MESO-Rx Exclusive Cardarine (GW501516)

[MESO-Rx Administrator]

MESO-Rx has a new original article on Cardarine (GW501516) written by @PeterBond :

"To date, however, there’s not a single approved drug that selectively acts on PPARδ. That’s not to say that the pharmaceutical industry hasn’t been interested in this receptor subtype: a tremendous amount of research has been done in this area. In this article I will focus on a candidate drug that acts on this receptor and made it into clinical trials: cardarine (GW501516). While the clinical trials showed promising results, two rodent studies that screened for carcinogenicity of the compound casted a dark shadow on it."

The Rise and Fall of Cardarine (GW501516)

Estimated reading time: 12 minutes Table of contentsIntroductionCardarine (GW501516) is a PPARδ agonist developed by GlaxoSmithKline (GSK)Cardarine

thinksteroids.com

 

[PeterBond]

Do you know what the equivalent rat dose would be in humans? I've seen people say numbers from low 40s mg to over 100mg. Also do you know if the rats are put on the drugs at birth or do they wait till they're considered mature? Lastly MPMD said(I haven't looked it up so he could be wrong) that the normal life expectancy of the rats is only 3 years and that cancer is the reason they usually die even in control groups. While going from 3 years to 2 years to die from cancer is concerning, if the rats normally die from cancer they seem like a poor choice to determine how carcinogenic a drug is

At the least, human and rat pharmacokinetic data would be required to answer your first question. To the best of my knowledge, this data is not made publically available by GSK. I've seen some calclulations thrown around to calculate the human equivalent dose based on a certain species-specific conversion factor. These are meant to get a ballpark estimate for first clinical trials and can be off by an order of magnitude with regard to tissue exposure as a result of pharmacokinetic differences.

Dosing isn't started until 4 to 6 weeks after birth (sometimes later). This is basically around the time when they're sexually mature.

The rats indeed lived only about 3 years, that's simply the life expectancy of a rat. The 2-year rodent bioassay is actually a very good choice to determine the carcinogenicity of a drug. This assay is mandated by both the FDA and its European equivalent the EMA for determing the carcinogencity of a new pharmaceutical that is to be marketed for chronic use. The assay has both good sensitivity and specificity for this purpose: The 2-year rodent bioassay in drug and chemical carcinogenesis testing: Sensitivity, according to the framework of carcinogenic action - PubMed

Meaning: it properly manages to detect carcinogenic compounds as such in most cases, and it properly manages to detect noncarcinogenic compounds as such in most cases.

Incidences of various types of neoplasms in the most popular rat strains can be found here: Differences in Types and Incidence of Neoplasms in Wistar Han and Sprague-Dawley Rats - PubMed

As there's decades of data available about this (since this assay has been de facto mandated for several decades now), researchers have a very good idea of what's to be expected and not. Even more so since there's always a control group to which the results can be compared.

These studies are usually performed with around 50 rats in each group (I have no idea how many GSK used, maybe they used more). Given the large nr. of different carcinomas and adenomas encountered in the rat assay, that the researchers attributed to usage of the compound, it's beyond a doubt carcinogenic. The times this assay would yield a false positive it wouldn't yield such a wide array of neoplasms.

 

[Regular Joe]

I'm also wondering about it being used before a cheat meal, at only 2.5mg it lowered triglycerides %15 instead of them raising %36. I know some take extra metformin before a shitty meal to combat insulin/carbs add the cardarine to negate the fats. Then you could enjoy the food at your mom's birthday party instead of having to eat in the corner with your weird vegan cousin because you two had to bring your own special stinky meals

 

[juicebro]

You could and maybe even should get
all the cancer markers checked before and during cardarine use.

 

[PeterBond]

You could and maybe even should get
all the cancer markers checked before and during cardarine use.

In general, blood tumor markers are neither sensitive nor specific, they should not be used for screening because of that. These should only be requested upon clinical suspicion, in conjunction with other measurements (e.g. a biopsy), or specific ones under certain conditions (e.g. PSA in men older than 50 years of age with no other known risk factors).

 

[grey]

Given the large nr. of different carcinomas and adenomas encountered in the rat assay, that the researchers attributed to usage of the compound, it's beyond a doubt carcinogenic

I don't doubt that at all... a huge number of things are carcinogenic (especially when consuming GIANT quantities!) which is why the state of California insists that damn near EVERYTHING get a label warning that it causes cancer. That said, 99%+ of these things are simply never consumed in the quantities or durations required for the carcinogenic effects to manifest within a human lifetime.

Hell even smoking tobacco was that way for large chunks of the smoking populace. Smoking increased your odds of developing any number of cancers but that in now way meant that smoking a pack of cigarettes or even that smoking for a 6 month run increased your cancer odds in any meaningful way. The odds of something else killing you in your 70's before any of that carcinogenic increase from you 6 month tobacco cycle gave you any kind of cancer were overwhelmingly greater.


Is human level dosing of GW1516 as bad as a 6 month smoking run? Smoking for 20 years? No one knows.

A drug company simply isn't going to proceed to market with these indicators from the rat study though as it lays the ground for an endless array of lawsuits from people who seem to think everyone would be immortal if companies were just testing enough shit.

 

[SupremeGainzzz]

Agreed. I’ve shared this personal anecdote in every cardarine thread I’ve come across here. Took 25mg/day for about a month. LDL increased dramatically and liver enzymes were elevated, so, 2 reasons I took it were to decrease both those numbers. This was science.bio. Again, just a personal anecdote, but, that result in and of itself should be alarming. @Demondosage loves the stuff. Like to get his reaction.

Just to be clear. You need to keep in mind. You didn’t only take cardarine. You took whatever other chemicals were used in making it into a liquid solution. That’s just but only one of the many other factors that make your anecdotal experience not quantifiable to general use amongst the general population. After all, this is a forum openly discussing performance enhancing compounds. Chances are you’re an outlier when it comes to pharmacological side effects and epigenetic influences.

 

[aestheticdaddy]

I take cardarine only for one purpose and its to bring back my HDL back up and LDL back down after running Var, winny or mast which is during my trt/cruise. Blood work afterwards always shows drastic improvments (within normal range), with no flagged health markers. Btw forgot to mention, good for Triglycerides. So far used Cardarine 3 times during my cruises/trt in between cycels. 10mg a day did me well.

 

[trtbuilder]

I take cardarine only for one purpose and its to bring back my HDL back up and LDL back down after running Var, winny or mast which is during my trt/cruise. Blood work afterwards always shows drastic improvments (within normal range), with no flagged health markers. Btw forgot to mention, good for Triglycerides. So far used Cardarine 3 times during my cruises/trt in between cycels. 10mg a day did me well.

lol

 

[BigJ1]

I've been recommended this a few times by people on other boards.

 

[PaintDrinker]

I’m friends with a guy that has been taking 20mgs a day for the last 9 years. He’s not in this forum, but I know he does rigorous bloodwork. I’ll ask him if he has ever tested for cancer markers and for permission to post his labs here. Obviously anecdote, but I’m curious to see the liver values. He does compete so I’m sure a few months out of the year liver enzymes are quite high.

 

[PaintDrinker]

MESO-Rx has a new original article on Cardarine (GW501516) written by @PeterBond :

"To date, however, there’s not a single approved drug that selectively acts on PPARδ. That’s not to say that the pharmaceutical industry hasn’t been interested in this receptor subtype: a tremendous amount of research has been done in this area. In this article I will focus on a candidate drug that acts on this receptor and made it into clinical trials: cardarine (GW501516). While the clinical trials showed promising results, two rodent studies that screened for carcinogenicity of the compound casted a dark shadow on it."

The Rise and Fall of Cardarine (GW501516)

Estimated reading time: 12 minutes Table of contentsIntroductionCardarine (GW501516) is a PPARδ agonist developed by GlaxoSmithKline (GSK)Cardarine

thinksteroids.com

Lanifibranor - Inventiva Pharma

inventivapharma.com

This is a PPAR agonist that is currently in stage 2 of clinical trials, curious to see what happens with it. I believe it activates all 3 PPAR isoforms.

 

[Burntoutn3rd]

Do you know what the equivalent rat dose would be in humans? I've seen people say numbers from low 40s mg to over 100mg. Also do you know if the rats are put on the drugs at birth or do they wait till they're considered mature? Lastly MPMD said(I haven't looked it up so he could be wrong) that the normal life expectancy of the rats is only 3 years and that cancer is the reason they usually die even in control groups. While going from 3 years to 2 years to die from cancer is concerning, if the rats normally die from cancer they seem like a poor choice to determine how carcinogenic a drug is

I mean, this is the same case with humans though. If we live long enough, eventually we're going to get cancer. A 3 year old rat is equivalent to a 92 year old human.

 

[Burntoutn3rd]

FWIW I was diagnosed with colon cancer after running both Cardarine and Mk-677 on 60 on/60off splits for about a year. Both oral and sub q.

I never took Cardarine higher than 20mg/day.

 

[grey]

FWIW I was diagnosed with colon cancer after running both Cardarine and Mk-677 on 60 on/60off splits for about a year. Both oral and sub q.

Brutal. Sorry to hear that dude.

When was your diagnosis and how is it going in terms of working through that?

 

[Burntoutn3rd]

Brutal. Sorry to hear that dude.

When was your diagnosis and how is it going in terms of working through that?

It was really rough for awhile man. Got to stage 3b. Got multiple blood infections from IV lines in the hospital including a fucking wicked MRSA/Candida dual infection. Lost part of my left hand (the initial IV site), had a right hip arthroplasty (scraping the joint out), a temporary pacemaker, partial right triceps removal, and tons of other smaller surgeries. All from pockets of infection being thrown everywhere.

For the actual cancer I only had 2.

Got on an immune therapy last fall and hit remission about 4 months ago though finally. I was diagnosed in December 2020.

At one point one of the immune therapy shots at the IM site had a wild reaction with the local capillaries and killed a small chunk of thigh muscle that had to be removed.


I definitely almost died, but I'm doing a Lot Better now.

Back onto TRT, in the gym, getting fit again quite easily from muscle memory.

I've got a cycle log I started the other day, with my doctor's clearance and my own certainty (I'm a medical professional myself, neurobiologist) I'm running something very mild to get the gears rolling again. Ive trained BJJ and Muay Thai since I was a teen and wanting to be back in competition shape sooner rather than later.

I'll post pictures there here soon of all the surgery injuries, me at my worst, and where I stand now 4 months back into training.

 

[derelict94]

FWIW I was diagnosed with colon cancer after running both Cardarine and Mk-677 on 60 on/60off splits for about a year. Both oral and sub q.

I never took Cardarine higher than 20mg/day.

How old are you if you don't mind me asking? Also race/ethnicity? Just curious if there were underlying predispositions. Glad to hear you are doing better, sounds like you had a hell of a fight.

 

[Burntoutn3rd]

How old are you if you don't mind me asking? Also race/ethnicity? Just curious if there were underlying predispositions. Glad to hear you are doing better, sounds like you had a hell of a fight.

Diagnosed at 27, almost 31 now. Dad's white as white can get, mom's half European and half Iranian.

 

[derelict94]

Diagnosed at 27, almost 31 now. Dad's white as white can get, mom's half European and half Iranian.

Not exactly the token demographic. Hoping for the best for you.