García-Alfonso Pilar, Muñoz Martín Andrés Jesús, Ortega Morán Laura, Soto Alsar Javier, Torres Pérez-Solero Gabriela, Blanco Codesido Montserrat, Calvo Ferrandiz Pilar Aitana, Grasso Cicala Silvina
Oncología Médica, Hospital General Universitario Gregorio Marañón, Calle Doctor Esquerdo 46, Madrid, 28009, Spain.
Oncología Médica, Hospital General Universitario Gregorio Marañón, Madrid, Spain.
Ther Adv Med Oncol. 2021 Apr 29;13:17588359211009001. doi: 10.1177/17588359211009001. eCollection 2021.
Colorectal cancer (CRC) is one of the most common forms of cancer, with an estimated 1.36 million new cases and almost 700,000 deaths annually. Approximately 21% of patients with CRC have metastatic disease at diagnosis. The objective of this article is to review the literature on the efficacy and safety of oral drugs available for the treatment of metastatic colorectal cancer (mCRC). Several such drugs have been developed, and fluoropyrimidines are the backbone of chemotherapy in this indication. They exert their antitumour activity by disrupting the synthesis and function of DNA and RNA. Oral fluoropyrimidines include prodrugs capecitabine, tegafur, eniluracil/5-fluorouracil, tegafur/uracil, tegafur/gimeracil/oteracil and trifluridine/tipiracil (FTD/TPI). Oral drugs offer several advantages over injectable formulations, including convenience, flexibility, avoidance of injection-related adverse events (AEs) and, in some circumstances, lower costs. However, oral drugs may not be suitable for patients with gastrointestinal obstruction or malabsorption, they may result in reduced treatment adherence and should not be co-administered with drugs that interfere with absorption or hepatic metabolism. Oral fluoropyrimidines such as capecitabine, as monotherapy or in combination with oxaliplatin, irinotecan or bevacizumab, are as effective as intravenous 5-fluorouracil (5-FU) in first-line treatment of mCRC. Other oral fluoropyrimidines, such as FTD/TPI, are effective in patients with mCRC who are refractory, intolerant or ineligible for 5-FU. In addition, oral fluoropyrimidines are used in adjuvant treatment of mCRC. Regorafenib is an oral multikinase inhibitor used in patients in whom several previous lines of therapy have failed. Frequent AEs associated with oral drugs used in the treatment of CRC include hand-foot syndrome and gastrointestinal and haematological toxicities.
结直肠癌（CRC）是最常见的癌症形式之一，估计每年有136万新发病例，近70万人死亡。约21%的CRC患者在诊断时已有转移性疾病。本文的目的是综述可用于治疗转移性结直肠癌（mCRC）的口服药物的疗效和安全性的文献。已经研发了几种此类药物，氟嘧啶是该适应症化疗的基础。它们通过破坏DNA和RNA的合成及功能发挥抗肿瘤活性。口服氟嘧啶包括前体药物卡培他滨、替加氟、依诺拉西/5-氟尿嘧啶、替加氟/尿嘧啶、替加氟/吉美嘧啶/奥替拉西和曲氟尿苷/替匹嘧啶（FTD/TPI）。与注射用制剂相比，口服药物具有多种优势，包括方便、灵活、避免注射相关不良事件（AE），在某些情况下成本更低。然而，口服药物可能不适用于胃肠道梗阻或吸收不良的患者，可能导致治疗依从性降低，并且不应与干扰吸收或肝代谢的药物联合使用。口服氟嘧啶如卡培他滨，作为单药或与奥沙利铂、伊立替康或贝伐单抗联合使用，在mCRC的一线治疗中与静脉注射5-氟尿嘧啶（5-FU）一样有效。其他口服氟嘧啶，如FTD/TPI，对难治、不耐受或不符合使用5-FU条件的mCRC患者有效。此外，口服氟嘧啶用于mCRC的辅助治疗。瑞戈非尼是一种口服多激酶抑制剂，用于先前多线治疗失败的患者。与用于治疗CRC的口服药物相关的常见AE包括手足综合征以及胃肠道和血液学毒性。
