TAS-102 is an orally administered combination of trifluridine and Tipiracil hydrochloride in a molar ratio of 1:0.5. Trifluridine is the active antitumor component of TAS-102; its monophosphate form inhibits thymidylate synthase, and its triphosphate form is incorporated into DNA in tumor cells.
In vivo, TAS-102 monotherapy has a significant antitumor activity against KM12C/5-FUFU-bearing nude mice. TAS-102 can overcome acquired resistance to 5-FU because the main mechanism of TAS-102 is not associated with main metabolic enzymes of 5-FU, such as TS and OPRT. TAS-102 has demonstrated efficacy in 5-FU-refractory cancers.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 10 mg/mL warmed|
TAS-102: a novel antimetabolite for the 21st century.
Uboha N, et al. Future Oncol. 2016 Jan;12(2):153-63. PMID: 26616466.
TAS-102, a novel antitumor agent: a review of the mechanism of action.
Lenz HJ, et al. Cancer Treat Rev. 2015 Nov;41(9):777-83. PMID: 26428513.
Exposure-dependent incorporation of trifluridine into DNA of tumors and white blood cells in tumor-bearing mouse.
Yamashita F, et al. Cancer Chemother Pharmacol. 2015 Aug;76(2):325-33. PMID: 26084259.
Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, with irinotecan hydrochloride on human colorectal and gastric cancer xenografts.
Nukatsuka M, et al. Anticancer Res. 2015 Mar;35(3):1437-45. PMID: 25750295.
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