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Besides colorectal cancer, it has also shown antitumor activity in other cancers such as breast, head and neck, pancreatic, gastrointestinal, and solid brain tumors. A prodrug of 5\u2010fluorouracil (5\u2010FU), carmofur has shown better gastrointestinal stability and superior antiproliferative activity compared to its active counterpart 5\u2010FU. Recently, carmofur has gained attention as an acid ceramidase inhibitor and as a potential lead compound against several noncancerous diseases such as coronavirus disease 2019, Krabbe disease, acute lung injury, Parkinson's disease, dementia, childhood ependymoma etc. Carmofur has also been reported to have antifungal, and antimicrobial properties. Nevertheless, no comprehensive review is available on this drug. Herein, we summarized the chemistry, pharmacokinetics, and pharmacology of carmofur based on the literature published between January 1976 and March 2022 as identified from <jats:italic>PubMed<\/jats:italic> and <jats:italic>Google Scholar<\/jats:italic> search engines.<\/jats:p>","DOI":"10.1002\/ddr.21984","type":"journal-article","created":{"date-parts":[[2022,8,29]],"date-time":"2022-08-29T01:39:25Z","timestamp":1661737165000},"page":"1505-1518","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":22,"title":["Versatile use of Carmofur: A comprehensive review of its chemistry and pharmacology"],"prefix":"10.1002","volume":"83","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-6248-3229","authenticated-orcid":false,"given":"Mohammad Mohiminul","family":"Islam","sequence":"first","affiliation":[{"name":"Department of Chemistry and Biochemistry University of Wisconsin\u2013Milwaukee Milwaukee Wisconsin USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0897-710X","authenticated-orcid":false,"given":"Shama P.","family":"Mirza","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biochemistry University of Wisconsin\u2013Milwaukee Milwaukee Wisconsin USA"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2022,8,28]]},"reference":[{"issue":"3","key":"e_1_2_14_2_1","first-page":"2115","article-title":"Apoptosis and p53 overexpression in human rectal cancer; relationship with response to hyperthermo\u2010chemo\u2010radiotherapy","volume":"21","author":"Abe T.","year":"2001","journal-title":"Anticancer Research"},{"key":"e_1_2_14_3_1","doi-asserted-by":"publisher","DOI":"10.1007\/s004010050482"},{"key":"e_1_2_14_4_1","doi-asserted-by":"publisher","DOI":"10.1136\/jnnp.2007.123737"},{"key":"e_1_2_14_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejca.2020.09.014"},{"key":"e_1_2_14_6_1","doi-asserted-by":"publisher","DOI":"10.1186\/s13023-019-1018-4"},{"key":"e_1_2_14_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejps.2015.12.005"},{"key":"e_1_2_14_8_1","doi-asserted-by":"publisher","DOI":"10.1038\/ncomms15432"},{"key":"e_1_2_14_9_1","doi-asserted-by":"crossref","unstructured":"Clifford R. 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