List of hormonal cytostatic antineoplastic agents

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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.

## Contents

* 1 Marketed
* 1.1 Estrogen-based
* 1.2 Corticosteroid-based
* 2 Never marketed
* 2.1 Estrogen-based
* 2.2 Androgen-based
* 2.3 Corticosteroid-based
* 3 References

## 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" (in en), 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, https://linkinghub.elsevier.com/retrieve/pii/B9780081010112000076, retrieved 2025-03-07

* v
* t
* e

Intracellular chemotherapeutic agents / antineoplastic agents (L01)

SPs/MIs
(M phase)|

| Block microtubule assembly|

* Vinca alkaloids (Vinblastine#
* Vincristine#
* Vinflunine§
* Vindesine
* Vinorelbine#)

|

Block microtubule disassembly|

* Taxanes (Cabazitaxel
* Docetaxel#
* Larotaxel
* Ortataxel†
* Paclitaxel#
* Tesetaxel)
* Epothilones (Ixabepilone)

DNA replication
inhibitor|

| DNA precursors/
antimetabolites
(S phase)|

| Folic acid|

* Dihydrofolate reductase inhibitor (Aminopterin
* Methotrexate#
* Pemetrexed
* Pralatrexate)
* Thymidylate synthase inhibitor (Raltitrexed
* Pemetrexed)

|

Purine|

* Adenosine deaminase inhibitor (Pentostatin)

* Halogenated/ribonucleotide reductase inhibitors (Cladribine
* Clofarabine
* Fludarabine)
* Nelarabine

* Thiopurine (Tioguanine#
* Mercaptopurine#)

Pyrimidine|

* Thymidylate synthase inhibitor (Fluorouracil#
* Capecitabine#
* Doxifluridine
* Tegafur (+gimeracil/oteracil)
* Carmofur
* Floxuridine)

* DNA polymerase inhibitor (Cytarabine#)

* Ribonucleotide reductase inhibitor (Gemcitabine#)

* Hypomethylating agent (Azacitidine
* Decitabine)

Deoxyribonucleotide|

* Ribonucleotide reductase inhibitor (Hydroxycarbamide#)

Topoisomerase inhibitors
(S phase)|

| I|

* Camptotheca (Camptothecin
* Cositecan†
* Belotecan
* Gimatecan
* Exatecan
* Irinotecan#
* Lurtotecan‡
* Silatecan§
* Topotecan
* Rubitecan‡)

|

II|

* Podophyllum (Etoposide#
* Teniposide)

II+Intercalation|

* Anthracyclines (Aclarubicin
* Daunorubicin#
* Doxorubicin#
* Epirubicin
* Idarubicin
* Amrubicin†
* Pirarubicin
* Valrubicin
* Zorubicin)
* Anthracenediones (Mitoxantrone
* Pixantrone)

Crosslinking of DNA
(CCNS)|

| Alkylating|

* Nitrogen mustards: Chlormethine
* Cyclophosphamide# (Ifosfamide#
* Trofosfamide)
* Chlorambucil# (Melphalan
* Prednimustine)
* Bendamustine#
* Uramustine

* Nitrosoureas: Carmustine
* Lomustine (Semustine)
* Fotemustine
* Nimustine
* Ranimustine
* Streptozocin

* Alkyl sulfonates: Busulfan (Mannosulfan
* Treosulfan)

* Aziridines: Carboquone
* Thiotepa
* Triaziquone
* Triethylenemelamine

|

Platinum-based|

* Carboplatin#
* Cisplatin#
* Dicycloplatin
* Nedaplatin
* Oxaliplatin#
* Satraplatin

Nonclassical|

* Hydrazines (Procarbazine#)
* Triazenes (Dacarbazine#
* Temozolomide)
* Altretamine
* Mitobronitol
* Pipobroman

Intercalation|

* Streptomyces (Actinomycin#
* Bleomycin#
* Mitomycins
* Plicamycin)

Photosensitizers/PDT|

* Aminolevulinic acid / Methyl aminolevulinate
* Efaproxiral
* Porphyrin derivatives (Porfimer sodium
* Talaporfin
* Temoporfin
* Verteporfin)

Other|

| Enzyme inhibitors|

* FI (Tipifarnib§)
* CDK inhibitors (Abemaciclib
* Alvocidib†
* Palbociclib
* Ribociclib
* Seliciclib†)
* PrI
* Bortezomib
* Carfilzomib
* Ixazomib
* PhI (Anagrelide)
* IMPDI (Tiazofurin§)
* LI (Masoprocol)
* PARP inhibitor (Niraparib
* Olaparib
* Rucaparib)
* HDAC (Belinostat
* Panobinostat
* Romidepsin
* Vorinostat)
* PIKI (Idelalisib)

|

Receptor antagonists|

* ERA (Atrasentan)
* Retinoid X receptor (Bexarotene)
* Sex steroid (Testolactone)

Other/ungrouped|

* Amsacrine
* Trabectedin
* Retinoids (Alitretinoin
* Tretinoin#)
* Arsenic trioxide
* Asparagine depleters (Asparaginase#/Pegaspargase)
* Celecoxib
* Demecolcine
* Elesclomol§
* Elsamitrucin
* Estramustine phosphate
* Etoglucid
* Lonidamine
* Lucanthone
* Mitoguazone
* Mitotane
* Oblimersen†
* Omacetaxine mepesuccinate
* Eribulin

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

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