Company: SC VERMODJE SRL (Moldova)
Description Exemever (Exemestane)
Exemever belongs to third generation aromatase inhibitors (like Arimidex (Anastrozole) and Femara (Letrozole)). The latter two substances can efficiently block the transformation of androgens into estrogen. So, why do we need Exemever, if we have, let’s say Letro, which is much more efficient aromatase inhibitor? Let’s compare.
Letro can decrease the levels of estrogen by 98% or more. At the dosage of 100 mcg it reaches maximum efficiency as to the aromatase inhibition. Nevertheless estrogen is an important hormone for keeping joints healthy and for immune system.
Thus, elimination of 98% of estrogen from your body is not a good solution. It can be helpful in a cutting cycle before the contest, or if you are predisposed to gyno problems, but certainly long term usage can endanger your joints and immune system.
Arimidex in its turn is not as powerful as Letrozole, but at the dosage of 5 mg/day can reduce estrogen levels to 50%. So, in usual cycles you can use Arimidex, but if you are predisposed to gyno or getting ready for a competition, use Letro.
Post Cycle Therapy (PCT)
Most athletes chose Nolvadex (Tamoxifen Citrate) instead of Clomid for post cycle therapy. Though, both of them rival estrogen in binding to receptor, improve lipid profile and increase testosterone levels, there is a difference. 20 mg of Nolvadex produce the same effect on testosterone elevation, FSH and LH, as 150 mg of Clomid. But Nolvadex doesn’t reduce the LH reaction to LHRH. So, most users agree that Nolvadex is better for PCT.
As to the PCT it’s important to increase testosterone levels by as many mechanisms as possible, including aromatase inhibitors (AI). So, which one do we use? If we use Letrozole or Arimidex along with Nolvadex, it will not be a good idea, as Nolvadex will greatly reduce their levels in blood plasma. Thus, it decreases their effectiveness. And this is where Exemever comes into the first position.
At the dosage 20-25 mg/day it will increase testosterone level by 60% and decrease the level of Sex Hormone Binding Globulin (SHBG) by 20%, therefore raising the ratio of active to bound testosterone. SHBG is an enzyme that captures testosterone, thus making it useless for bodybuilding. So, how does it come along with Nolvadex during PCT?
The difference between Type-1 and Type-2 inhibitors
To understand why Exemever is more effective with Nolvadex than Letro and A-dex, we need to closely examine the difference between Type-1 and Type-2 aromatase inhibitors. Type 1 inhibitors (Exemever) belong to steroidal substances, while Type 2 (Letro, A-dex) are non-steroidal ones.
One should mention that Type 1 inhibitors are prone to produce androgenic side-effects, so women should avoid it. Both types of inhibitors imitate normal substrates (androgens), thus competing with them for the binding site of aromatase. But when the binding happened their actions differ.
Type 1 inhibitor causes the enzyme to start reaction of hydroxylation. This hydroxylation results in unbreakable bond between enzyme and inhibitor.
Since that moment the enzyme is completely neutralized. Type 2 inhibitors reversibly attach to the active site of an enzyme. By this attachment inhibitor can cause either no changes or trigger some activity in enzyme. Then type 2 inhibitor eventually dissociates from the enzyme, and again takes part in a competition with substrate for binding the active site.
This means that efficiency of Type 2 inhibitors depends on their concentration and affinity (of both inhibitor and substrate). Since Exemever belongs to Type 1 inhibitors it permanently deactivates enzyme and is no longer needed, meanwhile Arimidex and Letrozole require constant concentrations to remain efficient. Probably this is why Nolvadex doesn’t affect Exemever activity.
As we can see Exemever is rather powerful estrogen suppressor (about 65%). You can safely use it along with Nolvadex during PCT. Besides, it makes positive effect on lipid metabolism and mineral metabolism in bones, which is not peculiar to non-steroidal aromatase inhibitors like Letrozole and Arimidex.