TABLE 3

AUC of tibolone metabolites and ratios and percentages of the metabolites in plasma and safety tissues

Ratios and percentages calculated using AUC and rounded to one decimal place and integers, respectively.


Plasma/Tissue

AUC

Percentage of 3OH Metabolites

Tissue Ratio Δ4-tib/(3α OH + 3β OH)
3α OH-tib
3β OH-tib
Δ4 -tib
3α S,17β OH
3β S,17β OH
3α S,17β S
3β S,17β S
Total S
Mono-S
ng/g · h
Plasma 58 3 7 151 74 3541 2079 99 4 0.1
Endometrium 22 3 66 18 9 822 441 98 2 2.7
Myometrium 38 5 57 18 6 566 698 97 2 1.4
Mammary glands 31 2 37 13 7 896 515 98 1 1.1
Mammary fat
88
4
101
10
4
520
326
90
2
1.1