Albini Adriana, Cesana Eugenio, Donatelli Francesco, Cammarota Rosaria, Bucci Eraldo O, Baravelli Massimo, Anzà Claudio, Noonan Douglas M
Oncology Research Division, Polo Scientifico e Tecnologico-IRCCS MultiMedica, Via Fantoli 16/15-20138, Milan, Italy.
Future Cardiol. 2011 Sep;7(5):693-704. doi: 10.2217/fca.11.54.
The HER family of tyrosine kinase receptors includes several members that are clinically important targets in cancer therapies, in particular HER1 (the EGF receptor) and HER2, other members include HER3 and HER4. Trastuzumab, a humanized monoclonal antibody and lapatinib, a tyrosine kinase inhibitor, are drugs that target HER2, which is highly expressed in 20-30% of breast cancers. Trastuzumab is recommended as an adjuvant therapy for lymph node positive, HER2-positive breast cancers, or node-negative cancer with high-risk of recurrence, as well as in stage IV cancers. One serious side effect of trastuzumab is cardiomyocyte dysfunction, resulting in reduced heart contractile efficiency. The incidence of collateral effects on the heart with trastuzumab therapy increases in people with cardiovascular risk factors, heart disease and when combined with other chemotherapeutics. When cardiotoxicity was observed with trastuzumab, several studies have addressed potential cardiac damage of trastuzumab itself and lapatinib. The differences in cardiovascular effects of these two compounds are somewhat unexpected and suggest distinct mechanisms of action, which have clear implications in clinical application and prevention of cardiotoxicity in cardio-oncological approaches.
酪氨酸激酶受体的HER家族包括几个成员,它们是癌症治疗中临床上重要的靶点,特别是HER1(表皮生长因子受体)和HER2,其他成员包括HER3和HER4。曲妥珠单抗,一种人源化单克隆抗体,和拉帕替尼,一种酪氨酸激酶抑制剂,都是靶向HER2的药物,HER2在20%-30%的乳腺癌中高表达。曲妥珠单抗被推荐作为淋巴结阳性、HER2阳性乳腺癌,或有高复发风险的淋巴结阴性癌症以及IV期癌症的辅助治疗。曲妥珠单抗的一个严重副作用是心肌细胞功能障碍,导致心脏收缩效率降低。曲妥珠单抗治疗对心脏产生副作用的发生率在有心血管危险因素、心脏病的人群中以及与其他化疗药物联合使用时会增加。当观察到曲妥珠单抗引起心脏毒性时,多项研究探讨了曲妥珠单抗本身和拉帕替尼潜在的心脏损害。这两种化合物在心血管效应方面的差异有些出人意料,提示了不同的作用机制,这对临床应用以及心脏肿瘤学方法中心脏毒性的预防具有明确的意义。