预约演示
更新于：2025-02-06
Ticlopidine Hydrochloride
盐酸噻氯匹定
更新于：2025-02-06
概要
基本信息
药物类型 小分子化药 |
别名 Ticlopidine hydrochloride (JP17/USP)、Tiolopidine Hydrochloride、4-C-32 + [20] |
作用机制 P2Y12 receptor拮抗剂(嘌呤P2Y12受体拮抗剂) |
治疗领域 |
在研适应症 |
非在研适应症- |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 日本 (1981-06-04), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C14H15Cl2NS |
InChIKeyMTKNGOHFNXIVOS-UHFFFAOYSA-N |
CAS号53885-35-1 |
关联
5
项与 盐酸噻氯匹定 相关的临床试验NCT03298906
A Fixed-sequence, Open-label Study to Assess the Effect of Ticlopidine on the Pharmacokinetics, Safety, and Tolerability of Intranasally Administered Esketamine in Healthy Subjects
NCT02133989
Ticlopidine+Ginkgo Biloba Versus Clopidogrel in Clopidogrel Resistant Patients Undergoing Cartoid Artery Stent Placement
NCT01214941
Effect of Itraconazole and Ticlopidine on the Pharmacokinetics and Pharmacodynamics of Oral Tramadol
100 项与 盐酸噻氯匹定 相关的临床结果
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100 项与 盐酸噻氯匹定 相关的转化医学
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100 项与 盐酸噻氯匹定 相关的专利（医药）
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3,888
项与 盐酸噻氯匹定 相关的文献（医药）2025-01-01JOURNAL OF PHARMACEUTICAL SCIENCES
Dissolution profiles of high-dose salt-form drugs in bicarbonate buffer and phosphate buffer
Article
作者: Sugano, Kiyohiko ; Tarumi, Yuki
The purpose of the present study was to compare the dissolution profiles of high-dose salt-form drugs in bicarbonate buffer (BCB) and phosphate buffer (PPB) focusing on the pH changes in the bulk phase. The pH titration curves of BCB and PPB (pH 6.5, buffer capacity (β) = 4.4 mmol/L/pH unit) were first theoretically calculated and experimentally validated. For dissolution tests, six drug salts with an acid counterion, one drug salt with a weak base counterion, and one free acid drug were employed (125-800 mg clinical dose). The dose/fluid volume ratio (Dose/FV) was aligned with the clinical condition. In the pH titration study, the pH value decreased below pH 6.0 by adding HCl > 2.8 mmol/L (BCB) or > 1.6 mmol/L (PPB) and increased above pH 7.0 by adding NaOH > 2.0 mmol/L (BCB) or > 2.4 mmol/L (PPB). In the dissolution test, even though the initial pH and β values were the same, the pH value at 4 h was lower in PPB than in BCB in all cases. For the drug salts with an acid counterion, the area under the dissolution curve was 1.2 to 2.6-fold lower in BCB than in PPB. A marked precipitation process was observed in BCB, but less pronounced or absent in PPB. The results of this study suggest the use of BCB and a clinically equivalent Dose/FV may be valuable in predicting the oral absorption of high-dose drug salts.
2024-12-31JOURNAL OF DERMATOLOGICAL TREATMENT
Risk of neutropenia in psoriasis patients prescribed anti-IL-23 antibody in comparison with anti-IL-17 antibody or adalimumab based on real-world data from the MID-NET
®
in Japan
Article
作者: Okada, Yusuke ; Nonaka, Takahiro ; Horiuchi, Naoya ; Komiyama, Noriyuki ; Kajiyama, Kazuhiro ; Komaki, Tomomi ; Ishiguro, Chieko ; Iguchi, Toyotaka ; Kuga, Wataru ; Uyama, Yoshiaki
BACKGROUND:
To evaluate the risk of neutropenia during treatment with anti-IL-23 antibodies in patients with psoriasis.
METHOD:
We conducted an observational study with cohort design using MID-NET® in Japan. We identified patients with psoriasis who were newly prescribed anti-IL-23 antibodies, anti-IL-17-antibodies, adalimumab, or apremilast between January 1, 2009, and March 31, 2021. We estimated the adjusted hazard ratio (aHR) of anti-IL-23 antibodies compared to that of anti-IL-17 antibodies, adalimumab, or apremilast, for the risk of grade 2 (neutrophil count < 1,500/μL) or grade 3 (neutrophil count < 1,000/μL) neutropenia.
RESULTS:
Overall, 287 patients on anti-IL-23 antibodies, 189 patients on anti-IL-17 antibodies, 293 patients on adalimumab, and 540 patients on apremilast were included. Compared with anti-IL-17 antibodies, the aHR (95% confidence interval (CI)) of anti-IL-23 antibodies was 0.83 (0.27-2.51) for grade 2 and 0.40 (0.02-7.60) for grade 3 neutropenia; that when compared with adalimumab was 0.76 (0.28-2.06) for grade 2 but was not calculated for grade 3 as no cases were found; and that compared with apremilast was 3.88 (0.62-24.48) for grade 2 and 0.43 (0.02-11.63) for grade 3 neutropenia.
CONCLUSION:
No clear increase in the risk of neutropenia with anti-IL-23 antibodies was observed.
2024-12-04Journal of the American Chemical Society
Rapid Exploration of Chemical Space by High-Throughput Desorption Electrospray Ionization Mass Spectrometry
Article
作者: Morato, Nicolás M. ; Cooks, R. Graham ; Feng, Yunfei ; Toney, Alexis ; Huang, Kai-Hung
This study leverages accelerated reactions at the solution/air interface of microdroplets generated by desorption electrospray ionization (DESI) to explore the chemical space. DESI is utilized to synthesize drug analogs at an overall rate of 1 reaction mixture per second, working on the low-nanogram scale. Transformations of multiple drug molecules at specific functionalities (phenol, hydroxyl, amino, carbonyl, phenyl, thiophenyl, and alkenyl) are achieved using electrophilic/nucleophilic, redox, C-H functionalization, and coupling reactions. These transformations occur under ambient conditions on the millisecond time scale with direct detection of products being successful in all but three of the reaction types studied. The large scope (22 bioactive compounds, >20 chemical transformations, and >300 functionalization reagents) and high speed (>3000 reactions/hour) provide access to a wide array of drug analogs that can be used for bioactivity testing. A total of ∼6800 unique reactions were examined through a data-driven workflow, and more than 3000 unique derivatives (∼44%) were identified tentatively by the m/z value and signal-to-control ratio in single-stage mass spectrometry (MS) analysis, with over 1000 being further characterized by tandem MS. The speed of the DESI-MS reaction screen provides potential advantages for emerging machine learning-based predictions of organic synthesis, and it sets the stage for future online DESI-MS bioassays and scaled-up microdroplet synthesis before formal characterization of hit compounds is sought using traditional methods of drug discovery.
100 项与 盐酸噻氯匹定 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 血栓栓塞 | 日本 | 1981-06-04 |
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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
N/A | - | 702 | 夢積艱鬱鑰齋鑰襯窪鹽(顧糧築獵簾觸蓋憲餘蓋) = 鑰蓋鏇範積選廠簾鏇簾 製網製遞顧築壓餘憲選 (糧願鬱齋夢壓襯醖壓鬱 ) 更多 | 积极 | 2012-05-01 | ||
(Control) | 衊襯艱膚築艱壓獵網醖(製廠齋蓋齋衊築壓蓋鏇) = 壓餘壓遞襯窪願鏇遞範 觸鹹網醖糧遞餘襯鬱壓 (鹹網齋糧鑰範製遞簾蓋 ) 更多 | ||||||
临床3期 | 22 | 鏇網醖膚醖餘廠鏇鏇襯(廠構構膚鑰網顧築範觸) = 襯衊鑰鑰簾範鏇夢鬱窪 壓蓋選蓋糧簾獵願積糧 (憲衊遞鏇顧製壓蓋願繭, 醖簾蓋膚餘遞餘膚繭製 ~ 遞壓遞觸範淵願網積餘) 更多 | - | 2012-04-05 |
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