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| Clinical data | |
|---|---|
| Other names | 6β-OH-7α-TMS; 6β,17α-Dihydroxy-7α-(methylthio)-3-oxo-pregn-4-ene-21-carboxylic acid γ-lactone |
| Drug class | Antimineralocorticoid |
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| Chemical and physical data | |
| Formula | C23H32O4S |
| Molar mass | 404.57 g·mol−1 |
| 3D model (JSmol) | |
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6β-Hydroxy-7α-thiomethylspironolactone (6β-OH-7α-TMS) is asteroidalantimineralocorticoid of thespirolactone group and a majoractive metabolite ofspironolactone.[1][2][3] Other importantmetabolites of spironolactone include7α-thiospironolactone (7α-TS; SC-24813),7α-thiomethylspironolactone (7α-TMS; SC-26519), andcanrenone (SC-9376).[4][2][1][3]
Spironolactone is aprodrug with a shortterminal half-life of 1.4 hours.[5][6][7] The active metabolites of spironolactone have extended terminal half-lives of 13.8 hours for 7α-TMS, 15.0 hours for 6β-OH-7α-TMS, and 16.5 hours for canrenone, and accordingly, these metabolites are responsible for the therapeutic effects of the drug.[5][6]
| Compound | CmaxTooltip Peak concentrations(day 1) | CmaxTooltip Peak concentrations(day 15) | AUCTooltip Area-under-the-curve concentrations(day 15) | t1/2Tooltip Elimination half-life |
|---|---|---|---|---|
| Spironolactone | 72 ng/mL (173 nmol/L) | 80 ng/mL (192 nmol/L) | 231 ng•hour/mL (555 nmol•hour/L) | 1.4 hours |
| Canrenone | 155 ng/mL (455 nmol/L) | 181 ng/mL (532 nmol/L) | 2,173 ng•hour/mL (6,382 nmol•hour/L) | 16.5 hours |
| 7α-TMSTooltip 7α-Thiomethylspironolactone | 359 ng/mL (924 nmol/L) | 391 ng/mL (1,006 nmol/L) | 2,804 ng•hour/mL (7,216 nmol•hour/L) | 13.8 hours |
| 6β-OH-7α-TMSTooltip 6β-Hydroxy-7α-thiomethylspironolactone | 101 ng/mL (250 nmol/L) | 125 ng/mL (309 nmol/L) | 1,727 ng•hour/mL (4,269 nmol•hour/L) | 15.0 hours |
| Sources: See template. | ||||
6β-Hydroxytestosterone, which is analogous to 6β-OH-7α-TMS, has been found to possess virtually noandrogenicity.[8]
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