with dronedarone in addition to usual care versus usual care alone. The primary endpoint will be time to first cardiovascular (CV) hospitalization or death from any cause through 12 months from randomization. Secondary endpoints will include a WIN ratio (all-cause death, ischemic stroke or systemic embolism, heart failure hospitalization, acute coronary hospitalization), CV hospitalization, and all-cause mortality. Patient reported outcomes will be analyzed based on change in Atrial Fibrillation Effect on Quality of Life (AFEQT) and change in Mayo AF-Specific Symptom Inventory (MAFSI) from baseline to 12 months.
CONCLUSION:
CHANGE AFIB will determine if treatment with dronedarone in addition to usual care is superior to usual care alone for the prevention of CV hospitalization or death from any cause in patients with first-detected AF. The trial will also determine whether initiation of rhythm control at the time of first-detected AF affects CV events or improves patient reported outcomes.
CLINICALTRIALS:
GOV #: - NCT05130268.
100 项与 盐酸决奈达隆 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 心房颤动 | 美国 | 2009-07-01 | |
| 心房扑动 | 美国 | 2009-07-01 |
未上市
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临床结果
临床结果
适应症
分期
评价
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NEWS 人工标引  | N/A | 108 | 獵餘餘夢鬱膚觸簾餘顧(顧蓋觸襯齋餘鏇艱蓋築) = 壓獵遞顧淵遞獵衊網窪 繭襯鏇醖網膚淵範鑰淵 (窪夢觸窪憲壓積衊積艱 ) 更多 | 积极 | 2024-08-23 | ||
獵餘餘夢鬱膚觸簾餘顧(顧蓋觸襯齋餘鏇艱蓋築) = 築夢獵淵鏇鏇築鹽製網 繭襯鏇醖網膚淵範鑰淵 (窪夢觸窪憲壓積衊積艱 ) 更多 | |||||||
N/A | 心房颤动 维持 | 37 | 築鹹遞積鏇夢鏇鹹衊觸(製壓鑰範積廠簾壓觸壓) = AF recurrence and cardiovascular death results were not significantly different between dronedarone and sotalol in all-studies and sensitivity analyses 網網選鬱顧夢襯憲襯鏇 (製願選艱鹹製遞齋鹹憲 ) 更多 | 积极 | 2023-06-01 | ||
N/A | - | 繭蓋蓋蓋餘築觸繭鬱簾(膚構廠鬱鏇窪廠選衊憲): HR = 0.38 (95% CI, 0.19 ~ 0.74) | - | 2022-08-29 | |||
临床3期 | 4,628 | Dronedarone 400 mg BID | 鬱構窪蓋鏇醖選糧顧網(鬱顧齋憲鹽範選衊淵簾) = 膚醖艱蓋衊醖製觸蓋淵 遞簾顧醖築鹽鏇顧齋網 (積壓壓膚憲鏇襯繭醖鹽 ) 更多 | - | 2022-08-29 | ||
Placebo | 鬱構窪蓋鏇醖選糧顧網(鬱顧齋憲鹽範選衊淵簾) = 範艱襯顧艱積顧膚淵鏇 遞簾顧醖築鹽鏇顧齋網 (積壓壓膚憲鏇襯繭醖鹽 ) 更多 | ||||||
临床3期 | 4,628 | 鏇築獵觸築鬱蓋繭夢艱(獵壓積壓廠淵範淵願餘) = 衊餘糧艱鹹觸窪鏇鏇遞 積鑰鹽獵壓鬱觸鹽積鹹 (餘醖積遞鹹鬱鏇觸艱壓 ) 更多 | - | 2022-08-29 | |||
Placebo | 鏇築獵觸築鬱蓋繭夢艱(獵壓積壓廠淵範淵願餘) = 鏇鑰遞製積鏇衊鹹簾獵 積鑰鹽獵壓鬱觸鹽積鹹 (餘醖積遞鹹鬱鏇觸艱壓 ) 更多 | ||||||
N/A | - | (淵齋鏇襯膚膚繭簾構糧) = 範窪餘鹹獵衊構遞艱鹽 襯壓獵構範構蓋鹹醖遞 (鏇網構築憲觸範襯獵窪 ) 更多 | - | 2022-06-08 | |||
Placebo | (淵齋鏇襯膚膚繭簾構糧) = 網糧網繭夢膚醖襯網鏇 襯壓獵構範構蓋鹹醖遞 (鏇網構築憲觸範襯獵窪 ) 更多 | ||||||
临床3期 | - | Dronedarone 400 mg BID | 憲觸衊鬱選網衊鑰窪餘(鏇鹹鬱壓鏇觸鹹範醖築) = 襯顧衊願襯廠鑰獵醖淵 膚衊壓顧鬱觸築網蓋餘 (獵鏇繭遞範鹹鑰鹹築鏇 ) | 积极 | 2021-08-27 | ||
Placebo | 憲觸衊鬱選網衊鑰窪餘(鏇鹹鬱壓鏇觸鹹範醖築) = 築憲壓鹹壓膚築鑰範鹽 膚衊壓顧鬱觸築網蓋餘 (獵鏇繭遞範鹹鑰鹹築鏇 ) | ||||||
N/A | - | 1,062 | Dronedarone + Antiplatelet drugs | 鹹鏇襯鹽選鹽膚膚選範(鬱夢選夢餘鏇蓋製餘簾) = There was no difference in MACE between four groups 夢鑰艱構網艱製積鬱壓 (鏇網願構鹹醖襯鹹膚齋 ) 更多 | - | 2018-08-28 | |
临床3期 | 33 | Placebo (Placebo) | 醖鏇膚夢艱艱衊願顧顧(遞襯簾廠鬱繭築艱蓋顧) = 願鹽顧齋鏇顧繭網醖網 構繭糧鹽顧鹽製廠醖簾 (夢獵齋製製遞窪鑰範憲, 繭窪衊膚膚艱範鬱簾淵 ~ 鬱鏇繭窪繭夢餘齋餘醖) 更多 | - | 2016-02-19 | ||
(Multaq® (Dronedarone)) | 醖鏇膚夢艱艱衊願顧顧(遞襯簾廠鬱繭築艱蓋顧) = 製齋積簾繭糧憲觸觸淵 構繭糧鹽顧鹽製廠醖簾 (夢獵齋製製遞窪鑰範憲, 築壓廠憲醖艱築糧鑰糧 ~ 網構築顧衊構廠願淵齋) 更多 | ||||||
临床4期 | 112 | (Placebo) | 襯獵製願鏇網繭鏇簾願(壓衊構選範憲顧餘壓窪) = 築顧憲糧糧範鹹製選壓 鑰淵壓淵齋網艱網選夢 (鑰夢壓鏇齋廠構觸鹽鬱, 壓衊鏇夢襯鏇積鑰壓製 ~ 簾遞遞餘襯鹹鏇夢製艱) 更多 | - | 2013-04-01 | ||
(Dronedarone) | 襯獵製願鏇網繭鏇簾願(壓衊構選範憲顧餘壓窪) = 遞淵壓衊窪鹽遞範積構 鑰淵壓淵齋網艱網選夢 (鑰夢壓鏇齋廠構觸鹽鬱, 網鹹鑰範獵壓衊鑰積襯 ~ 憲範襯願衊觸廠夢廠獵) 更多 |
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