a The Institute of Cancer Research , London , SW3 6JB , UK.
b The Gynaecology Unit , The Royal Marsden NHS Foundation Trust , 203 Fulham Road, London , SW3 6JJ , UK.
Expert Opin Investig Drugs. 2017 Sep;26(9):1073-1081. doi: 10.1080/13543784.2017.1353599.
Advanced ovarian cancer remains an unmet clinical need. Angiogenesis is considered a therapeutic target in ovarian cancer, with bevacizumab, a monoclonal antibody against VEGF, being the first drug to show a progression-free survival benefit. Nintedanib is an oral tyrosine kinase inhibitor targeting VEGF receptor 1-3, FGFR 1-3 and PDGFR α and β, which has entered phase III trial development in ovarian cancer. Areas covered: This article reviews the preclinical and clinical efficacy of nintedanib in ovarian cancer, its pharmacokinetic and pharmacodynamics profile, safety issues, together with an overview of clinical trials carried out so far. A literature search was made in PubMed for nintedanib, ovarian cancer, angiogenesis, and on ClinicalTrials.gov site for clinical trials with nintedanib. Expert opinion: An ongoing phase III trial investigating nintedanib combined with first-line chemotherapy in ovarian cancer has shown a statistically significant progression free survival benefit, although there were toxicity issues. The true clinical benefit of nintedanib in ovarian cancer including its optimal treatment setting and dosage still need to be addressed.
高级卵巢癌仍然存在未满足的临床需求。血管生成被认为是卵巢癌的治疗靶点，贝伐单抗是一种针对 VEGF 的单克隆抗体，是第一个显示无进展生存期获益的药物。尼达尼布是一种口服酪氨酸激酶抑制剂，针对 VEGF 受体 1-3、FGFR 1-3 和 PDGFRα和β，已进入卵巢癌的 III 期临床试验开发阶段。
本文综述了尼达尼布在卵巢癌中的临床前和临床疗效、药代动力学和药效学特征、安全性问题，以及迄今为止进行的临床试验概述。在 PubMed 上对尼达尼布、卵巢癌、血管生成进行了文献检索，并在 ClinicalTrials.gov 网站上对尼达尼布的临床试验进行了检索。
一项正在进行的 III 期临床试验表明，尼达尼布联合一线化疗治疗卵巢癌可显著提高无进展生存期，但存在毒性问题。尼达尼布在卵巢癌中的真正临床获益，包括其最佳治疗方案和剂量，仍需进一步研究。
