Princess Margaret Hospital, Toronto, Ontario, M5G2M9 Canada.
Expert Opin Investig Drugs. 2011 Apr;20(4):577-86. doi: 10.1517/13543784.2011.565329. Epub 2011 Mar 11.
Angiogenesis inhibition represents a rational therapeutic strategy in the management of solid tumors. Brivanib is a dual tyrosine kinase inhibitor with selectivity against VEFGR-2 and FGFR.
This review provides an updated summary of preclinical and clinical experience with brivanib in cancer. Data presented in abstract form from international conferences or journal articles found with a PubMed search of published literature up to December 2010 are described in this review.
Brivanib appears tolerable and exhibits favorable pharmacokinetic and pharmacodynamic profiles with evidence of target inhibition in surrogate tissues. Clinical and pharmacodynamic data support an oral once daily administration at 800 mg. Brivanib shows promising activity as single agent in hepatocellular carcinoma and in combination with cetuximab in colorectal cancer. Further evaluations with cytotoxic chemotherapy and in other solid tumors are currently ongoing.
血管生成抑制在实体瘤的治疗中是一种合理的治疗策略。Brivanib 是一种双重酪氨酸激酶抑制剂，对 VEGFR-2 和 FGFR 具有选择性。
本综述提供了关于 Brivanib 在癌症中的临床前和临床经验的最新总结。本综述中描述的是在国际会议上以摘要形式呈现的数据，或使用 PubMed 搜索已发表文献中找到的期刊文章。
Brivanib 具有良好的耐受性，表现出有利的药代动力学和药效学特征，在替代组织中具有靶标抑制的证据。临床和药效学数据支持每日一次口服 800mg 的给药方案。Brivanib 作为单一药物在肝细胞癌中显示出有希望的活性，并且与西妥昔单抗联合在结直肠癌中显示出活性。目前正在进行与细胞毒性化疗和其他实体瘤的进一步评估。
