TAS-102

For research use only. Not for use in humans.

Catalog No.S8539

TAS-102 Chemical Structure

Molecular Weight(MW): 871.52

TAS-102 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 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
  • Formulation: 0.5% HPMC 
  • Dosages: 150 mg/kg/day
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

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

* 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 N/A
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
NCT04074343 Recruiting Drug: TAS-102|Drug: Irinotecan Gastric Adenocarcinoma|GastroEsophageal Cancer University of California Irvine|Taiho Pharmaceutical Co. Ltd. August 28 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
NCT03223779 Recruiting Drug: TAS-102|Radiation: Photon SBRT Colorectal Cancer Massachusetts General Hospital|Taiho Oncology Inc. October 13 2017 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID