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ACS 化学神经科学分子特写：Telcagepant（MK-0974）。

ACS chemical neuroscience molecule spotlight on Telcagepant (MK-0974).

机构信息

Department of Pharmacology and Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Vanderbilt University, Nashville, Tennessee 37232-6600, USA.

出版信息

ACS Chem Neurosci. 2011 Jul 20;2(7):334-5. doi: 10.1021/cn200059f.

DOI:10.1021/cn200059f
PMID:22816019
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3369750/
Abstract

Telcagepant (MK-0974) is a novel calcitonin gene-related peptide (CGRP) receptor antagonist currently undergoing clinical trials for migraine (http://www.merck.com/research/pipeline/home.html). MK-0974 is currently being studied in phase III clinical trials.

摘要

特利加压素（MK-0974）是一种新型降钙素基因相关肽（CGRP）受体拮抗剂，目前正在进行偏头痛临床试验（http://www.merck.com/research/pipeline/home.html）。MK-0974 目前正在进行 III 期临床试验研究。

相似文献

1
ACS chemical neuroscience molecule spotlight on Telcagepant (MK-0974).ACS 化学神经科学分子特写：Telcagepant（MK-0974）。
ACS Chem Neurosci. 2011 Jul 20;2(7):334-5. doi: 10.1021/cn200059f.
2
Is there an inherent limit to the efficacy of calcitonin gene-related peptide receptor antagonists in the acute treatment of migraine? A comment.降钙素基因相关肽受体拮抗剂在偏头痛急性治疗中的疗效是否存在固有限制？评论。
J Headache Pain. 2009 Dec;10(6):389-91. doi: 10.1007/s10194-009-0157-8. Epub 2009 Sep 25.
3
Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial.降钙素基因相关肽受体新型口服拮抗剂MK-0974（替卡普坦）与佐米曲普坦治疗急性偏头痛的疗效及耐受性比较：一项随机、安慰剂对照、平行治疗试验
Lancet. 2008 Dec 20;372(9656):2115-23. doi: 10.1016/S0140-6736(08)61626-8. Epub 2008 Nov 25.
4
CGRP receptor antagonists: an expanding drug class for acute migraine?降钙素基因相关肽受体拮抗剂：急性偏头痛治疗的新兴药物类别？
Expert Opin Investig Drugs. 2012 Jun;21(6):807-18. doi: 10.1517/13543784.2012.681044. Epub 2012 Apr 19.
5
Telcagepant, a calcitonin gene-related peptide antagonist for the treatment of migraine.替卡格雷泮，一种用于治疗偏头痛的降钙素基因相关肽拮抗剂。
Curr Opin Investig Drugs. 2009 Jul;10(7):711-20.
6
Calcitonin gene-related peptide (CGRP) receptor antagonists in the treatment of migraine.降钙素基因相关肽（CGRP）受体拮抗剂在偏头痛治疗中的应用。
CNS Drugs. 2010 Jul;24(7):539-48. doi: 10.2165/11534920-000000000-00000.
7
Excellent tolerability but relatively low initial clinical efficacy of telcagepant in migraine.曲坦类药物替拉那肽治疗偏头痛的耐受性良好，但初始临床疗效相对较低。
Headache. 2011 Jan;51(1):118-23. doi: 10.1111/j.1526-4610.2010.01797.x. Epub 2010 Nov 10.
8
Optimal balance of efficacy and tolerability of oral triptans and telcagepant: a review and a clinical comment.口服曲坦类药物和替利加喷与耐受性的最佳平衡：综述和临床评论。
J Headache Pain. 2011 Jun;12(3):275-80. doi: 10.1007/s10194-011-0309-5. Epub 2011 Feb 25.
9
Molecule of the month. Telcagepant.本月分子。替卡格雷泮。
Drug News Perspect. 2009 Mar;22(2):115.
10
Comparison of the vasoconstrictor effects of the calcitonin gene-related peptide receptor antagonist telcagepant (MK-0974) and zolmitriptan in human isolated coronary arteries.比较降钙素基因相关肽受体拮抗剂 telcagepant（MK-0974）和佐米曲普坦在人离体冠状动脉中的血管收缩作用。
J Cardiovasc Pharmacol. 2010 May;55(5):518-21. doi: 10.1097/FJC.0b013e3181d7665f.

引用本文的文献

1
CGRP receptor activity in mice with global expression of human receptor activity modifying protein 1.在全身性表达人受体活性修饰蛋白1的小鼠中的降钙素基因相关肽受体活性
Br J Pharmacol. 2017 Jun;174(12):1826-1840. doi: 10.1111/bph.13783. Epub 2017 Apr 22.

本文引用的文献

1
Excellent tolerability but relatively low initial clinical efficacy of telcagepant in migraine.曲坦类药物替拉那肽治疗偏头痛的耐受性良好，但初始临床疗效相对较低。
Headache. 2011 Jan;51(1):118-23. doi: 10.1111/j.1526-4610.2010.01797.x. Epub 2010 Nov 10.
2
Antimigraine efficacy of telcagepant based on patient's historical triptan response.基于患者既往曲坦类药物反应的替拉那肽的抗偏头痛疗效。
Headache. 2011 Jan;51(1):64-72. doi: 10.1111/j.1526-4610.2010.01790.x. Epub 2010 Nov 4.
3
New drugs in migraine treatment and prophylaxis: telcagepant and topiramate.偏头痛治疗和预防的新药：telcagepant 和托吡酯。
Lancet. 2010 Aug 21;376(9741):645-55. doi: 10.1016/S0140-6736(10)60323-6. Epub 2010 Apr 21.
4
Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial.降钙素基因相关肽受体新型口服拮抗剂MK-0974（替卡普坦）与佐米曲普坦治疗急性偏头痛的疗效及耐受性比较：一项随机、安慰剂对照、平行治疗试验
Lancet. 2008 Dec 20;372(9656):2115-23. doi: 10.1016/S0140-6736(08)61626-8. Epub 2008 Nov 25.
5
Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).用于治疗偏头痛的强效口服生物可利用降钙素基因相关肽受体拮抗剂：N-[(3R,6S)-6-(2,3-二氟苯基)-2-氧代-1-(2,2,2-三氟乙基)氮杂环庚烷-3-基]-4-(2-氧代-2,3-二氢-1H-咪唑并[4,5-b]吡啶-1-基)哌啶-1-甲酰胺（MK-0974）的发现
J Med Chem. 2007 Nov 15;50(23):5564-7. doi: 10.1021/jm070668p. Epub 2007 Oct 11.
6
The global burden of headache: a documentation of headache prevalence and disability worldwide.全球头痛负担：全球头痛患病率与残疾情况的记录。
Cephalalgia. 2007 Mar;27(3):193-210. doi: 10.1111/j.1468-2982.2007.01288.x.
7
CGRP may play a causative role in migraine.降钙素基因相关肽（CGRP）可能在偏头痛中起致病作用。
Cephalalgia. 2002 Feb;22(1):54-61. doi: 10.1046/j.1468-2982.2002.00310.x.
8
The relative role of genetic and environmental factors in migraine without aura.遗传和环境因素在无先兆偏头痛中的相对作用。
Neurology. 1999 Sep 22;53(5):995-9. doi: 10.1212/wnl.53.5.995.
9
Vasoactive peptide release in the extracerebral circulation of humans during migraine headache.偏头痛发作时人体脑外循环中血管活性肽的释放
Ann Neurol. 1990 Aug;28(2):183-7. doi: 10.1002/ana.410280213.