TAS-103 has been reported to be a potent topoisomerase II poison. TAS-103 showed the strongest antitumor activity among the conventional anticancer agents for colorectal cancer (p<0.05). The combination with CDDP augmented the antitumor activity of TAS-103 (p<0.05), indicating that CDDP is one of the most potent candidates to be used in combination with TAS-103. TAS-103 may be useful in the chemotherapy of colorectal cancer. TAS-103 is a novel type of anticancer agent with a unique mechanism and could be useful as a lead compound for development of new drugs.TAS-103 will be expected to show excellent antitumor activities against a wide range of human tumors. TAS-103 showed the strongest antitumor activity among the conventional anticancer agents for colorectal cancer (p<0.05).
|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||Water 40 mg/mL|
Promising antitumor activity of a novel quinoline derivative, TAS-103, against fresh clinical specimens of eight types of tumors measured by flow cytometric DNA analysis.
Fujimoto S. Biol Pharm Bull. 2007 Oct;30(10):1923-9. PMID: 17917263.
In vitro antitumor activity of TAS-103 against freshly-isolated human colorectal cancer.
Tsunoda T, et al. Anticancer Res. 2001 Nov-Dec;21(6A):3897-902. PMID: 11911266.
A dual topoisomerase inhibitor, TAS-103, induces apoptosis in human cancer cells.
Ohyama T, et al. Jpn J Cancer Res. 1999 Jun;90(6):691-8. PMID: 10429663.
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