Table 1A.
HE3286 metabolites
| Abundance1,2,3 |
||||
|---|---|---|---|---|
| Structure* | Code | Transformation | Animals | Humans |
| 3β,7β,17β-triol | HE3286 | None | Major: mouse, dog, monkey. Minor: rats | Major |
| 3β,7α,17β-triol | HE3291 | C-7 inversion | Major: mouse, dog. Minor: rats | Major |
| 3β,17β-diol-7-one | HE3393 | C-7 oxidation | Major: mouse, dog. Minor: rats | Minor |
| androst-4,6-dien-3-one | HE3633 | C-3 oxidation and dehydration | Major: all | Major |
| 3α,7β,17β-triol | HE3545 | C-3 inversion | Major: mouse, rat. Minor: dog, rabbit | Minor |
| 3β,7β,16α,17β-tetrol | HE3553 | C-16 hydroxlation | Detected only in mice | ND5 |
| 2α,3β,7β,17β-tetrol | HE3892 | C-2 hydroxylation | Major: all (rat4) | Major |
*derivatives of 17α-ethynyl-androst-5-ene, except for metabolite HE3633 HE3633 (17α-ethynyl-17β-hydroxy-androst-4,6-dien-3-one);
1
metabolites were not characterized in monkeys;
2
considered minor in animals if the daily AUC was less than 5% relative to HE3286;
3
considered minor in humans if usually undetected from 20 mg HE3286 daily dose;
4
present as 2α,3α,7β,17β-tetrol in rats, compound code HE3834;
5
not detected