Exemestane, in Young Males

[mick-G]

TweetFrom the Journals of Clinical Endocronology and Metabolism Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males
Nelly Mauras, John Lima, Deval Patel, Annie Rini, Enrico di Salle, Ambrose Kwok and Barbara Lippe
Nemours Children’s Clinic and Research Programs (N.M., J.L., A.R.), Jacksonville, Florida 32207; and University of Florida Health Sciences Center (D.P.) and Amersham Pharmacia Biotech (E.d.S., A.K., B.L.), Peapack, New Jersey 07977


Suppression of estrogen, via estrogen receptor or aromatase blockade, is being investigated in the treatment of different conditions. Exemestane (Aromasin) is a potent and selective irreversible aromatase inhibitor. To characterize its suppression of estrogen and its pharmacokinetic (PK) properties in males, healthy eugonadal subjects (14–26 yr of age) were recruited. In a cross-over study, 12 were randomly assigned to 25 and 50 mg exemestane daily, orally, for 10 d with a 14-d washout period. Blood was withdrawn before and 24 h after the last dose of each treatment period. A PK study was performed (n = 10) using a 25-mg dose. Exemestane suppressed plasma estradiol comparably with either dose [25 mg, 38% (P 0.002); 50 mg, 32% (P 0.008)], with a reciprocal increase in testosterone concentrations (60% and 56%; P 0.003 for both). Plasma lipids and IGF-I concentrations were unaffected by treatment. The PK properties of the 25-mg dose showed the highest exemestane concentrations 1 h after administration, indicating rapid absorption. The terminal half-life was 8.9 h. Maximal estradiol suppression of 62 ± 14% was observed at 12 h. The drug was well tolerated. In conclusion, exemestane is a potent aromatase inhibitor in men and an alternative to the choice of available inhibitors. Long-term efficacy and safety will need further study.

This work was supported by a grant from Amersham Pharmacia Biotech.

Abbreviations: AUC, Area under the curve; CBC, cell blood count; HDL, high density lipoprotein; LDL, low density lipoprotein; PK, pharmacokinetic.

[956Vette]

TweetWow, that study gave some stout doses for sure! 20mg/day can dry out my joints

[mick-G]

Tweetthey were only on for 10 days and they are young men, lol Common now! Only thing iam leary is about igf and i would personally think lipids would increase being it lowers estrogen even more so than with armidex in long-term useage.

[TestRip7]

TweetMaybe I read into it wrong, but exemestane at the given doses increased testosterone???

[956Vette]

Tweet

Maybe I read into it wrong, but exemestane at the given doses increased testosterone???

You read it correct. Similar studies show the same senario with arimidex, etc

Basically when you are lowering your bodies estrogen, your body wants to get back to homeostatis. So by triggering more testosterone, your body is trying to increase aromatization to get your estrogen back to normal. Very vague, unscientific answer, but follow me?

[TestRip7]

Tweet

You read it correct. Similar studies show the same senario with arimidex, etc

Basically when you are lowering your bodies estrogen, your body wants to get back to homeostatis. So by triggering more testosterone, your body is trying to increase aromatization to get your estrogen back to normal. Very vague, unscientific answer, but follow me?

I follow you. Much better explaniation, you got to spell it out for us southerners. LOL