Pharmacokinetics and pharmacodynamics of a new long-acting androgen ester: maintenance of physiological androgen levels for 4 months after a single injection

Contraception
M Rajalakshmi, P R Ramakrishnan

Abstract

The pharmacokinetics and pharmacodynamics of testosterone trans-4-n-butylcyclohexyl carboxylate (Code name: 20 Aet-1), a new long-acting androgen ester, were evaluated in castrated adult rhesus monkeys and compared with those of testosterone enanthate (TE). A single intramuscular injection of 40 mg of 20 Aet-1 returned serum testosterone (T) to within or close to the diurnal physiological range for 80-136 days. In contrast, a similar dose of TE increased serum T to supraphysiological levels and the response evoked was of short duration. The ratio of T to dihydrotestosterone (T/DHT) ratio in monkeys treated with 20 Aet-1 was comparable to that found in control animals while in TE-treated animals, it was highly elevated. Serum estradiol (E2) elevation by 20 Aet-1 was also of smaller magnitude compared to TE. 20-Aet-1 suppressed LH levels from day 5 until day 115. The levels of LH on day 115 were 45.8% lower compared to the levels on day 13 post-castration. TE suppressed LH levels from day 1-7 post-injection. The values on day 7 were 76.6% lower compared to values on day 13 post-castration. Thus, TE-induced suppression of LH was of shorter duration, but of greater magnitude compared to the effect caused by 20 Aet-1. Similarly, FSH...Continue Reading

Citations

Dec 15, 1990·Lancet·M Pollard
Sep 1, 1994·The Journal of Steroid Biochemistry and Molecular Biology·C MonderR P Blye
Sep 28, 2005·Treatments in Endocrinology·Emily Darby, Bradley D Anawalt
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