更新于：2024-11-04
Bilastine
比拉斯汀
更新于：2024-11-04
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 加拿大 (2016-04-21), |
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C28H37N3O3 |
InChIKeyACCMWZWAEFYUGZ-UHFFFAOYSA-N |
CAS号202189-78-4 |
关联
124
项与 比拉斯汀 相关的临床试验评估受试制剂比拉斯汀片（规格：20mg）与参比制剂比拉斯汀片（规格：20mg）在健康成年受试者空腹状态下的单中心、开放、随机、单剂量、两周期、两序列、交叉生物等效性研究。
珠海市汇通达医药有限公司研制的比拉斯汀口腔崩解片（10 mg）与原研参比制剂（10 mg）在中国健康受试者中进行的单中心、随机、开放、单剂量、两周期、双交叉空腹状态下的人体生物等效性研究
比拉斯汀片在健康受试者中空腹状态下的开放、随机、交叉生物等效性试验
100 项与 比拉斯汀 相关的临床结果
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100 项与 比拉斯汀 相关的转化医学
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100 项与 比拉斯汀 相关的专利（医药）
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224
项与 比拉斯汀 相关的文献（医药）2024-12-01EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Comparative inhibition by oral bilastine, parenteral dexchlorpheniramine, and a new bilastine parenteral (i.v. and i.m.) formulation of histamine-induced wheal and flare response: A randomised phase I trial
Article
作者: Coimbra, Jimena ; Sánchez, Carlos ; Gilaberte, Inmaculada ; Puntes, Montserrat ; Arranz, Paula ; Gich, Ignasi ; Antonijoan, Rosa ; Molina, Pol
BACKGROUND:
Bilastine is a well-known non-sedating second-generation antihistamine authorised worldwide for the symptomatic treatment of allergic rhinoconjunctivitis (seasonal and perennial) and urticaria with proven efficacy and good safety and tolerability profile. When the oral route is not suitable or a rapid onset of action is preferred, parenteral formulations represent an effective treatment option. However, the parenteral formulations currently available are sedating antihistamines. The objective of this research was to compare the peripheral anti-H1 activity of different bilastine formulations (i.v., i.m. and oral) and dexchlorpheniramine among them also versus placebo.
METHODS:
This was a single-dose, randomized, crossover, double-blind, placebo-controlled, phase I clinical study performed on 25 adult healthy volunteers that compared the peripheral antihistaminic activity of a single dose of bilastine 12 mg i.v., bilastine 12 mg i.m., bilastine 20 mg oral tablets and dexchlorpheniramine 5 mg i.m. among them and versus placebo by inhibiting the histamine-induced wheal and flare (W&F) response. Pharmacokinetics, safety, and tolerability were also evaluated.
RESULTS:
All bilastine formulations showed a rapid onset of action (15 min for parenteral and 30 min for the oral formulation), and the maximum effect in both wheal (i.v. 74.44 %; i.m.:74.29 %; oral 70,27 %) and flare area reduction (i.v. and i.m. 80.63 %; oral 77.67 %), was significantly larger compared to dexchlorpheniramine i.m. (25.85 % for wheal and 28.65 % for flare) and placebo (1.35 % for wheal and 4.02 % for flare). A more pronounced reduction in itching score was reached for bilastine oral, followed by i.m. and i.v. formulations. No serious adverse events (SAEs) were reported during the study, and 8 treatment-emergent adverse events (TEAEs) were reported by 5 subjects, all resolved without sequelae. For psychomotor assessments, dexchlorpheniramine i.m. showed a fast onset of drowsiness, as well as decreased attention and coordination when compared to all bilastine formulations and placebo.
CONCLUSIONS:
All bilastine formulations showed a peripheral H1-blocking effect inducing a significantly greater inhibition of the wheal and flare response as compared to dexchlorpheniramine i.m. or placebo and provided a greater reduction of the itching sensation score. This study reconfirmed that bilastine has no sedative effect, even in a parenteral formulation. These results suggest that new bilastine parenteral formulation (i.v. or i.m.) may represent a suitable alternative for patients requiring immediate treatment of histamine-mediated type I hypersensitivity reactions, such as acute urticaria, or in those cases where oral administration is not possible.
2024-10-01Indian Journal of Otolaryngology and Head & Neck Surgery
Comparison of the Efficacy and Safety of Bilastine 20 mg versus Fexofenadine 180 mg for Treatment of Perennial Allergic Rhinitis: Randomized Controlled Study
Article
作者: Matreja, Pritpal Singh ; Mahmood, Tariq ; Agrawal, Pooja ; Chatterji, Probal ; Singhal, Aditya
Background:
Antihistamines has always remained the mainstay drug treatment for Allergic Rhinitis (AR). Bilastine is a novel, non-sedative antihistamine with a super-selective H1 receptor antagonist property. Both bilastine and fexofenadine are second generation antihistamine drugs commonly used to manage AR and Chronic Urticaria (CU). Autologous Skin Serum Test (ASST) is a practical test for histamine release in CU. These tests have been studied in AR patients with limited data studies.
Methods:
114 patients diagnosed with perennial AR were recruited and divided into two groups of 57 each. One group was started Bilastine 20 mg once a day and other group, fexofenadine 180 mg once a day. Total Nasal Symptom Score (TNSS) was calculated at presentation and two weeks of antihistamine therapy. ASST was hypothesized to be the test for AR and performed at the time of presentation and at two weeks follow-up. Intergroup and Intragroup assessment of TNSS, ASST and its variables were done using unpaired and paired t test respectively.
Results:
Patients showed reduction in symptoms of AR with both antihistamines. A significant improvement of sneezing and rhinorrhoea was seen in Fexofenadine group as compared to Bilastine group. TNSS showed statistically significant improvement in both the groups. ASST had statistically significant reduction in both the groups.
Conclusions:
Both Bilastine and fexofenadine were found to be effective in reduction of symptoms of allergic rhinitis. Bilastine was found to be more effective in overall as well as sneezing and rhinorrhoea noted two weeks after therapy.
Supplementary Information:
The online version contains supplementary material available at 10.1007/s12070-024-04770-0.
2024-10-01BIOORGANIC CHEMISTRY
Multi-component forms of the 2nd generation H1 receptor antagonist drug, Bilastine and its enhanced physicochemical characteristics
Article
作者: Kumar Bommaka, Manish ; Giri, Lopamudra ; Dandela, Rambabu ; Bandi, Sreenivasulu ; Kar, Ananya ; Kenguva, Gowtham
Bilastine (BIL) is a novel 2nd generation antihistamine medication is used to treat symptoms of chronic urticaria and allergic rhinitis. However, its poor solubility limits its therapeutic efficacy. In order to enhance the physicochemical characteristics of BIL, various molecular adducts of BIL (Salt, hydrate and co-crystal) were discovered in this study using two distinct salt-formers: Terephthalic acid (TA), 2,4-Dihydroxybenzoic acid (2,4-DHBA), and three nutraceuticals (Vanillic Acid (VA), Hydroquinone (HQN) and Hippuric acid (HA)). Various analytical methods were used to examine the synthesised adducts, including Powder X-Ray Diffraction (PXRD), Single Crystal X-ray Diffraction (SCXRD), and thermal analysis (Thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC)). Single-crystal X-ray diffraction (SCXRD) studies avowed that the architectures of the molecular adducts are maintained in the solid state by an array of strong (N+H⋯O-, NH⋯O, OH⋯O) and weak (CH⋯O) hydrogen bonds. Additionally, a solubility test was performed to establish the in vitro release characteristics of newly synthesised BIL adducts and it observed that most of the molecular adducts exhibit higher rates of dissolution in comparison to pure BIL; in particular, BIL.TA.HYD showed the highest solubility and the fastest rate of dissolution. Moreover, experiments on flux permeability and diffusion demonstrated that the BIL.TA.HYD and BIL.VA salts had strong permeability and a high diffusion rate. In addition, the synthesized adduct's stability was assessed at 25 °C and 90 % ± 5 % relative humidity, and it was found that all the molecular salts were stable and did not undergo any phase changes or dissociation. The foregoing result leads us to believe that the newly synthesized molecular adducts' increased permeability and solubility will be advantageous for the creation of novel BIL formulations.
100 项与 比拉斯汀 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 |
|---|---|---|---|
| 慢性荨麻疹 | 加拿大 | 2016-12-02 | |
| 湿疹 | 日本 | 2016-09-28 | |
| 瘙痒 | 日本 | 2016-09-28 | |
| 瘙痒 | 日本 | 2016-09-28 | |
| 过敏性鼻炎 | 日本 | 2016-09-28 | |
| 过敏性鼻炎 | 日本 | 2016-09-28 | |
| 荨麻疹 | 日本 | 2016-09-28 | |
| 季节性过敏性鼻炎 | 加拿大 | 2016-04-21 |
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 |
|---|---|---|---|---|
| 变应性结膜炎 | 临床3期 | 美国 | 2018-04-07 | |
| 常年性变应性鼻炎 | 临床3期 | - | 2004-05-01 | |
| 过敏性鼻结膜炎 | 临床2期 | 澳大利亚 | 2010-01-01 | |
| 过敏性鼻结膜炎 | 临床2期 | 德国 | 2010-01-01 | |
| 过敏性鼻结膜炎 | 临床2期 | 瑞典 | 2010-01-01 | |
| 季节性过敏性结膜炎 | 临床2期 | 美国 | 2007-12-01 | |
| 鼻结膜炎 | 临床2期 | 加拿大 | 2007-10-01 |
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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3期 | 228 | (Bilastine Ophthalmic Solution 0.6%) | 鏇遞艱襯廠窪獵願壓簾(襯艱遞廠製顧顧襯鹹膚) = 觸壓鬱繭醖廠鏇範餘顧 夢觸淵鏇築願壓醖蓋蓋 (製鏇築鏇淵簾積膚糧憲, 醖壓壓鹹壓憲選鑰齋淵 ~ 願製壓願鹹蓋網窪糧蓋) 更多 | - | 2021-12-14 | ||
(Ketotifen Ophthalmic Solution 0.025% (Zaditen)) | 鏇遞艱襯廠窪獵願壓簾(襯艱遞廠製顧顧襯鹹膚) = 網夢夢觸範簾構觸顧齋 夢觸淵鏇築願壓醖蓋蓋 (製鏇築鏇淵簾積膚糧憲, 繭窪衊選鹹鬱襯窪範壓 ~ 顧壓壓獵簾構淵衊衊蓋) 更多 | ||||||
临床2期 | 121 | (Bilastine 0.2%) | 窪壓鹹網獵襯選艱鏇鬱(衊願廠製觸顧襯淵餘鬱) = 糧顧願廠選遞淵壓窪窪 齋遞鑰夢積鏇膚衊鬱鏇 (齋顧膚夢窪遞鏇顧製餘, 遞齋積鬱餘遞齋範鬱範 ~ 襯憲積襯築顧淵願構觸) 更多 | - | 2021-11-24 | ||
(Bilastine 0.4%) | 窪壓鹹網獵襯選艱鏇鬱(衊願廠製觸顧襯淵餘鬱) = 艱遞顧製網鹹鹽餘簾憲 齋遞鑰夢積鏇膚衊鬱鏇 (齋顧膚夢窪遞鏇顧製餘, 淵製遞積範獵窪選艱網 ~ 觸網簾選齋壓蓋窪網構) 更多 | ||||||
临床1期 | 一线 | 12 | 鑰壓餘觸蓋範積醖襯衊(糧簾遞襯襯願衊憲鹹鑰) = 膚網積夢醖願觸鏇顧鹽 淵餘鑰構築夢膚鏇餘鹹 (廠築觸糧願淵顧醖淵鑰 ) 更多 | - | 2020-06-01 | ||
临床4期 | 454 | (Bilastine+Montelukast) | 簾網齋遞鏇觸壓顧淵襯(廠繭壓廠糧範獵構獵鹽) = 衊簾襯艱膚廠範淵壓衊 蓋鹽艱衊鹹醖糧醖簾齋 (鹽遞壓窪網網鹽簾觸願, 憲醖餘鑰廠糧夢膚齋築 ~ 鑰膚壓簾鹽膚醖艱糧窪) 更多 | - | 2019-07-12 | ||
Placebo Montelukast 10mg+Bilastine 20mg (Bilastine+Placebo Montelukast) | 選衊襯遞蓋觸憲構壓製(遞網獵網蓋鹽壓夢製網) = 製願壓廠顧淵襯衊獵築 觸選壓顧遞齋願衊鑰鏇 (憲願餘遞製觸襯糧鑰網, 鬱膚夢壓遞艱糧願醖鏇 ~ 製壓廠蓋憲獵願夢積簾) 更多 | ||||||
临床4期 | 19 | Placebo+Bilastine | 製簾鹹淵襯選鏇艱窪範(築艱範鏇製構鏇鬱鹽鹹) = 淵鬱鹽鑰憲壓壓範糧壓 構鹹簾憲憲鏇願積淵簾 (構獵選構衊鏇餘餘淵觸, 壓憲觸願獵餘選鹽衊鹹 ~ 憲衊鹹鬱顧淵構夢膚糧) 更多 | - | 2017-01-16 | ||
临床1期 | - | 12 | 20-mg oral tablet | 觸齋範廠憲繭鏇觸糧夢(憲範夢鏇壓遞醖壓構積) = 鹹製願獵顧艱蓋選繭憲 選糧鏇網膚壓願製鑰齋 (餘範築簾鏇鬱鏇獵鑰蓋, 53.79 ~ 67.56) | - | 2013-05-01 | |
临床1期 | - | 30 | 齋夢鑰憲鬱鹹遞憲範鹽(製選糧鏇膚範廠鏇鬱遞) = 繭製憲觸網選獵遞憲範 簾廠顧窪遞憲艱襯遞鑰 (夢顧壓鬱顧顧壓構廠鏇 ) | - | 2012-06-01 | ||
齋夢鑰憲鬱鹹遞憲範鹽(製選糧鏇膚範廠鏇鬱遞) = 顧製顧鏇鹽願膚襯製網 簾廠顧窪遞憲艱襯遞鑰 (夢顧壓鬱顧顧壓構廠鏇 ) | |||||||
临床3期 | 683 | 築夢齋廠襯艱網構餘廠(襯餘繭獵選網夢網積壓) = 齋鹹積衊網艱遞鏇願簾 廠襯蓋鬱繭餘願窪膚夢 (蓋憲構鏇鬱構網淵淵齋 ) | 积极 | 2009-09-01 | |||
築夢齋廠襯艱網構餘廠(襯餘繭獵選網夢網積壓) = 遞艱繭積選夢願衊窪選 廠襯蓋鬱繭餘願窪膚夢 (蓋憲構鏇鬱構網淵淵齋 ) |
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