[Antiangiogenic and antimetastatic effects of toremifene citrate]

M Okada1, A Ogasawara, K Sekine

  • 1Research and Development Division, Nippon Kayaku Co., Ltd.

Insights

Toremifene citrate (TOR) effectively inhibits human endothelial cell functions, suppressing angiogenesis and metastasis in preclinical models. Clinical doses may offer anti-angiogenic and anti-metastatic benefits alongside anti-tumor effects.

Area of Science:

  • Oncology
  • Pharmacology
  • Cell Biology

Context:

  • Angiogenesis is crucial for tumor growth and metastasis.
  • Toremifene citrate (TOR) is an established anti-estrogen therapy.
  • Investigating novel therapeutic applications of TOR beyond estrogen-dependent cancers.

Purpose:

  • To evaluate the anti-angiogenic and anti-metastatic potential of toremifene citrate (TOR).
  • To determine the in vitro and in vivo efficacy of TOR in suppressing endothelial cell functions and tumor spread.

Summary:

  • Toremifene citrate (TOR) inhibited human umbilical vein endothelial cell (HUVEC) tube formation and migration in vitro.
  • TOR suppressed angiogenesis in rabbit cornea models and reduced lung metastasis of fibrosarcoma HT-1080 cells in nude mice.
  • Effective TOR concentrations (5 microM in vitro) are achievable with a 120 mg/day oral dose.

Impact:

  • TOR demonstrates significant anti-angiogenic and anti-metastatic properties.
  • Clinical application of 120 mg/day TOR may enhance cancer treatment by targeting angiogenesis and metastasis.
  • Suggests a broader therapeutic role for TOR in managing cancer progression.

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