PMID- 33995592 OWN - NLM STAT- PubMed-not-MEDLINE LR - 20230920 IS - 1758-8340 (Print) IS - 1758-8359 (Electronic) IS - 1758-8340 (Linking) VI - 13 DP - 2021 TI - Oral drugs in the treatment of metastatic colorectal cancer. PG - 17588359211009001 LID - 10.1177/17588359211009001 [doi] LID - 17588359211009001 AB - 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. CI - (c) The Author(s), 2021. FAU - Garcia-Alfonso, Pilar AU - Garcia-Alfonso P AUID- ORCID: 0000-0002-4373-9978 AD - Oncologia Medica, Hospital General Universitario Gregorio Maranon, Calle Doctor Esquerdo 46, Madrid, 28009, Spain. FAU - Munoz Martin, Andres Jesus AU - Munoz Martin AJ AD - Oncologia Medica, Hospital General Universitario Gregorio Maranon, Madrid, Spain. FAU - Ortega Moran, Laura AU - Ortega Moran L AD - Oncologia Medica, Hospital General Universitario Gregorio Maranon, Madrid, Spain. FAU - Soto Alsar, Javier AU - Soto Alsar J AD - Oncologia Medica, Hospital General Universitario Gregorio Maranon, Madrid, Spain. FAU - Torres Perez-Solero, Gabriela AU - Torres Perez-Solero G AD - Oncologia Medica, Hospital General Universitario Gregorio Maranon, Madrid, Spain. FAU - Blanco Codesido, Montserrat AU - Blanco Codesido M AD - Oncologia Medica, Hospital General Universitario Gregorio Maranon, Madrid, Spain. FAU - Calvo Ferrandiz, Pilar Aitana AU - Calvo Ferrandiz PA AD - Oncologia Medica, Hospital General Universitario Gregorio Maranon, Madrid, Spain. FAU - Grasso Cicala, Silvina AU - Grasso Cicala S AD - Medical Affairs Servier, Madrid, Spain. LA - eng PT - Journal Article PT - Review DEP - 20210429 PL - England TA - Ther Adv Med Oncol JT - Therapeutic advances in medical oncology JID - 101510808 PMC - PMC8111515 OTO - NOTNLM OT - S-1 OT - TAS-102 OT - UFT OT - adjuvant OT - capecitabine OT - colorectal cancer OT - first-line OT - metastatic COIS- Conflict of interest statement: The authors declare relevant conflicts of interest relating to: consultancy services or participation in advisory boards (*); speaking engagements (dagger); receipt of research funding (double dagger); support for attendance at congresses or other events (including travel and accommodation) ( section sign); employment of self or a close family member (#); and participation in speaker bureaux ( paragraph sign); for the following named commercial entities. Pilar Garcia-Alfonso: Amgen*dagger, Bayer*, Bristol-Myers Squibb*, Celgene*, Ipsen*dagger, Lilly*dagger, Merck*dagger, MSD*, Roche*dagger, Sanofi* and Servier*dagger. Andres Jesus Munoz Martin: Bayer paragraph sign, Bristol-Myers Squibb*, Celgene* section sign, Daiichi-Sankyo*, Eli Lilly paragraph sign, Halozyme*, Leo Pharma*double dagger, MSD paragraph sign, Pfizer*, Roche section sign, Rovi paragraph sign, Sanofi*double dagger and Servier paragraph sign. Dr Munoz Martin 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 Moran: Amgendagger section sign, Leo Pharmadagger section sign, Roche section sign and Sanofi*dagger section sign Javier Soto Alsar: Angelini section sign, MSD section sign, Pfizer section sign#, Rovi section sign, Roche section sign, Sanofi# and Vifor Pharma section sign Gabriela Torres Perez-Solero: Amgendagger, Ipsen section sign, Lilly section sign, Merckdagger section sign, Pfizer section sign, Rochedagger section sign, Servierdagger, Sanofidagger and Advanced Accelerator Applications, a Novartis owned company* section sign Montserrat Blanco Codesido: Astellasdouble dagger, Beigenedouble dagger, Bristol-Myers Squibbdouble dagger, Ipsendagger section sign, Lillydaggerdouble dagger section sign and Roche section sign Silvina Grasso Cicala: Servier# Pilar Aitana Calvo Ferrandiz declares no conflicts of interest. EDAT- 2021/05/18 06:00 MHDA- 2021/05/18 06:01 PMCR- 2021/04/29 CRDT- 2021/05/17 06:05 PHST- 2020/12/10 00:00 [received] PHST- 2021/03/17 00:00 [accepted] PHST- 2021/05/17 06:05 [entrez] PHST- 2021/05/18 06:00 [pubmed] PHST- 2021/05/18 06:01 [medline] PHST- 2021/04/29 00:00 [pmc-release] AID - 10.1177_17588359211009001 [pii] AID - 10.1177/17588359211009001 [doi] PST - epublish SO - Ther Adv Med Oncol. 2021 Apr 29;13:17588359211009001. doi: 10.1177/17588359211009001. eCollection 2021.