The in vitro and in vivo metabolism of structurally related synthetic steroidal hormones.

About seventy years ago, steroidal hormones were isolated from e.g. urine and testis extracts and their chemical structures were subsequently identified. Investigators wanted to use these steroids for clinical purposes like oral contraception and hormone replacement therapy, but the bioavailability of these endogenous steroids was very low after oral administration. The steroids were inactivated very quickly by metabolism in the gastrointestinal tract and liver. Most steroids are very lipophilic substances, which are transformed enzymatically by a variety of pathways into polar, water-soluble, and more readily excreted metabolites. This process is called biotransformation. ...

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Summary

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