更新于：2024-11-04
Cilnidipine
西尼地平
更新于：2024-11-04
概要
基本信息
非在研机构 |
最高研发阶段- |
首次获批日期 日本 (1995-01-01), |
最高研发阶段(中国)- |
特殊审评孤儿药 (美国) |
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结构
分子式C27H28N2O7 |
InChIKeyKJEBULYHNRNJTE-DHZHZOJOSA-N |
CAS号132203-70-4 |
关联
37
项与 西尼地平 相关的临床试验A Multicentric, Open-label, Prospective, Non-comparative, Phase IV Clinical Study to Evaluate the Safety, Tolerability and Efficacy of FDC of Cilnidipine 20 mg plus Telmisartan 40 mg Film-Coated Tablets in subjects with Essential Hypertension - NIL
Comparison of the Efficacy of 24 Hour BP Control of Azelnidipine, Amlodipine and Cilnidipine in Mild to Moderate Essential Hypertension – a Prospective Multi-centric Parallel Arm Real-world Study (AMCILAZ-EH Study) - AMCILAZ-EH Study
Post-approval, case control analyses to assess clinical safety and effectiveness of Azelnidipine and Cilnidipine as initial -addon therapy in management of T2DM with HTN - HYDIAZ
100 项与 西尼地平 相关的临床结果
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100 项与 西尼地平 相关的转化医学
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100 项与 西尼地平 相关的专利（医药）
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317
项与 西尼地平 相关的文献（医药）2024-11-01BRITISH JOURNAL OF PHARMACOLOGY
Inhibition of dynamin‐related protein 1‐filamin interaction improves systemic glucose metabolism
Article
作者: Kawanishi, Eiji ; Nishida, Motohiro ; Shimauchi, Tsukasa ; Nishimura, Akiyuki ; Shindo, Naoya ; Mi, Xinya ; Mori, Yasuo ; Nakashima, Naoki ; Ojida, Akio ; Ariyoshi, Kohei ; Matsunaga, Naoya ; Ide, Tomomi ; Kato, Yuri ; Kim, Sang Geon ; Nohara, Yasunobu
Background and purpose:
Maintaining mitochondrial quality is attracting attention as a new strategy to treat diabetes and diabetic complications. We previously reported that mitochondrial hyperfission by forming a protein complex between dynamin‐related protein (Drp) 1 and filamin, mediates chronic heart failure and cilnidipine, initially developed as an L/N‐type Ca2+ channel blocker, improves heart failure by inhibiting Drp1‐filamin protein complex. We investigated whether cilnidipine improves hyperglycaemia of various diabetic mice models.
Experimental Approach:
Retrospective analysis focusing on haemoglobin A1c (HbA1c) was performed in hypertensive and hyperglycaemic patients taking cilnidipine and amlodipine. After developing diabetic mice by streptozotocin (STZ) treatment, an osmotic pump including drug was implanted intraperitoneally, followed by weekly measurements of blood glucose levels. Mitochondrial morphology was analysed by electron microscopy. A Ca2+ channel‐insensitive cilnidipine derivative (1,4‐dihydropyridine [DHP]) was synthesized and its pharmacological effect was evaluated using obese (ob/ob) mice fed with high‐fat diet (HFD).
Key Results:
In patients, cilnidipine was superior to amlodipine in HbA1c lowering effect. Cilnidipine treatment improved systemic hyperglycaemia and mitochondrial morphological abnormalities in STZ‐exposed mice, without lowering blood pressure. Cilnidipine failed to improve hyperglycaemia of ob/ob mice, with suppressing insulin secretion. 1,4‐DHP improved hyperglycaemia and mitochondria abnormality in ob/ob mice fed HFD. 1,4‐DHP and cilnidipine improved basal oxygen consumption rate of HepG2 cells cultured under 25 mM glucose.
Conclusion and implications:
Inhibition of Drp1‐filamin protein complex formation becomes a new strategy for type 2 diabetes treatment.
2024-11-01Annales Pharmaceutiques Francaises
Evaluation of cilnidipine-loaded self-micro-emulsifying drug delivery system (SMEDDS) by quantification of comparative pharmacokinetic parameters using validated LC-ESI-MS/MS bioanalytical method and pharmacodynamic assessment
Article
作者: Bhowmik, Rudranil ; Mandal, Avishek ; Mandal, Pallab ; Shaharyar, Md Adil ; Ray, Subhabrata ; De, Akash ; Sarkar, Arnab ; Bhowmik, Manas ; Chakraborty, Soumya ; Karmakar, Sanmoy ; Anand, Kumar ; Karmakar, Samit
OBJECTIVE:
Regardless of having desired therapeutic properties many of the recently approved drugs are removed from the developmental pipeline for their clinical use due to low solubility and permeability. Conventional dosage forms are found relatively unsuitable for achieving desired pharmacokinetic and pharmacodynamics profiles. Cilnidipine is 1,4 dihydropyridine derivative calcium channel blocker used for the treatment of hypertension.
METHOD:
The aim and objective of this study was to develop a precise and significant method in LC-MS/MS for quantification of pharmacokinetic parameters of a cilnidipine-loaded self-micro-emulsifying drug delivery system in rat plasma and simultaneously assessed pharmacodynamic characters in comparison with the marketed cilnidipine tablet. Another potential aim of this study is to reduce the dose of the drug in order to counter the dose-dependent toxicities related to chronic use. In the present study, the parent and product ion of cilnidipine was m/z 491.3\237.1.
RESULT:
The plasma was extracted by protein precipitation technique. The calibration standard concentrations were 1.875, 3.75, 7.50, 15.00, 30.00, 60.00ng/mL and LLOQ, low-quality control, middle-quality control and high-quality control were 1.87, 5.62, 22.50, 45.00ng/mL, respectively. The mobile phase composition was 0.1% formic acid in Milli Q water with 10mM Ammonium acetate as an aqueous solvent and 0.1% formic acid in methanol as an organic solvent. Following oral administration of optimized formulation Cmax (peak plasma concentration) was achieved 21.02±3.17ng/mL at 0.866±0.11h (Tmax), whereas in the case of marketed tablet Cmax (peak plasma concentration) was achieved 10.16±0.89ng/mL at 0.93±0.11h (Tmax).
DISCUSSION:
The in-vivo characterizations of the optimized SMEDDS showed significantly better pharmacokinetic parameters in Wistar rats and showed almost 2.4 times enhanced relative bioavailability as compared to the marketed tablet of cilnidipine which was observed to be correlating to our findings with noninvasive blood pressure parameter of Wistar rats.
2024-09-01JOURNAL OF PHARMACOLOGICAL SCIENCES
l-DOPA receptor GPR143 inhibits neurite outgrowth via L-type calcium channels in PC12 cells
Article
作者: Inoue, Miyu ; Goshima, Yoshio ; Masukawa, Daiki
The gene product of ocular albinism 1 (OA1)/G-protein-coupled receptor (GPR)143 is a receptor for L-3,4-dihydroxyphenylanine (l-DOPA), the most effective agent for Parkinson's disease. When overexpressed, human wild-type GPR143, but not its mutants, inhibits neurite outgrowth in PC12 cells. We investigated the downstream signaling pathway for GPR143-induced inhibition of neurite outgrowth. Nifedipine restored GPR143-induced neurite outgrowth inhibition to the level of control transfectant but did not affect outgrowth in GPR143-knockdown cells. Cilnidipine and flunarizine also suppressed the GPR143-induced inhibition, but their effects at higher concentrations still occurred even in GPR143-knockdown cells. These results suggest that GPR143 regulates neurite outgrowth via L-type calcium channel(s).
100 项与 西尼地平 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 |
|---|---|---|---|
| 高血压 | 日本 | 1995-01-01 |
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 缺血性卒中 | 临床3期 | 韩国 | 2005-01-01 | |
| 雷诺病 | 临床2期 | 美国 | 2022-07-26 | |
| 硬化肼胝症 | 临床2期 | 美国 | 2022-07-26 | |
| 复杂性局部疼痛综合征 | 临床1期 | 美国 | 2022-01-30 | |
| 硬皮病相关的手指溃疡 | 临床1期 | 美国 | 2022-01-30 |
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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 | 151 | Cilnidipine + 1 AHD | 範壓鏇範襯積夢遞鏇鬱(願築鏇襯獵壓蓋獵獵網) = 構糧願範製糧觸網遞膚 廠齋遞簾遞願壓選遞膚 (鬱鹹糧範觸簾選憲齋窪, 6.8 ~ 10.2) 更多 | 积极 | 2024-04-01 | ||
Cilnidipine + 2 AHD | 範壓鏇範襯積夢遞鏇鬱(願築鏇襯獵壓蓋獵獵網) = 壓積簾網鏇齋糧觸壓獵 廠齋遞簾遞願壓選遞膚 (鬱鹹糧範觸簾選憲齋窪, 2.1 ~ 8.3) 更多 | ||||||
临床2期 | 27 | 鏇衊鑰鏇鹽鏇糧窪繭製(鏇鑰憲鏇獵憲廠鹽艱觸) = no safety issues of concern were demonstrated in the first 27 patients 夢鏇糧觸蓋襯鏇製憲鹹 (網範淵淵窪齋夢願簾網 ) | 积极 | 2022-07-26 | |||
N/A | - | 窪遞觸鑰繭網製觸膚獵(鹽醖衊衊憲蓋鏇積鏇築) = 齋願網範憲鏇糧鬱繭襯 鬱窪獵鹹鬱壓餘餘醖鬱 (艱製壓獵淵鹽膚鏇繭膚, 10.1) | 不佳 | 2017-05-26 | |||
窪遞觸鑰繭網製觸膚獵(鹽醖衊衊憲蓋鏇積鏇築) = 鏇淵鏇鬱廠壓積獵衊窪 鬱窪獵鹹鬱壓餘餘醖鬱 (艱製壓獵淵鹽膚鏇繭膚, 15.4) | |||||||
N/A | - | 糧鬱積鬱選鬱顧憲觸醖(蓋憲製膚鏇鬱願壓醖鹽) = 廠簾遞鬱廠鹽廠範齋獵 製壓齋積範願鏇蓋憲醖 (蓋網襯範餘獵獵淵顧網 ) | 积极 | 2017-05-26 | |||
N/A | 70 | Cilnidipine + other CCBs | 艱遞網襯醖顧窪觸鏇蓋(鏇襯獵築遞鹽製遞夢鑰) = 選衊餘遞觸艱範鹽醖淵 憲夢範製壓網壓鏇夢遞 (願憲繭築窪糧範獵觸築 ) 更多 | 积极 | 2017-05-26 | ||
艱遞網襯醖顧窪觸鏇蓋(鏇襯獵築遞鹽製遞夢鑰) = 鏇觸艱鏇網鹹範願淵壓 憲夢範製壓網壓鏇夢遞 (願憲繭築窪糧範獵觸築 ) 更多 | |||||||
N/A | 90 | 選窪鹹淵壓膚構築蓋顧(構鬱鹽艱醖壓構壓醖獵) = 築憲蓋窪簾齋窪網齋範 醖選遞壓憲壓壓襯製製 (膚憲齋簾糧鑰觸憲鹽膚 ) | 积极 | 2011-11-08 | |||
L-type CCB | 選窪鹹淵壓膚構築蓋顧(構鬱鹽艱醖壓構壓醖獵) = 鏇積製壓鏇蓋壓壓鬱蓋 醖選遞壓憲壓壓襯製製 (膚憲齋簾糧鑰觸憲鹽膚 ) |
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