[Antitumor Molecular Mechanism of Trifluridine and Tipiracil Hydrochloride (TAS-102: TFTD)]

Hiroyuki Kitao1, Kazuaki Matsuoka, Makoto Iimori

  • 1Dept. of Molecular Oncology, Graduate School of Medical Sciences, Kyushu University.

Insights

Treatment with TAS-102 (trifluridine/tipiracil) significantly improves survival for patients with metastatic colorectal cancer (mCRC) resistant to chemotherapy. This drug offers a new option for difficult-to-treat mCRC cases.

Area of Science:

  • Oncology
  • Pharmacology
  • Clinical Trials

Background:

  • Metastatic colorectal cancer (mCRC) patients refractory to standard chemotherapy have limited treatment options.
  • TAS-102 (trifluridine/tipiracil) is an investigational drug showing promise in this patient population.

Purpose of the Study:

  • To review the clinical development history of TAS-102 (TFTD).
  • To elucidate the molecular mechanism of action of TAS-102 and its component trifluridine.

Main Methods:

  • A global, multicenter, randomized, double-blind, phase III study (RECOURSE) was conducted.
  • Patient outcomes, including overall survival and safety, were evaluated.

Main Results:

  • TAS-102 (TFTD) significantly improved overall survival in mCRC patients refractory to standard chemotherapy (HR=0.68, p<0.001).
  • The drug demonstrated a favorable safety profile.

Conclusions:

  • TAS-102 (TFTD) is an important new treatment option for salvage-line therapy in mCRC.
  • Regulatory reviews are underway in the US and Europe following its approval in Japan.

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