THE PHARMACOLOGY AND METABOLISM OF TESTOSTERONE UNDECANOATE (TU), A NEW ORALLY ACTIVE ANDROGEN

Abstract

ABSTRACT Testosterone undecanoate (TU), either dissolved in arachis oil or as micro-crystal suspension, displays androgenic activity on oral administration to rats in the Hershberger test. The solution in arachis oil is more active than the crystal suspension. When [3H]TU is administered orally to rats, most of it is metabolized in the intestinal wall. The majority of the metabolites probably lose their undecanoate group and are absorbed via the portal vein. The non-metabolized [3H]TU and at least two metabolites are absorbed exclusively via the lymphatic system. One of these metabolites has been identified as 5α-dihydrotestosterone undecanoate (5α-DHTU). TU has no harmful effects on the liver of the rabbits on oral administration.