Fugate Susan E, Cudd Laura A
College of Pharmacy, University of Oklahoma, Oklahoma City, OK 73190-5040, USA.
Ann Pharmacother. 2006 May;40(5):925-30. doi: 10.1345/aph.1G120. Epub 2006 Apr 4.
To review and assess available literature on the chemistry, pharmacology, pharmacodynamics, pharmacokinetics, clinical studies, adverse events, drug interactions, special populations, and dosing and administration for cangrelor, a product in late stage Phase II clinical trials.
A literature search of MEDLINE (1966-March 2006), International Pharmaceutical Abstracts (1970-February 2006), and Cochrane database (first quarter 2006) was conducted using key terms of cangrelor, AR-C69931MX, and P2Y12 receptor antagonist. Bibliographies of relevant articles were reviewed for additional references. The Medicines Company Web site was reviewed, and a company representative was contacted.
Available English-language literature, including abstracts, preclinical studies, clinical trials, and review articles, was reviewed.
Cangrelor is a P2Y12 antagonist under development for treatment of acute coronary syndrome. Cangrelor has been studied as an intravenous infusion in doses of 2 or 4 microg/kg/min. It inhibits platelet aggregation with rapid onset and offset and does not require metabolism for therapeutic activity. Published Phase II trials have demonstrated safety and inhibition of platelet aggregation.
Cangrelor is a promising investigational medication for inhibition of platelet aggregation in acute arterial coronary events. Phase II trials have shown safety and a greater inhibition of platelet aggregation over clopidogrel. Phase III trials will provide more definitive information on clinical efficacy and safety. Until then, the role of cangrelor is uncertain.
回顾和评估有关坎格雷洛的现有文献,内容涉及化学、药理学、药效学、药代动力学、临床研究、不良事件、药物相互作用、特殊人群以及给药剂量和方式,坎格雷洛是一种处于II期临床试验后期阶段的产品。
使用坎格雷洛、AR-C69931MX和P2Y12受体拮抗剂等关键词,对MEDLINE(1966年 - 2006年3月)、国际药学文摘(1970年 - 2006年2月)和Cochrane数据库(2006年第一季度)进行文献检索。查阅相关文章的参考文献以获取更多资料。查阅了 Medicines Company网站,并联系了该公司代表。
查阅了可得的英文文献,包括摘要、临床前研究、临床试验和综述文章。
坎格雷洛是一种正在研发用于治疗急性冠脉综合征的P2Y12拮抗剂。已对坎格雷洛进行了研究,静脉输注剂量为2或4微克/千克/分钟。它能快速起效并终止抑制血小板聚集,且治疗活性无需代谢。已发表的II期试验证明了其安全性和对血小板聚集的抑制作用。
坎格雷洛是一种有前景的用于抑制急性动脉冠脉事件中血小板聚集的研究用药。II期试验已显示出其安全性以及比氯吡格雷对血小板聚集更强的抑制作用。III期试验将提供有关临床疗效和安全性的更确切信息。在此之前,坎格雷洛的作用尚不确定。