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Definition: "An ergogenic aid is any substance or phenomenon that enhances performance "
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24.03.2019 |
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MK-4541: a SARM that makes muscles stronger and kills cancer cells
In the second decade of this century, the research department of pharma giant Merck investigated a SARM that switches off the androgen receptor in the prostate, kills prostate cancer cells, but increases muscle mass and strength. As promising as this may sound, we, the Ergo-Log whines, are wondering whether MK-4541 will ever be released.
MK-4541
That SARM was called MK-4541. It is, just like finasteride and dutasteride, a 4-azosteroid. The researchers found MK-4541 when they screened three thousand potentially interesting substances.
Merck is searching for new drugs against androgen-sensitive prostate cancer. Nowadays, prostate cancer patients' treatment still relies heavily on antiandrogens such as bicalutamide, which eliminate all androgen hormones. Bicalutamide attaches itself to the androgen receptor so that other hormones can no longer do so, without cells subsequently behaving differently. Bicalutamide therefore switches off the androgen receptor.
The researchers are working on a new generation of antiandrogens that deactivate the androgen receptor in prostate cancer cells, but take over the role of hormones such as testosterone and DHT in other cell types. MK-4541 may be such a new antiandrogen. Merck discovered that, in test tubes, MK-4541 activated the caspase-3 suicide enzyme in prostate cancer cells.
Click on the figure below for a larger version.
Second study
In that study, the researchers gave MK-4541 to castrated rats, and saw that the SARM increased lean body mass [in this case: both muscle mass and bone mass] and muscle strength. If the mice had been 80 kilo people, they would have swallowed 400 milligrams [no sir, it's not a typo] of MK-4541 daily.
This dose did reduce testosterone levels in intact mice. The effect you see below is not statistically significant, but the trend is unmistakable. Higher doses of MK-4541 did induce a statistically significant reduction in testosterone levels.
Conclusion
"Importantly, MK-4541 also increased lean body mass and skeletal muscle function, as well as increased general activity levels during the wake cycle in castrated adult mice, while maintaining normal activity and body composition in intact rodents. Thus, MK-4541 is an exciting and promising candidate to be tested clinically to treat prostate cancer. "
We wonder whether Merck's research department has continued the MK-4541 project. The doses required for biological effects are very, very high...
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