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Ticlopidine

Clopidogrel

Prasugrel

Thienopyridines are a class of selective, irreversible^[1] ADP receptor/P2Y12 inhibitors used for their anti-platelet activity.

Examples

Drugs in this class are: prasugrel (Effient),^[2] ticlopidine (Ticlid), and clopidogrel (Plavix).

Alternatives

Ticagrelor (Brilinta) is often listed with thienopyridine inhibitors and has similar indications for use but is not a thienopyridine. It is a cyclo-pentyltriazolo-pyrimidine that reversibly inhibits the P2Y₁₂ receptor.^[1]

References

^ ^a ^b Alexopoulos, Dimitrios (2014). "P2Y12 Receptor Inhibitors in Acute Coronary Syndromes: From the Research Laboratory to the Clinic and Vice Versa". Cardiology 127 (4): 211–219. doi:10.1159/000357399.
^ Angiolillo DJ, Bates ER, Bass TA (August 2008). "Clinical profile of prasugrel, a novel thienopyridine". Am. Heart J. 156 (2 Suppl): S16–22. doi:10.1016/j.ahj.2008.06.005. PMID 18657682.

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UpToDate Contents

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1. 待機的経皮的冠動脈インターベンションのための抗血栓療法：一般的使用 antithrombotic therapy for elective percutaneous coronary intervention general use
2. 非ST上昇型急性冠症候群における抗血小板薬 antiplatelet agents in acute non st elevation acute coronary syndromes
3. 心血管疾患の二次および一次予防におけるアスピリンの利益とリスク benefits and risks of aspirin in secondary and primary prevention of cardiovascular disease
4. 脳卒中の二次予防のための抗血小板療法 antiplatelet therapy for secondary prevention of stroke
5. 待機的経皮的冠動脈インターベンションのための抗血栓療法：臨床研究 antithrombotic therapy for elective percutaneous coronary intervention clinical studies

English Journal

Discovery and structure-activity relationships study of novel thieno[2,3-b]pyridine analogues as hepatitis C virus inhibitors.

Wang NY1, Zuo WQ1, Xu Y1, Gao C1, Zeng XX2, Zhang LD3, You XY3, Peng CT3, Shen Y4, Yang SY1, Wei YQ1, Yu LT5.Author information 1State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.2Department of Pharmaceutical and Bioengineering, School of Chemical Engineering, Sichuan University, Chengdu, Sichuan 610065, China.3State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China; Department of Pharmaceutical and Bioengineering, School of Chemical Engineering, Sichuan University, Chengdu, Sichuan 610065, China.4WuXi PharmaTech Co., Ltd., No. 1 Building, 288 FuTe ZhongLu, WaiGaoQiao Free Trade Zone, Shanghai 200131, China.5State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China. Electronic address: yuluot@scu.edu.cn.AbstractCurrent treatment for hepatitis C is barely satisfactory, there is an urgent need to develop novel agents for combating hepatitis C virus infection. This study discovered a new class of thieno[2,3-b]pyridine derivatives as HCV inhibitors. First, a hit compound characterized by a thienopyridine core was identified in a cell-based screening of our privileged small molecule library. And then, structure activity relationship study of the hit compound led to the discovery of several potent compounds without obvious cytotoxicity in vitro (12c, EC50=3.3μM, SI >30.3, 12b, EC50=3.5μM, SI >28.6, 10l, EC50=3.9μM, SI >25.6, 12o, EC50=4.5μM, SI >22.2, respectively). Although the mechanism of them had not been clearly elucidated, our preliminary optimization of this class of compounds had provided us a start point to develop new anti-HCV agents.
Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2014 Mar 15;24(6):1581-8. doi: 10.1016/j.bmcl.2014.01.075. Epub 2014 Feb 3.
Current treatment for hepatitis C is barely satisfactory, there is an urgent need to develop novel agents for combating hepatitis C virus infection. This study discovered a new class of thieno[2,3-b]pyridine derivatives as HCV inhibitors. First, a hit compound characterized by a thienopyridine core
PMID 24529869

New antithrombotics for secondary prevention of acute coronary syndrome.

Goto S1, Tomita A.Author information 1Department of Medicine (Cardiology), Tokai University School of Medicine, Isehara, Kanagawa, Japan.AbstractPatients with acute coronary syndrome (ACS) usually receive acetylsalicylic acid plus an adenosine diphosphate (ADP) receptor inhibitor to reduce the long-term risk of recurrent events. However, patients receiving standard antiplatelet prophylaxis still face a substantial risk of recurrent events. Strategies involving 3 antithrombotic agents with different modes of action have now been tested. In Thrombin Receptor Antagonists for Clinical Event Reduction (TRA-CER), compared with standard care alone, bleeding complications including intracranial hemorrhage (ICH) were increased with the addition of vorapaxar, without efficacy benefit. In Trial to Assess the Effects of SCH 530348 in Preventing Heart Attack and Stroke in Patients With Atherosclerosis (TRA 2°P-TIMI 50), the addition of vorapaxar reduced recurrent events compared with standard care in stable patients with prior myocardial infarction. This study was terminated early in patients with prior stroke owing to excess ICH, though an increased risk of ICH or fatal bleeding was not detected in patients with prior myocardial infarction. The Apixaban for Prevention of Acute Ischemic and Safety Events 2 (APPRAISE-2) trial of standard-dose apixaban added to standard care in patients with ACS was also stopped early owing to excess serious bleeding. However, in Rivaroxaban in Combination With Aspirin Alone or With Aspirin and a Thienopyridine in Patients With Acute Coronary Syndromes (ATLAS ACS 2 TIMI 51), fatal bleeding or fatal ICH did not increase with low-dose rivaroxaban added to low-dose acetylsalicylic acid-based standard care compared with standard care alone. In that trial, a significant reduction of recurrent vascular events was shown with 3 antithrombotic regimens compared with standard care. Therefore, depending on drug dose and patient population, further reductions in recurrent vascular events after ACS may be possible in future clinical practice, with a favorable benefit-risk profile.
Clinical cardiology.Clin Cardiol.2014 Mar;37(3):178-87. doi: 10.1002/clc.22233. Epub 2014 Jan 22.
Patients with acute coronary syndrome (ACS) usually receive acetylsalicylic acid plus an adenosine diphosphate (ADP) receptor inhibitor to reduce the long-term risk of recurrent events. However, patients receiving standard antiplatelet prophylaxis still face a substantial risk of recurrent events. S
PMID 24452610

Transient receptor potential ankyrin 1 (TRPA1) channel activation by the thienopyridine-type drugs ticlopidine, clopidogrel, and prasugrel.

Schulze A1, Hartung P1, Schaefer M1, Hill K2.Author information 1Rudolf-Boehm-Institute of Pharmacology and Toxicology, Medical Faculty, University of Leipzig, Leipzig, Germany.2Rudolf-Boehm-Institute of Pharmacology and Toxicology, Medical Faculty, University of Leipzig, Leipzig, Germany. Electronic address: kerstin.hill@medizin.uni-leipzig.de.AbstractTransient receptor potential A1 (TRPA1) is widely expressed throughout the human and animal organism, including the dorsal root ganglia as well as the bladder, stomach and small intestine. Here, we examined the effect of three platelet aggregation inhibitors on TRPA1: ticlopidine, clopidogrel and prasugrel. Utilising fluorometric Ca2+ influx analysis and electrophysiological whole cell measurements in TRPA1-expressing HEK293 and in human enterochromaffin-like QGP-1 cells, we found that ticlopidine, clopidogrel and prasugrel are direct activators of TRPA1. Although this polymodal channel commonly contributes to the perception of pain, temperature and chemical irritants, recent studies provide evidence for its involvement in the release of serotonin (5-HT) from enterochromaffin cells. Therefore, we further investigated the ability of ticlopidine, clopidogrel and prasugrel to stimulate 5-HT release from QGP-1 cells. We could determine 5-HT in supernatants from cultured QGP-1 cells upon treatment with ticlopidine and clopidogrel but not with prasugrel. These findings indicate that a robust TRPA1 activation by ticlopidine and clopidogrel correlates with the stimulatory effect on the secretion of 5-HT. As recipients of ticlopidine and clopidogrel frequently complain about gastrointestinal adverse events such as nausea, vomiting and diarrhoea, an activation of TRPA1 may contribute to adverse effects of such drugs in the digestive system.
Cell calcium.Cell Calcium.2014 Feb 25. pii: S0143-4160(14)00036-0. doi: 10.1016/j.ceca.2014.02.014. [Epub ahead of print]
Transient receptor potential A1 (TRPA1) is widely expressed throughout the human and animal organism, including the dorsal root ganglia as well as the bladder, stomach and small intestine. Here, we examined the effect of three platelet aggregation inhibitors on TRPA1: ticlopidine, clopidogrel and pr
PMID 24636274

Japanese Journal

Dual Antiplatelet Therapy for Coronary Artery Disease

Circulation Journal 79(2), 255-262, 2015
NAID 130004927081

新規抗血小板剤の可能性

循環器内科 76(6), 585-588, 2014-12
NAID 40020298922

Dual Antiplatelet Therapy for Coronary Artery Disease

Circulation Journal advpub(0), 2014
NAID 130004927148

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