For research use only. Not for therapeutic Use.
Tegafur (INN) is a chemotherapeutic 5-FU prodrug used in the treatment of cancers. It is a component of tegafur-uracil. When metabolized, it becomes 5-FU. T egafur-uracil is a formulated therapeutic oral agent consisting of a combination of the 5-fluorouracil (5-FU) congener prodrug tegafur (tetrahydrofuranyl-5-fluorouracil) and uracil (1:4). The high concentration of uracil reversibly inhibits the uracil-reducing enzyme dihydropyrimidine dehydrogenase (DPD), thereby inhibiting first-pass DPD-mediated hepatic metabolism of the uracil analogue 5-FU and permitting administration of 5-FU as the orally bioavailable prodrug tegafur. Tegafur is bioactivated to 5-FU by liver microsomal cytochrome P450 enzymes.
| Catalog Number | A000295 |
| CAS Number | 17902-23-7 |
| Synonyms | Fluorafur |
| Molecular Formula | C8H9FN2O3 |
| Purity | ≥95% |
| Target | Nucleoside Antimetabolite/Analog |
| Solubility | >8.9mg/mL in DMSO |
| Storage | 3 years -20C powder |
| Reference | </br>1: Kim J, Kim SH, Lee MG, Chung KY, Kim DS. Eccrine Squamous Syringometaplasia of Underlying Syringoma Associated with Tegafur/Gimeracil/Oteracil (TS-1). Acta Derm Venereol. 2015 Mar 13. doi: 10.2340/00015555-2092. [Epub ahead of print] PubMed PMID: 25766447.</br>2: Maolake A, Izumi K, Takahashi R, Itai S, Machioka K, Yaegashi H, Nohara T, Kitagawa Y, Kadono Y, Konaka H, Mizokami A, Namiki M. Efficacy of Tegafur-Uracil in Advanced Urothelial Cancer Patients after the Treatment Failure of Platinum-based Chemotherapy. Anticancer Res. 2015 Mar;35(3):1603-6. PubMed PMID: 25750316.</br>3: Suda H, Kochi M, Fujii M, Kanamori N, Mihara Y, Tamegai H, Funada T, Watanabe M, Takayama T. Complete response to uracil-tegafur alone in advanced rectal cancer. Hepatogastroenterology. 2014 Nov-Dec;61(136):2212-4. PubMed PMID: 25699353.</br>4: Sakaguchi I, Motohara T, Saito F, Takaishi K, Fukumatsu Y, Tohya T, Shibata S, Mimori H, Tashiro H, Katabuchi H. High-dose oral tegafur-uracil maintenance therapy in patients with uterine cervical cancer. J Gynecol Oncol. 2015 Feb 17. [Epub ahead of print] PubMed PMID: 25686399.</br>5: Wang HF, Lv JQ. The Clinical Evaluation of Tegafur Gimeracil Oteracil Combined with THP and DDP for Second-Line Treatment of Advanced Cardiac Carcinoma. Cell Biochem Biophys. 2015 Jan 25. [Epub ahead of print] PubMed PMID: 25618173.</br>6: Ishizuna K, Ninomiya J, Ogawa T, Kojima M, Tsuji E, Kawashima M, Nozaki M, Yamagishi H, Ueda Y. Effectiveness and safety of tegafur-gimeracil-oteracil potassium (TS-1) for metastatic breast cancer: a single-center retrospective study. Gan To Kagaku Ryoho. 2014 Dec;41(13):2577-82. PubMed PMID: 25596051.</br>7: Eguchi K, Oyama T, Tajima A, Abiko T, Sawafuji M, Horio H, Hashizume T, Matsutani N, Kato R, Nakayama M, Kawamura M, Kobayashi K. Intratumoral gene expression of 5-fluorouracil pharmacokinetics-related enzymes in stage I and II non-small cell lung cancer patients treated with uracil-tegafur after surgery: a prospective multi-institutional study in Japan. Lung Cancer. 2015 Jan;87(1):53-8. doi: 10.1016/j.lungcan.2014.10.013. Epub 2014 Nov 3. PubMed PMID: 25468199.</br>8: Inoue K, Sugiura F, Kogita A, Yoshioka Y, Sukegawa Y, Hida J, Okuno K. [Clinical trial of a seven-peptide vaccine and tegafur-uracil/leucovorin as combination therapy for advanced colorectal cancer]. Gan To Kagaku Ryoho. 2014 Oct;41(10):1276-9. Japanese. PubMed PMID: 25335716.</br>9: Shiono S, Harada M, Abiko M, Sato T, Takanashi I. [A case of recurrent lung cancer with bone metastases treated with tegafur-uracil and zoledronic acid for long-term survival]. Gan To Kagaku Ryoho. 2014 Jun;41(6):757-9. Japanese. PubMed PMID: 25129089.</br>10: Yamamiya I, Yoshisue K, Ishii Y, Yamada H, Yoshida K. Species variation in the enantioselective metabolism of tegafur to 5-fluorouracil among rats, dogs and monkeys. J Pharm Pharmacol. 2014 Dec;66(12):1686-97. doi: 10.1111/jphp.12304. Epub 2014 Aug 13. PubMed PMID: 25117829.</br> |
