Cytestrol acetate
Chemical compound / From Wikipedia, the free encyclopedia
Cytestrol acetate is a steroidal antiestrogen and a cytostatic antineoplastic agent (i.e., chemotherapeutic) which was developed for the treatment of breast cancer but was never marketed.[1][2][3][4]
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Other names | 11α-Hydroxyethinylestradiol 3-(bis(2-chloroethyl)carbamate) 11α,17β-diacetate; 17α-Ethynylestra-1,3,5(10)-triene-3,11α,17β-triol 11α,17β-diacetate 3-(bis(2-chloroethyl)carbamate) |
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Chemical and physical data | |
Formula | C29H35Cl2NO6 |
Molar mass | 564.50 g·mol−1 |
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It is an 11α-hydroxylated derivative of ethinylestradiol in which a bis(2-chloroethyl)amine nitrogen mustard moiety has been attached as an ester at the C3 position and acetate esters have been attached at the C11α and C17β positions.[1][2][3][4] The mechanism of action of cytestrol acetate in breast cancer is two-fold: (1) acting as an antiestrogen similarly to fulvestrant or ICI-164384; and (2) having cytostatic actions via the carbamate–nitrogen mustard moiety analogously to estramustine phosphate.[1][2][3][4] The drug shows potent efficacy against breast cancer superior to that of tamoxifen in in vitro models.[1][2][3]