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Review
. 2021 Apr 29:13:17588359211009001.
doi: 10.1177/17588359211009001. eCollection 2021.

Oral drugs in the treatment of metastatic colorectal cancer

Pilar García-Alfonso  1 , Andrés Jesús Muñoz Martín  2 , Laura Ortega Morán  2 , Javier Soto Alsar  2 , Gabriela Torres Pérez-Solero  2 , Montserrat Blanco Codesido  2 , Pilar Aitana Calvo Ferrandiz  2 , Silvina Grasso Cicala  3
Affiliations
Review

Oral drugs in the treatment of metastatic colorectal cancer

Pilar García-Alfonso et al. Ther Adv Med Oncol. .

Abstract

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.

Keywords: S-1; TAS-102; UFT; adjuvant; capecitabine; colorectal cancer; first-line; metastatic.

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Conflict of interest statement

Conflict of interest statement: The authors declare relevant conflicts of interest relating to: consultancy services or participation in advisory boards (*); speaking engagements (†); receipt of research funding (‡); support for attendance at congresses or other events (including travel and accommodation) (§); employment of self or a close family member (#); and participation in speaker bureaux (¶); for the following named commercial entities. Pilar García-Alfonso: Amgen*†, Bayer*, Bristol-Myers Squibb*, Celgene*, Ipsen*†, Lilly*†, Merck*†, MSD*, Roche*†, Sanofi* and Servier*†. Andrés Jesús Muñoz Martín: Bayer¶, Bristol-Myers Squibb*, Celgene*§, Daiichi-Sankyo*, Eli Lilly¶, Halozyme*, Leo Pharma*‡, MSD¶, Pfizer*, Roche§, Rovi¶, Sanofi*‡ and Servier¶. Dr Muñoz Martín also declares ownership of and receipt of royalties in relation to patents and other intellectual property in respect of a risk assessment model for venous thromboembolism in patients with cancer. Laura Ortega Morán: Amgen†§, Leo Pharma†§, Roche§ and Sanofi*†§ Javier Soto Alsar: Angelini§, MSD§, Pfizer§#, Rovi§, Roche§, Sanofi# and Vifor Pharma§ Gabriela Torres Pérez-Solero: Amgen†, Ipsen§, Lilly§, Merck†§, Pfizer§, Roche†§, Servier†, Sanofi† and Advanced Accelerator Applications, a Novartis owned company*§ Montserrat Blanco Codesido: Astellas‡, Beigene‡, Bristol-Myers Squibb‡, Ipsen†§, Lilly†‡§ and Roche§ Silvina Grasso Cicala: Servier# Pilar Aitana Calvo Ferrandiz declares no conflicts of interest.

Figures

Figure 1.
Figure 1.
Therapies available for the treatment of metastatic colorectal cancer. Unshaded: drugs administered by injection; shaded: oral drugs. 5-FU, 5-fluoruracil; FTD/TPI, trifluridine/tipiracil; S-1, tegafur/gimeracil/oteracil; UFT, tegafur/uracil.
See this image and copyright information in PMC

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