U.S. flag

An official website of the United States government

Format

Send to:

Choose Destination

Tegafur response

MedGen UID:
338948
Concept ID:
C1852514
Finding
Synonym: TEGAFUR, POOR METABOLISM OF
Drug:
Tegafur
MedGen UID:
5286
Concept ID:
C0016778
Pharmacologic Substance
A congener of the antimetabolite fluorouracil with antineoplastic activity. Tegafur is a prodrug that is gradually converted to fluorouracil in the liver by the cytochrome P-450 enzyme. Subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by inhibiting thymidylate synthase and reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate. (NCI04) [from NCI]
 
Gene (location): DPYD (1p21.3)
 
OMIM®: 122720

Definition

Tegafur is a chemotherapeutic agent and a member of the fluoropyrimidine group of substances. It is a prodrug of 5-fluorouracil and mainly used to treat solid tumors, such as colorectal, breast and aerodigestive cancers. Dihydropyrimidine dehydrogenase (DPD, encoded by the DPYD gene) is the rate-limiting enzyme for fluoropyrimidine metabolism and is therefore responsible for the detoxification of these types of drugs. Patients who are homozygous for variants in DPYD that lead to a non-functional protein, such as *2A or *13, have a high risk of severe or fatal drug toxicities and may benefit from receiving an alternative chemotherapeutic drug. Patients heterozygous for these variants also have an increased risk for drug toxicities, and reduced dosing is recommended for these individuals. Guidelines regarding the use of pharmacogenomic tests in dosing for tegafur have been published in Clinical Pharmacology and Therapeutics by the Clinical Pharmacogenetics Implementation Consortium (CPIC) and are available on the PharmGKB website. [from PharmGKB]

Professional guidelines

PubMed

Wörmann B, Bokemeyer C, Burmeister T, Köhne CH, Schwab M, Arnold D, Blohmer JU, Borner M, Brucker S, Cascorbi I, Decker T, de Wit M, Dietz A, Einsele H, Eisterer W, Folprecht G, Hilbe W, Hoffmann J, Knauf W, Kunzmann V, Largiadèr CR, Lorenzen S, Lüftner D, Moehler M, Nöthen MM, Pox C, Reinacher-Schick A, Scharl A, Schlegelberger B, Seufferlein T, Sinn M, Stroth M, Tamm I, Trümper L, Wilhelm M, Wöll E, Hofheinz RD
Oncol Res Treat 2020;43(11):628-636. Epub 2020 Oct 23 doi: 10.1159/000510258. PMID: 33099551
Lunenburg CATC, van der Wouden CH, Nijenhuis M, Crommentuijn-van Rhenen MH, de Boer-Veger NJ, Buunk AM, Houwink EJF, Mulder H, Rongen GA, van Schaik RHN, van der Weide J, Wilffert B, Deneer VHM, Swen JJ, Guchelaar HJ
Eur J Hum Genet 2020 Apr;28(4):508-517. Epub 2019 Nov 19 doi: 10.1038/s41431-019-0540-0. PMID: 31745289Free PMC Article
Deenen MJ, Terpstra WE, Cats A, Boot H, Schellens JH
Ann Intern Med 2010 Dec 7;153(11):767-8. doi: 10.7326/0003-4819-153-11-201012070-00023. PMID: 21135311

Recent clinical studies

Etiology

Morizane C, Okusaka T, Mizusawa J, Katayama H, Ueno M, Ikeda M, Ozaka M, Okano N, Sugimori K, Fukutomi A, Hara H, Mizuno N, Yanagimoto H, Wada K, Tobimatsu K, Yane K, Nakamori S, Yamaguchi H, Asagi A, Yukisawa S, Kojima Y, Kawabe K, Kawamoto Y, Sugimoto R, Iwai T, Nakamura K, Miyakawa H, Yamashita T, Hosokawa A, Ioka T, Kato N, Shioji K, Shimizu K, Nakagohri T, Kamata K, Ishii H, Furuse J; members of the Hepatobiliary and Pancreatic Oncology Group of the Japan Clinical Oncology Group (JCOG-HBPOG)
Ann Oncol 2019 Dec 1;30(12):1950-1958. doi: 10.1093/annonc/mdz402. PMID: 31566666
He AB, Peng XL, Song J, Zhang JX, Dong WG, Luo RF, Tang Y
World J Gastroenterol 2015 Apr 14;21(14):4358-64. doi: 10.3748/wjg.v21.i14.4358. PMID: 25892887Free PMC Article
Zohar S, Katsahian S, O'Quigley J
Stat Med 2011 Jul 30;30(17):2109-16. Epub 2011 Feb 23 doi: 10.1002/sim.4121. PMID: 21344473
Shiroyama T, Komuta K, Imamura F, Hirashima T, Kijima T, Tachibana I, Kawase I
Lung Cancer 2011 Oct;74(1):85-8. Epub 2011 Feb 20 doi: 10.1016/j.lungcan.2011.01.017. PMID: 21342712
Koizumi W, Narahara H, Hara T, Takagane A, Akiya T, Takagi M, Miyashita K, Nishizaki T, Kobayashi O, Takiyama W, Toh Y, Nagaie T, Takagi S, Yamamura Y, Yanaoka K, Orita H, Takeuchi M
Lancet Oncol 2008 Mar;9(3):215-21. Epub 2008 Feb 20 doi: 10.1016/S1470-2045(08)70035-4. PMID: 18282805

Diagnosis

Ohmura H, Ito M, Uchino K, Okada C, Tanishima S, Yamada Y, Momosaki S, Komoda M, Kuwayama M, Yamaguchi K, Okumura Y, Nakano M, Tsuchihashi K, Isobe T, Ariyama H, Kusaba H, Oda Y, Akashi K, Baba E
FEBS Open Bio 2020 Jan;10(1):147-157. Epub 2019 Dec 3 doi: 10.1002/2211-5463.12765. PMID: 31736281Free PMC Article
Ishigami H, Fujiwara Y, Fukushima R, Nashimoto A, Yabusaki H, Imano M, Imamoto H, Kodera Y, Uenosono Y, Amagai K, Kadowaki S, Miwa H, Yamaguchi H, Yamaguchi T, Miyaji T, Kitayama J
J Clin Oncol 2018 Jul 1;36(19):1922-1929. Epub 2018 May 10 doi: 10.1200/JCO.2018.77.8613. PMID: 29746229
Okubo K, Uenosono Y, Arigami T, Mataki Y, Matsushita D, Yanagita S, Kurahara H, Sakoda M, Kijima Y, Maemura K, Natsugoe S
Eur J Surg Oncol 2017 Jun;43(6):1050-1055. Epub 2017 Feb 12 doi: 10.1016/j.ejso.2017.01.241. PMID: 28233633
Kubota T, Weisenthal L
Gastric Cancer 2006;9(2):82-7. doi: 10.1007/s10120-006-0366-7. PMID: 16767362
Sasaki T
Gastric Cancer 2003;6 Suppl 1:9-12. doi: 10.1007/s10120-003-0229-4. PMID: 12775013

Therapy

Li C, Tian Y, Zheng Y, Yuan F, Shi Z, Yang L, Chen H, Jiang L, Wang X, Zhao P, Zhang B, Wang Z, Zhao Q, Dong J, Lian C, Xu S, Zhang A, Zheng Z, Wang K, Dang C, Wu D, Chen J, Xue Y, Liang B, Cheng X, Wang Q, Chen L, Xia T, Liu H, Xu D, Zhuang J, Wu T, Zhao X, Wu W, Wang H, Peng J, Hou Z, Zheng R, Chen Y, Yin K, Zhu Z
J Clin Oncol 2025 Feb;43(4):464-474. Epub 2024 Oct 9 doi: 10.1200/JCO.24.00795. PMID: 39383487Free PMC Article
Fukuda M, Funaki S, Yamazaki T, Sato S, Mukae H, Takenoyama M, Fukuoka J, Nabeshima K, Tateyama H, Ashizawa K, Hara M, Seto T, Okumura M, Sugio K
Thorac Cancer 2020 Mar;11(3):693-696. Epub 2020 Feb 5 doi: 10.1111/1759-7714.13319. PMID: 32020735Free PMC Article
Morizane C, Okusaka T, Mizusawa J, Katayama H, Ueno M, Ikeda M, Ozaka M, Okano N, Sugimori K, Fukutomi A, Hara H, Mizuno N, Yanagimoto H, Wada K, Tobimatsu K, Yane K, Nakamori S, Yamaguchi H, Asagi A, Yukisawa S, Kojima Y, Kawabe K, Kawamoto Y, Sugimoto R, Iwai T, Nakamura K, Miyakawa H, Yamashita T, Hosokawa A, Ioka T, Kato N, Shioji K, Shimizu K, Nakagohri T, Kamata K, Ishii H, Furuse J; members of the Hepatobiliary and Pancreatic Oncology Group of the Japan Clinical Oncology Group (JCOG-HBPOG)
Ann Oncol 2019 Dec 1;30(12):1950-1958. doi: 10.1093/annonc/mdz402. PMID: 31566666
Ishigami H, Fujiwara Y, Fukushima R, Nashimoto A, Yabusaki H, Imano M, Imamoto H, Kodera Y, Uenosono Y, Amagai K, Kadowaki S, Miwa H, Yamaguchi H, Yamaguchi T, Miyaji T, Kitayama J
J Clin Oncol 2018 Jul 1;36(19):1922-1929. Epub 2018 May 10 doi: 10.1200/JCO.2018.77.8613. PMID: 29746229
Koizumi W, Narahara H, Hara T, Takagane A, Akiya T, Takagi M, Miyashita K, Nishizaki T, Kobayashi O, Takiyama W, Toh Y, Nagaie T, Takagi S, Yamamura Y, Yanaoka K, Orita H, Takeuchi M
Lancet Oncol 2008 Mar;9(3):215-21. Epub 2008 Feb 20 doi: 10.1016/S1470-2045(08)70035-4. PMID: 18282805

Prognosis

Boku N, Omori T, Shitara K, Sakuramoto S, Yamaguchi K, Kato K, Kadowaki S, Tsuji K, Ryu MH, Oh DY, Oh SC, Rha SY, Lee KW, Chung IJ, Sym SJ, Chen LT, Chen JS, Bai LY, Nakada T, Hagihara S, Makino R, Nishiyama E, Kang YK
Gastric Cancer 2024 Nov;27(6):1287-1301. Epub 2024 Aug 20 doi: 10.1007/s10120-024-01535-0. PMID: 39162872Free PMC Article
Boku N, Ryu MH, Kato K, Chung HC, Minashi K, Lee KW, Cho H, Kang WK, Komatsu Y, Tsuda M, Yamaguchi K, Hara H, Fumita S, Azuma M, Chen LT, Kang YK
Ann Oncol 2019 Feb 1;30(2):250-258. doi: 10.1093/annonc/mdy540. PMID: 30566590Free PMC Article
He AB, Peng XL, Song J, Zhang JX, Dong WG, Luo RF, Tang Y
World J Gastroenterol 2015 Apr 14;21(14):4358-64. doi: 10.3748/wjg.v21.i14.4358. PMID: 25892887Free PMC Article
Shiroyama T, Komuta K, Imamura F, Hirashima T, Kijima T, Tachibana I, Kawase I
Lung Cancer 2011 Oct;74(1):85-8. Epub 2011 Feb 20 doi: 10.1016/j.lungcan.2011.01.017. PMID: 21342712
Koizumi W, Narahara H, Hara T, Takagane A, Akiya T, Takagi M, Miyashita K, Nishizaki T, Kobayashi O, Takiyama W, Toh Y, Nagaie T, Takagi S, Yamamura Y, Yanaoka K, Orita H, Takeuchi M
Lancet Oncol 2008 Mar;9(3):215-21. Epub 2008 Feb 20 doi: 10.1016/S1470-2045(08)70035-4. PMID: 18282805

Clinical prediction guides

Boku N, Omori T, Shitara K, Sakuramoto S, Yamaguchi K, Kato K, Kadowaki S, Tsuji K, Ryu MH, Oh DY, Oh SC, Rha SY, Lee KW, Chung IJ, Sym SJ, Chen LT, Chen JS, Bai LY, Nakada T, Hagihara S, Makino R, Nishiyama E, Kang YK
Gastric Cancer 2024 Nov;27(6):1287-1301. Epub 2024 Aug 20 doi: 10.1007/s10120-024-01535-0. PMID: 39162872Free PMC Article
Morizane C, Okusaka T, Mizusawa J, Katayama H, Ueno M, Ikeda M, Ozaka M, Okano N, Sugimori K, Fukutomi A, Hara H, Mizuno N, Yanagimoto H, Wada K, Tobimatsu K, Yane K, Nakamori S, Yamaguchi H, Asagi A, Yukisawa S, Kojima Y, Kawabe K, Kawamoto Y, Sugimoto R, Iwai T, Nakamura K, Miyakawa H, Yamashita T, Hosokawa A, Ioka T, Kato N, Shioji K, Shimizu K, Nakagohri T, Kamata K, Ishii H, Furuse J; members of the Hepatobiliary and Pancreatic Oncology Group of the Japan Clinical Oncology Group (JCOG-HBPOG)
Ann Oncol 2019 Dec 1;30(12):1950-1958. doi: 10.1093/annonc/mdz402. PMID: 31566666
Kimura K, Itoh Y, Okada T, Nakahara R, Kawamura M, Kubota S, Itoh J, Hiramatsu M, Fujimoto Y, Shibata T, Naganawa S
Anticancer Res 2015 Apr;35(4):2385-90. PMID: 25862904
Ge F, Xu N, Bai Y, Ba Y, Zhang Y, Li F, Xu H, Jia R, Wang Y, Lin L, Xu J
Oncologist 2014 Nov;19(11):1133-4. Epub 2014 Oct 1 doi: 10.1634/theoncologist.2014-0223. PMID: 25273077Free PMC Article
Diasio RB
Oncology (Williston Park) 2000 Oct;14(10 Suppl 9):19-23. PMID: 11098485

Recent systematic reviews

Abdel-Rahman O, Elsayed Z, Elhalawani H
Cochrane Database Syst Rev 2018 Apr 6;4(4):CD011746. doi: 10.1002/14651858.CD011746.pub2. PMID: 29624208Free PMC Article
Chionh F, Lau D, Yeung Y, Price T, Tebbutt N
Cochrane Database Syst Rev 2017 Jul 28;7(7):CD008398. doi: 10.1002/14651858.CD008398.pub2. PMID: 28752564Free PMC Article
Ter Veer E, Mohammad NH, Lodder P, Ngai LL, Samaan M, van Oijen MG, van Laarhoven HW
Gastric Cancer 2016 Jul;19(3):696-712. Epub 2016 Jan 11 doi: 10.1007/s10120-015-0587-8. PMID: 26754295Free PMC Article
Li D, Chen C, Zhou Y, Chen R, Fan X, Bi Z, Li Z, Liu Y
Medicine (Baltimore) 2015 Sep;94(35):e1345. doi: 10.1097/MD.0000000000001345. PMID: 26334891Free PMC Article
Ward S, Kaltenthaler E, Cowan J, Brewer N
Health Technol Assess 2003;7(32):1-93. doi: 10.3310/hta7320. PMID: 14604497

Supplemental Content

Table of contents

    Clinical resources

    Practice guidelines

    • PubMed
      See practice and clinical guidelines in PubMed. The search results may include broader topics and may not capture all published guidelines. See the FAQ for details.
    • Bookshelf
      See practice and clinical guidelines in NCBI Bookshelf. The search results may include broader topics and may not capture all published guidelines. See the FAQ for details.

    Consumer resources

    Recent activity

    Your browsing activity is empty.

    Activity recording is turned off.

    Turn recording back on

    See more...