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Drugs. 2019 Sep;79(14):1583-1590. doi: 10.1007/s40265-019-01195-w.
Trifluridine/tipiracil (Lonsurf) is a fixed-dose combination tablet comprising trifluridine, an antineoplastic nucleoside analogue, and tipiracil, a thymidine phosphorylase inhibitor. Trifluridine/tipiracil has recently been granted an additional indication in the USA for the treatment of metastatic gastric cancer, including gastroesophageal junction adenocarcinoma, in patients who have been previously treated with at least two systemic treatment regimens, and has received a positive opinion for this indication in the EU. In the large pivotal phase III TAGS trial, trifluridine/tipiracil plus best supportive care (BSC) significantly prolonged overall survival (OS; primary endpoint) compared with placebo plus BSC in this patient group. Progression-free survival (PFS) and the disease control rate were also improved with trifluridine/tipiracil relative to placebo. Health-related quality of life was not adversely affected by the addition of trifluridine/tipiracil to BSC and time to deterioration of Eastern Cooperative Oncology Group (ECOG) performance status was significantly delayed. The most common adverse events were mainly haematological (neutropenia, leucopenia and anaemia) and gastrointestinal (nausea, vomiting and diarrhoea), and were generally manageable with dosage modifications and/or supportive care. Adverse events ≥ Grade 3 were most frequently haematological in nature. Thus, trifluridine/tipiracil provides a valuable and much needed treatment option for patients with metastatic gastric or gastroesophageal junction adenocarcinoma that has progressed on at least two prior therapies.
替拉氟嘧啶/曲氟尿苷（Lonsurf）是一种固定剂量的复方片剂，包含替拉氟嘧啶（一种抗肿瘤核苷类似物）和曲氟尿苷（胸苷磷酸化酶抑制剂）。替拉氟嘧啶/曲氟尿苷最近在美国获得了另一个适应症，用于治疗转移性胃癌，包括胃食管交界处腺癌，适用于至少接受过两种全身治疗方案的患者，并且在欧盟获得了这一适应症的积极意见。在大型关键性 III 期 TAGS 试验中，与安慰剂加最佳支持治疗（BSC）相比，替拉氟嘧啶/曲氟尿苷加 BSC 显著延长了该患者群体的总生存期（OS；主要终点）。与安慰剂相比，无进展生存期（PFS）和疾病控制率也得到了改善。替拉氟嘧啶/曲氟尿苷加 BSC 并未对健康相关生活质量产生不利影响，并且 ECOG 体能状态恶化的时间也明显延迟。最常见的不良反应主要是血液学的（中性粒细胞减少症、白细胞减少症和贫血）和胃肠道的（恶心、呕吐和腹泻），通常可以通过剂量调整和/或支持性护理来管理。≥3 级的不良反应最常见的是血液学性质。因此，替拉氟嘧啶/曲氟尿苷为至少接受过两种先前治疗的转移性胃或胃食管交界处腺癌患者提供了一种有价值且非常需要的治疗选择。
