More On Exemestane (Aromasin)

[LCohen]

As you know Exemestane (Aromasin) is a powerful aromatase inhibitor and anti-estrogen. It binds irreversibly to the aromatase enzyme. But looks like its magic not limited to estrogen.

1. Anti-inflammatory and Antioxidant Activities of Exemestane
This study is quite long. In summary Exemestane induces cytoprotective enzymes, protects some cells against oxidative damage, protect against UV radiation, protect against hypoxia–reoxygenation injury, inhibits nitric oxide, shows a inhibitory effect on inflammatory cytokines like NF-κB. It aims nitric oxide a lot.

2. Protective for Parkinson's Disease
Again it inhibits nitric oxide and induces Nrf2 antioxidant enzyme. Helpful against PD.

3. No need to say. It's actually/originally used for breast cancer.

4. No need to say again it skyrockets T levels.

 

[vulture]

Seems promising:
Comparative assessment in young and elderly men of the gonadotropin response to aromatase inhibition. - PubMed - NCBI

But what's the downside on it?

 

[benaoao]

I'd be wary of progesterone inhibition from AIs, I'd need to take some time to look it up regarding exemestane specifically

 

[Baltazar]

Anti estrogen are pain in the ****

Estrogen is so needed to have a good strength and stamina

Aromasin is good for sometimes
Not forever

It gives lot of boneaches and you feel so weak if you do it alot

Just be careful

 

[LCohen]

I'd be wary of progesterone inhibition from AIs, I'd need to take some time to look it up regarding exemestane specifically

Can't find anything about Aromasin-Progesterone. Letrozole reduces progesterone.

 

[RisingSun]

Seems promising:
Comparative assessment in young and elderly men of the gonadotropin response to aromatase inhibition. - PubMed - NCBI

But what's the downside on it?

Moodiness, potentially irreversible joint damage, poor lipid profile, muscle loss, body hair loss, erectile dysfunction.

 

[benaoao]

the one thing I'm regretting about exemestane is that the FDA clearly states that its effects start at 5mg per dose but most of the studies use the absurd doses of 12.5 up to 50mg per day.

Considering its mechanism of action, PK and PD, 5mg every 3rd day or more could already start producing some effect. I'd go very slow anyhow when introducing it.

 

[ddjd]

inhibits nitric oxide

Which isoform of NO?

 

[LCohen]

Which isoform of NO?

iNOS

 

[ddjd]

iNOS

Any idea what effects it has on eNOS or nNOS?

 

[Lyall]

Could somebody link the research into letrozole decreasing progesterone? I can’t find it.

 

[benaoao]

It’s mostly tied to estrogen inducing a stimulation of a progesterone receptor

Effects of estrogen on progesterone receptor synthesis during endometrial cell culture. - PubMed - NCBI
http://www.jbc.org/content/253/7/2223.full.pdf

And so on. So I’d use anti estrogens or aromatase inhibitors at very conservative doses. Anecdotal but some people report feeling better when taking very low doses of clomid such as 12.5mg eod or bi weekly. Should be the same with AIs.

Exemestane specifically mentioned here but I can’t access the full paper rn:

(progesterone receptor) downregulation in EC tissue (a marker of attenuated estrogenic stimulation) was most expressed with exemestane

 

[ecstatichamster]

Ground cooked button mushrooms are safer.

 

[Baltazar]

Well me I'm on anastrazol

I take it twice a week 0.5 mg

More makes me got pain all over my body

But for people not on trt

They can take it daily on a dosage 0.1 mg

And they will increase their T like 20 percent at least
If they eat high protein high carb high fat

150 /150 / 150

 

[benaoao]

150-150-150 isn't high carb high fat, more like low carb. Unless you meant 33% each

Have you got experience with such a dose of arimidex? That would be something close to 5mg of aromasin every 3/4 day (rough equivalences basing myself on the standard doses studied for both and the fact that aromasin is suicidal and its effect last for 3+ days)

 

[Baltazar]

If I was normal guy


I would do 0.5 arimidex daily two weeks every year

Me I have very high T
I'm on trt

I'm 2800 ng...

Arimidex is a must for me

 

[Lyall]

It’s mostly tied to estrogen inducing a stimulation of a progesterone receptor

Effects of estrogen on progesterone receptor synthesis during endometrial cell culture. - PubMed - NCBI
http://www.jbc.org/content/253/7/2223.full.pdf

And so on. So I’d use anti estrogens or aromatase inhibitors at very conservative doses. Anecdotal but some people report feeling better when taking very low doses of clomid such as 12.5mg eod or bi weekly. Should be the same with AIs.

Exemestane specifically mentioned here but I can’t access the full paper rn:

Thanks so much, very interesting. I wasn’t sure also if I heard it here but it could force estrogen, the ai, into tissues? So low serum estrogen but higher tissue estrogen?

 

[ddjd]

Haidut says Androsterone is of similar potency to Exemestane I think

 

[ecstatichamster]

If I was normal guy


I would do 0.5 arimidex daily two weeks every year

Me I have very high T
I'm on trt

I'm 2800 ng...

Arimidex is a must for me

Why is it so high? That seems damaging.

 

[benaoao]

@Baltazar that is not a trt. The way I perceive trt now, considering how unnaturally stable T levels are when injecting it, I’d shoot for a lower level than whats deemed as optimal in naturals. Because in a natural individual T peaks in the morning and is lower at night. There would be some Area Under Curve work to do. I’d shoot for 500-600 ng/dl which may or may not be the equivalent of someone who has 800+ in the morning naturally.

Plus exogenous androgens lower SHBG so, same calculation with free hormones.

Thanks so much, very interesting. I wasn’t sure also if I heard it here but it could force estrogen, the ai, into tissues? So low serum estrogen but higher tissue estrogen?

Never read this before. Very interesting. @RisingSun maybe?