The potential for a novel pure anti-oestrogen.
ICI 164,384 is a novel agent, which has all the characteristics of a pure anti-oestrogen in preclinical studies. It completely inhibited oestradiol or tamoxifen-induced uterine growth in immature rats. In intact rats, ICI 164,384 produced a reduction in uterine weight, almost equivalent to that in ovariectomised rats. ICI 164,384 also demonstrated a peripherally selective action in intact rats. ICI 164,384 has a high affinity for the oestrogen receptor and was more effective than tamoxifen in blocking proliferation of MCF-7 human breast cancer cells. Extrapolation of these observations to the therapy of breast cancer would imply that a pure anti-oestrogen might provide additional benefit, compared with Nolvadex, in terms of onset, duration or completeness of response.
Wakeling
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ICI Pharmaceuticals, Macclesfield, Cheshire, UK.
D000818:Animals; D001943:Breast Neoplasms / Q000503:physiopathology; D002460:Cell Line; D004958:Estradiol / Q000031:analogs & derivatives* / Q000494:pharmacology; D004965:Estrogen Antagonists / Q000494:pharmacology*; D005260:Female; D006801:Humans; D053284:Polyunsaturated Alkamides; D051381:Rats; D011960:Receptors, Estrogen / Q000187:drug effects*; D013629:Tamoxifen / Q000494:pharmacology*; D014599:Uterus / Q000187:drug effects*
D004965:Estrogen Antagonists; D053284:Polyunsaturated Alkamides; D011960:Receptors, Estrogen; D013629:Tamoxifen; D004958:Estradiol; C051781:ICI 164384