Department of Internal Medicine I, University Medical Centre of the Johannes Gutenberg-University, Langenbeckstrasse 1, 55131 Mainz, Germany.
Nat Rev Gastroenterol Hepatol. 2014 Jul;11(7):447-52. doi: 10.1038/nrgastro.2014.10. Epub 2014 Feb 4.
The antiangiogenic multikinase inhibitor sorafenib was the first systemic agent to demonstrate a significant improvement in the overall survival of patients with advanced hepatocellular carcinoma (HCC), thereby introducing molecularly-targeted therapy in a therapeutic field of unmet needs. However, survival benefits for patients on sorafenib treatment are modest in clinical practice and advancing the field is far more challenging than initially anticipated. Molecular and clinical heterogeneity diminishes signals of potential activity in unselected populations, and underlying liver cirrhosis seals the fate of many novel targeted agents by causing relevant toxicity and mortality. The failure of subsequent randomized controlled phase III trials underscores the urgent need to identify the driver targets and to develop matched active agents with manageable toxicities in specific phase I studies in patients with cirrhosis. Refinement of phase II-III trial designs with a biomarker-enriched patient-selection process and stratification according to prognostic baseline factors is indispensable to prevent another 5-year vain endeavour in systemic therapy of HCC.
多激酶抑制剂索拉非尼是首个能显著提高晚期肝细胞癌(HCC)患者总生存期的系统治疗药物,从而在这一尚未满足需求的治疗领域引入了分子靶向治疗。然而,索拉非尼治疗患者的生存获益在临床实践中并不显著,并且推进这一领域的进展比最初预期的更加具有挑战性。分子和临床异质性降低了在未经选择的人群中潜在活性的信号,而潜在的肝硬化则通过引起相关毒性和死亡率来决定许多新型靶向药物的命运。随后的随机对照 III 期临床试验的失败突显了迫切需要在肝硬化患者的特定 I 期研究中确定驱动靶点,并开发具有可管理毒性的匹配活性药物。通过生物标志物富集的患者选择过程和根据预后基线因素进行分层来完善 II-III 期试验设计,对于防止 HCC 系统治疗中又一个 5 年徒劳无益的努力是必不可少的。