TAS-102

For research use only.

Catalog No.S8539 Synonyms: Trifluridine-Tipiracil Hydrochloride Mixture

TAS-102 Chemical Structure

CAS No. 733030-01-8

TAS-102 (Trifluridine-Tipiracil Hydrochloride Mixture) is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.

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Biological Activity

Description TAS-102 (Trifluridine-Tipiracil Hydrochloride Mixture) is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.
In vitro

TAS-102 is an oral combination drug consisting of trifluridine (FTD), which is a thymidine-based nucleoside analog, and tipiracil hydrochloride (TPI), which improves the bioavailability of FTD by inhibiting its catabolism by thymidine phosphorylase (TP)[1]. Phosphorylated form of trifluridine is incorporated into DNA resulting in DNA dysfunction and cell cycle arrest. Thymidine phosphorylase inhibitor inhibits degradation of FTD and inhibits angiogenesis. Thus, TAS-102 treatment results in massive trifluridine incorporation into DNA and in activation of similar DNA damage response pathways, which involve phosphorylation of Chk1 and cycle arrest during the G2/M-phase[2].

In vivo The elimination half-life of FTD after intravenous administration to humans is very rapid (18 minutes), due to the rapid degradation of FTD to its major metabolite, 5-trifluoromethyl-2,4(1H,3H)-pyrimidinedione. In monkeys, the plasma FTD level after oral administration alone is very low, suggesting extensive first-pass metabolism by the liver and intestine TPase. However, the addition of TPI(tipiracil hydrochloride) is found to enable oral administration. By inhibiting TP, TPI inhibits the degradation of FTD in the liver and intestines following oral administration and thereby improves its bioavailability. The TP enzyme catalyzes the phosphorolysis of pyrimidine 2'-deoxynucleosides such as FTD. Studies using human CRC tumor xenografts in mice determine that the maximum antitumor activity is achieved with a 1:0.5 molar ratio, and studies in mice and monkeys show that the maximum plasma concentration of FTD is almost achieved with the same ratio. Moreover, this ratio produces a favorable balance between antitumor activity and toxicity. Lower toxicity in mice is observed with TPI coadministration than with FTD alone. TAS-102 (FTD) 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[1].

Protocol

Animal Research:

[2

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  • Animal Models: Male nude mice
  • Dosages: 150 mg/kg/day
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (114.74 mM)
Water 15 mg/mL warmed (17.21 mM)
Ethanol ''100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 871.52
Formula

C10H11F3N2O5.C9H11ClN4O2.HCl

CAS No. 733030-01-8
Storage powder
in solvent
Synonyms Trifluridine-Tipiracil Hydrochloride Mixture
Smiles Cl.OCC1OC(CC1O)N2C=C(C(=O)NC2=O)C(F)(F)F.OCC3OC(CC3O)N4C=C(C(=O)NC4=O)C(F)(F)F.ClC5=C(CN6CCCC6=N)NC(=O)NC5=O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04868773 Recruiting Drug: Cabozantinib|Drug: TAS-102 Colorectal Cancer|Colorectal Carcinoma|Metastatic Cancer|CRC University of California Irvine July 2021 Phase 1
NCT04074343 Recruiting Drug: TAS-102|Drug: Irinotecan Gastric Adenocarcinoma|GastroEsophageal Cancer University of California Irvine|Taiho Pharmaceutical Co. Ltd. August 26 2019 Phase 1
NCT03810742 Recruiting Drug: Nanoliposomal Irinotecan Refractory Solid Tumors PharmaEngine March 5 2019 Phase 1
NCT03717038 Withdrawn Drug: Sym004|Drug: TAS-102 Metastatic Colorectal Cancer|Colorectal Cancer Metastatic|Carcinoma Symphogen A/S February 2019 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID