List of hormonal cytostatic antineoplastic agents

Estramustine phosphate, the only dual hormonal and cytostatic antineoplastic agent to have been marketed. A normustine and phosphate ester of estradiol. Used in the treatment of prostate cancer.

This is a list of dual hormonal and cytostatic antineoplastic agents.

Marketed

Estrogen-based

• Estramustine phosphate (Emcyt, Estracyt; Leo 299, NSC-89199, Ro 21-8837/001; estradiol 3-[bis(2-chloroethyl)carbamate] dihydrogen phosphate) – arrests anaphase stage of cell division ^[1]

Corticosteroid-based

• Prednimustine (Mostarina, Sterecyst; chlorambucil prednisolone ester; prednisolone 21-(4-(4-(bis(2-chloroethyl)amino)phenyl)butanoate))

Never marketed

Estrogen-based

• Alestramustine (estradiol 3-(bis(2-chloroethyl)carbamate) 17β-(L-alaninate))
• Atrimustine (bestrabucil, busramustine; KM-2210; estradiol 3-benzoate 17β-((4-(4-(bis(2-chloroethyl)amino)phenyl)-1-oxobutoxy)acetate)
• Cytestrol acetate (1α-hydroxyethinylestradiol 3-(bis(2-chloroethyl)carbamate) 11α,17β-diacetate)
• Estradiol mustard (NSC-112259; chlorphenacyl estradiol diester; estradiol 3,17β-bis(4-(bis(2-chloroethyl)amino)phenyl)acetate)
• Estramustine (Leo 275, Ro 21–8837; estradiol 3-(bis(2-chloroethyl)carbamate) ester)
• Estromustine (Leo 271 f; estrone-cytostatic complex; estrone 17β-3-N-bis(2-chloroethyl)carbamate)
• ICI-85966 (Stilbostat; diethylstilbestrol bis(di(2-chloroethyl)carbamate)
• Phenestrol (fenestrol; NSC-183736; hexestrol bis[4-[bis(2-chloroethyl)amino]phenylacetate)

Androgen-based

• LS-1727 (nandrolone 17β-N-(2-chloroethyl)-N-nitrosocarbamate)
• Sturamustine (dehydroepiandrosterone 17β-N-(2-chloroethyl)-N-nitrosourea)
• Testifenon (testiphenon, testiphenone; chlorphenacyl dihydrotestosterone ester; dihydrotestosterone 17β-(4-(bis(2-chloroethyl)amino)phenyl)acetate)

Corticosteroid-based

• Cortifen (cortiphen, kortifen, fencoron; chlorphenacyl 11-deoxycortisol ester; 11-deoxycortisol 21-(4-(bis(2-chloroethyl)amino)phenyl)acetate)

References

1. Zhao, Qingjie; Huang, Guozheng (2017), "Anticancer Hybrids", Design of Hybrid Molecules for Drug Development, Elsevier, pp. 193–218, doi:10.1016/b978-0-08-101011-2.00007-6, ISBN   978-0-08-101011-2 , retrieved 2025-03-07