Newly discovered orally active pure antiestrogens |
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Authors: | Kanbe Yoshitake Kim Myung-Hwa Nishimoto Masahiro Ohtake Yoshihito Yoneya Takaaki Ohizumi Iwao Tsunenari Toshiaki Taniguchi Kenji Kaiho Shin-ichi Nabuchi Yoshiaki Araya Hiroshi Kawata Setsu Morikawa Kazumi Jo Jae-Chon Kwon Hee-An Lim Hyun-Suk Kim Hak-Yeop |
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Affiliation: | Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd, 1-135, Komakado, Gotemba, Shizuoka 412-8513, Japan. kanbeyst@chugai-pharm.co.jp |
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Abstract: | In order to develop orally active pure antiestrogens, we incorporated the carboxy-containing side chains into the 7alpha-position of the steroid scaffold and found that 17-keto derivative CH4893237 (12b) functioned as a pure antiestrogen with its oral activity much superior to clinically used pure antiestrogen, ICI182,780. Results from the pharmacokinetic evaluation indicated that the potent antiestrogen activity at oral dosing in mice attributed to both improved absorption from the intestinal wall and metabolic stability in liver. |
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