Agonists vs. antagonists (the latter not to be confused with a character in a novel!)

[bluesnjazz]

I know many of you on this site are beyond ADT, but for those who are still holding on in that space, I'd like to share my experience with the newer antagonists drugs, degarelix ( U.S. brand, Firmagon) and relugolix (U.S. brand, Orgovyx). I started ADT exactly 8 years ago this month and during my off-and-on treatments since then have tried a half-dozen different drugs in the older agonist category (leuprolide, for example) attempting to find one with the fewest (or at least the most tolerable) side-effects.

In my research, at the beginning of the COVID-19 pandemic, I discovered this new class called antagonists, with the most appealing point being less nasty effects on the heart than the agonists. I have no heart trouble, yet when on the agonists, heart palpitations became so awful at times, they scared the shit out of me. Another plus for me was that the antagonists drop one's hormone levels almost immediately and recover rather quickly, while the agonists actually spike a guy's hormones first, then drop them, then take longer to recover. So I requested it from my urologist and never looked back. I've found during the last four years of use that the stuff causes few if any heart palpitations and that the hot flashes and depression that were so severe for me with the agonists are noticeably less so. Yet a 1-month injection continues to work for 3-4 months, meaning I've usually only had three per year.

For those who are in the U.S., you are lucky if you want to use this class of drugs as relugolix has been approved for use for PCa and are in tablet form. In Japan, where I live, it's in the approval process for woman's issues only, while degarelix--a liquid that's injected into the belly--is approved here for PCa. That bunch of liquid injected into one's flesh causes severe swelling and pain for a week or two.

Another strong point for those whose PCa is more advanced is the more powerful control of hormones with anagonists.

Here are some links if you are interested in reading up on these:

cancer.org/cancer/types/pro...

cancer.gov/news-events/canc...

drugs.com/relugolix.html

[JohnInTheMiddle]

Hi Blues. Great write up about ADT antagonists. It seems most people are just by default on the agonists such as Eligard AKA Lupron. It was especially interesting to see you note both possibly better side effects with the antagonists and the apparently better heart profile too.

I'm going to share my collection of discussions on this topic here so anyone interested has them in one place. (The references here are to a reply I have made but it's worth scrolling up and down to see other parts of the conversations.)

healthunlocked.com/advanced...

healthunlocked.com/advanced...

healthunlocked.com/advanced...

[bluesnjazz in reply to JohnInTheMiddle]

Hello, John. Yes, it seems to me few folks who have serious diseases actually do any research on their own and just depend on their doctors for everything. I do think doctors mostly have the best intentions, but they are often so busy, so overwhelmed by paperwork, etc., that many of them do not seem to keep up on the latest info. My doc here in Japan hadn't even heard of the antagonists when I told him I wanted to try one.