MK-0974 -: Calcitonin gene-related peptide (CGRP) antagonist antimigraine agent

被引：1

作者：

Wang, Y. ^{[1
]}

Serradell, N. ^{[2
]}

Rosa, E. ^{[2
]}

Bolos, J. ^{[2
]}

机构：

[1] IBC, Frederick, MD 21702 USA

[2] Prous Sci, Barcelona 08080, Spain

来源：

DRUGS OF THE FUTURE | 2008年 / 33卷 / 02期

关键词：

D O I：

10.1358/dof.2008.033.02.1183428

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Calcitonin gene-related peptide (CGRP) has been suggested to play a key role in migraine pathophysiology. MK-0974, an oral CGRP receptor antagonist, is being developed by Merck for the treatment of acute migraine attacks. In preclinical studies, MK-0974 demonstrated high affinity and selectivity for the human CGRP receptor. The agent has favorable pharmacokinetic parameters in animals, including rats, dogs and rhesus monkeys, and humans. MK-0974 was generally well tolerated in clinical studies, and adverse events did not increase with dose. Compared to placebo, MK-0974 significantly improved mean migraine pain relief and pain freedom 2 h after dosing, and the effects on pain freedom were sustained for 24 h. The dose of 300 mg was identified as the most promising.

引用

页码：116 / 122

页数：7

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