Laboratoire de Pharmacocinetique - UFR Pharmacie, 27 Bd Jean Moulin, 13385 Marseille, France.
Curr Top Med Chem. 2012;12(15):1643-8. doi: 10.2174/156802612803531351.
Targeted therapies have dramatically modified treatment strategies in oncology since the early 2000's, especially for treating digestive cancers. These new biotherapies such as anti-VEGF (bevacizumab) or anti-EGFR (cetuximab) monoclonal antibodies have given oncologists new opportunities to use innovative treatment schedules or combinations with cytotoxics. Consequently, significant improvements in response rates, with trends to longer progression-free survival and/or overall survival have been achieved in patients with metastatic colorectal cancer (mCRC). Panitumumab is a novel, 100% human, anti-EGFR1 (HER1) antibody that has been approved in late 2007 for use as monotherapy in mCRC patients resistant to standard chemotherapy, provided that their tumor express EGFR and display wild-type K-Ras status. Panitumumab has been recently further approved in combination with chemotherapy in mCRC patients. However, owing to the fact that its mechanism of action for targeting EGFR is similar to that of chimeric cetuximab, picturing the specificities in pharmacological and pharmacokinetic properties of this 100% human antibody could help the oncologists to better define their strategies at the bedside.
自 21 世纪初以来,靶向治疗在肿瘤学中极大地改变了治疗策略,尤其是在治疗消化系统癌症方面。这些新的生物疗法,如抗血管内皮生长因子(bevacizumab)或抗表皮生长因子受体(cetuximab)单克隆抗体,为肿瘤学家提供了新的机会,使他们可以使用创新的治疗方案或与细胞毒素联合使用。因此,转移性结直肠癌(mCRC)患者的反应率显著提高,无进展生存期和/或总生存期呈延长趋势。帕尼单抗是一种新型的、100%人源化的抗表皮生长因子受体 1(HER1)抗体,于 2007 年末被批准用于对标准化疗耐药的 mCRC 患者的单药治疗,前提是其肿瘤表达 EGFR 且显示野生型 K-Ras 状态。帕尼单抗最近已被进一步批准与化疗联合用于 mCRC 患者。然而,由于其针对 EGFR 的作用机制与嵌合 cetuximab 相似,因此了解这种 100%人源化抗体在药理学和药代动力学特性方面的特异性,可能有助于肿瘤学家更好地制定床边策略。