How Exemestane works
Exemestane acts as a false substrate for the aromatase enzyme.
It also prevents the conversion of androgens to estrogens.
It is a synthetic androgen analog that binds irreversibly to and inhibits the enzyme aromatase.
Aromatase inhibitors (AI) have been used in males in idiopathic short stature, constitutional delay of puberty, precocious puberty, gynecomastia, oligospermia, hypogonadism related to obesity and ageing.
With the first detailed study of the pharmacological effects of exemestane in male subjects were given doses of 25 and 50mg.
Exemestane results in men
Both dosages were comparable in suppressing all circulating estrogens and had a similar impact of increasing serum androstenedione and testosterone concentrations.
Results showed that a 38%, 71%, and 45% decrease in estradiol, estrone, and estrone sulphate concentrations.
Respectively, after ten days of administration of the last dose, a 60% and 32% increase of testosterone and androstenedione were measured.
The rise in the aromatase substrates, testosterone, and androstenedione, is probably secondary to the feedback increase in gonadotropins.
The 21% decrease in SHBG concentrations was also expected.
There are effects of aromatase inhibition on the release of the follicle-stimulating hormone.
Although FSH release is primarily under the control of inhibin, circulating estradiol has an impact on men.
The use of an AI results in a three-fold increase in levels of FSH in eugonadal men and may potentially stimulate sperm production.
Aromataze Inhibitors in Men
Comparative study on individual aromatase inhibitors
The third-generation aromatase inhibitors (AIs: anastrozole, letrozole, and exemestane) have now become standard. AIs block estradiol biosynthesis from androgens by inhibiting aromatase.
Estrogen receptors are detected in vascular and muscle cells. Estrogen receptor plays a significant role in protecting the heart and circulatory system.
Reducing circulating estrogen in plasma can also lead to High-density lipoprotein cholesterol (HDL) decline after three months after AI use.
Exemestane can induce androgen-like effects that are still controversial.
Tamoxifen lowers serum cholesterol after two weeks of administration, and this may contribute to cardiac protection.
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