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| Trade names | Thioderon |
| Other names | 10364-S; Epitiostanol 17β-(1-methoxy)cyclopentyl ether; 17β-[(1-Methoxycyclopentyl)oxy]-2α,3α-epithio-5α-androstane |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration | By mouth |
| Drug class | Androgen;Anabolic steroid;Androgen ether;Antiestrogen |
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| Chemical and physical data | |
| Formula | C25H40O2S |
| Molar mass | 404.65 g·mol−1 |
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Mepitiostane, sold under the brand nameThioderon, is anorally activeantiestrogen andanabolic–androgenic steroid (AAS) of thedihydrotestosterone (DHT) group which is marketed inJapan as anantineoplastic agent for the treatment ofbreast cancer.[1][2][3][4][5] It is aprodrug ofepitiostanol.[6][7] The drug was patented and described in 1968.[1]
Mepitiostane is used as an antiestrogen and antineoplastic agent in the treatment of breast cancer.[1][2][3][5] It is also used as an AAS in the treatment ofanemia ofrenal failure.[5] A series ofcase reports have found it to be effective in the treatment of anestrogen receptor (ER)-dependentmeningiomas as well.[8][9][10][11]
Mepitiostane shows a high rate ofvirilizingside effects such asacne,hirsutism, andvoice changes in women.[12]
Mepitiostane is described as similar totamoxifen as an antiestrogen,[8] and through its active form epitiostanol, binds directly to andantagonizes the ER.[13][14][15][16] It is also an AAS.[1][3]
Mepitiostane is converted intoepitiostanol in the body.[6][7]
Mepitiostane, also known as epitiostanol 17β-(1-methoxy)cyclopentyl ether,[6] is asyntheticandrostanesteroid and aderivative of DHT.[1][2][3] It is the C17β (1-methoxy)cyclopentylether of epitiostanol, which itself is 2α,3α-epithio-DHT or 2α,3α-epithio-5α-androstan-17β-ol.[6][17] A related AAS ismethylepitiostanol (17α-methylepitiostanol), which is an orally active variant of epitiostanol similarly to mepitiostane, though also has a risk ofhepatotoxicity.[18]
Mepitiostane is thegeneric name of the drug and itsINNTooltip International Nonproprietary Name andJANTooltip Japanese Accepted Name.[1][2][3]
