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拉帕替尼:在治疗人表皮生长因子受体 2 过表达、曲妥珠单抗耐药、晚期或转移性乳腺癌中的应用评价。

Lapatinib: a review of its use in the treatment of HER2-overexpressing, trastuzumab-refractory, advanced or metastatic breast cancer.

机构信息

Adis, Auckland, New Zealand.

出版信息

Drugs. 2009 Oct 22;69(15):2125-48. doi: 10.2165/11203240-000000000-00000.

DOI:10.2165/11203240-000000000-00000
PMID:19791830
Abstract

Lapatinib (Tyverb, Tykerb) is an orally active, small molecule, reversible, dual tyrosine kinase inhibitor of human epidermal growth factor receptor type 1 (HER1) and type 2 (HER2). In the EU, lapatinib in combination with capecitabine is indicated for the treatment of women with HER2-overexpressing, advanced or metastatic breast cancer that has progressed after treatment with regimens that include anthracyclines, taxanes and, in the metastatic setting, trastuzumab. The orally administered combination of lapatinib and capecitabine was a more effective treatment than capecitabine alone, and was a generally well tolerated, conveniently administered combination for women with trastuzumab-refractory, HER2-positive advanced or metastatic breast cancer in a clinical trial. Lapatinib combined with capecitabine provides an effective therapeutic option for a group of patients who currently have few treatment choices.

摘要

拉帕替尼(泰立沙,泰克布)是一种口服活性、小分子、可逆的、人表皮生长因子受体 1(HER1)和 2(HER2)的双重酪氨酸激酶抑制剂。在欧盟,拉帕替尼联合卡培他滨用于治疗人表皮生长因子受体 2(HER2)过表达的、晚期或转移性乳腺癌,这些患者在接受包含蒽环类药物、紫杉烷类药物和转移性曲妥珠单抗的方案治疗后疾病进展。与卡培他滨单药治疗相比,拉帕替尼联合卡培他滨口服治疗更有效,并且在临床试验中,对于曲妥珠单抗耐药、HER2 阳性的晚期或转移性乳腺癌的女性患者,是一种耐受性良好、使用方便的联合治疗方案。拉帕替尼联合卡培他滨为目前治疗选择有限的一组患者提供了有效的治疗选择。

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Br J Clin Pharmacol. 2009 Apr;67(4):421-6. doi: 10.1111/j.1365-2125.2009.03370.x.
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