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【drug-news】辉瑞全球停售抗肺动脉高血压药西他
美国辉瑞制药有限公司10日宣布将治疗肺动脉高血压的药物西他生坦紧急撤出市场，并停止对该药开展的所有临床试验，因为这种药可能引起肝损伤，严重时可致患者死亡。
据辉瑞公司介绍，西他生坦既未在中国销售，也没有进入中国的医学临床试验。
辉瑞在一份声明中说，该公司已经撤回了西他生坦在美国的销售申请，并将这种药从欧盟、加拿大和澳大利亚的市场撤出。
声明说，辉瑞对临床试验数据和市场销售报告进行评估后发现，西他生坦可能会引起肝损伤。在临床试验中，已有两名患者在服用这种药后死亡。
声明建议服用西他生坦或正在参与这种药物临床试验的患者尽快咨询医疗专家，在有其他药物可以选择的情况下，最好不要服用西他生坦。
NEW YORK (AP) - Pfizer Inc. said Friday it is pulling its blood pressure drug Thelin off the market and stopping all clinical trials because the drug can cause fatal liver damage.
Thelin is sold in the European Union, Canada, and Australia as an oral treatment for severe pulmonary arterial hypertension, or high blood pressure in the pulmonary artery. Pfizer said two patients who were taking Thelin died during a clinical trial, and a review of data from clinical studies and post-marketing reports showed a new link to liver injury.
Liver damage was a known side effect of Thelin and similar drugs, the company said, but the review uncovered a link to liver damage that was not tied to identifiable risk factors. It said the problem was unlikely to be detected by routine monitoring, and in some cases, the problems did not go away after patients stopped taking Thelin.
Pfizer said the withdrawal was voluntary and added that it has withdrawn its filing for marketing approval in the U.S.
Since there are other treatment options, Pfizer said the benefits of Thelin don't outweigh the risks. It is stopping all studies of the drug, which Pfizer acquired in 2008 when it bought Encysive Pharmaceuticals Inc. Encysive had been trying to win marketing approval for Thelin since 2005, but the Food and Drug Administration said it was not effective enough. Other agencies only approved the drug for hypertension that was so debilitating that patients' physical activity was severely limited.
The New York company said worldwide sales of Thelin, or sitaxsentan, totaled $44.4 million in the first nine months of 2010.
In afternoon trading, shares of Pfizer added 12 cents to $16.88.
(Copyright 2010 The Associated Press. All rights reserved. This material may not be published, broadcast, rewritten or redistributed.) 辉瑞公司发言人艾伦说，因为Thelin与一种“罕见和难以预料”的新肝脏问题有关，所以公司决定将其撤出市场。
http://en.wikipedia.org/wiki/Sitaxentan 导读：1.商品名:Thelin 通用名:sitaxsentan sodium 3.适应证:本品适用于治疗肺动脉高压(PAH).本品由美国EncysiivePharmaceuticals公司开发
1.商品名:Thelin
通用名:sitaxsentan sodium
2.开发与上市厂商
本品由美国EncysiivePharmaceuticals公司开发.2006年11月在英国首次上市12月在德国上市。LGLifeScienoes公司获得本品在亚洲市场(不包括日本)的授权，Encysive公司保留欧洲、北美和日本市场的权利。（ Pfizer to acquire Encysive Pharmaceuticals）
3.适应证
本品适用于治疗肺动脉高压(PAH).
4.药理作用
内皮素(ET)-1是肺脏血管中旁分泌和自分泌的强力收缩肤.能促进纤维化、细胞增生和心脏肥厚。以H患者的血浆和肺组织内ET-1浓度异常升高,而ET-1通过其受体A(ETA)作用于肌肉细胞通过受体B(ET作用于内皮细胞。ETA的主要作用是血管收缩和再造.而ETB的主要作用是血管扩张和抗增生作用。当PAH患者体内缺乏ET-1受体阻断剂时，ET-1浓度升高与疾病的严重程度和预后密切相关。本品是有效且高选择性的ETA受体阻断剂.对ETA的选择性比对ETB高6500倍从而产生血管舒张作用。
本品口服后迅速吸收，4小时内达血药峰浓度。绝对生物利用度为70%一100%。当与高脂餐同服本品的吸收率(Cm})比空腹时降低430/0.Tmax延迟(增加2倍)。本品的血浆蛋白(白蛋白)结合率超过99%.且不受浓度影响。本品不渗入红细胞，且不透过血脑屏障。健康志愿者口服本品后可高度代谢。在体外.本品主要经CYP2C9和CYP3A4代谢。本品口服剂量的50%-60%随尿液排泄,其余随粪便排泄.其中原药不足1%,终末消除T1/2为10小时。
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作者:admin@医学,生命科学 2010-12-27 00:02
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