Ormeloxifene is a non-steroidal Selective Estrogen Receptor Modulator (SERM) that is used as an oral contraceptive.
Recent studies have shown its potent anti-cancer activities in breast, head and neck, and chronic myeloid leukemia
cells. Several in vivo and clinical studies have reported that ormeloxifene possesses an excellent therapeutic index and
has been well-tolerated, without any haematological, biochemical or histopathological toxicity, even with chronic administration.
A reasonably long period of time and an enormous financial commitment are required to develop a lead compound
into a clinically approved anti-cancer drug. For these reasons and to circumvent these obstacles, ormeloxifene is a
promising candidate on a fast track for the development or repurposing established drugs as anti-cancer agents for cancer
treatment. The current review summarizes recent findings on ormeloxifene as an anti-cancer agent and future prospects of
this clinically safe pharmacophore.
Keywords: Breast cancer, cancer, chemo-resistance, chronic myeloid leukemia, contraceptive, head and neck squamous cell
carcinoma, ormeloxifene, ovarian cancer, prostate cancer, SERM.
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