Like other AAS, drostanolone is an agonist of the androgen receptor (AR).  It is not a substrate for 5α-reductase and is a poor substrate for 3α-hydroxysteroid dehydrogenase (3α-HSD), and therefore shows a high ratio of anabolic to androgenic activity.  As a DHT derivative, drostanolone is not a substrate for aromatase and hence cannot be aromatized into estrogenic metabolites .  While no data are available on the progestogenic activity of drostanolone, it is thought to have low or no such activity similarly to other DHT derivatives.  Since the drug is not 17α-alkylated , it is not known to cause hepatotoxicity . 
“The reality is, especially with this whole steroid epidemic, one thing we have to realize is the use of steroids is less than 100 years old,” Rogan said. “There’s always been something people have taken, but the actual use of anabolic steroids in human beings is relatively recent in human history. As time goes on, they’re going to create more powerful, crazy sh-t, and it’s going to get to the point where you’re going to test negative because it’s not in your system anymore, but your body will forever change.”
Stephan Bonnar and Josh Barnett , mixed martial arts (MMA) fighters from the UFC and PRIDE Fighting Championships , have also tested positive for the banned substance.  After the World Extreme Cagefighting show on January 20, 2006 Muay Thai turned MMA fighter Kit Cope also tested positive for boldenone.  Following the Strikeforce card on June 22, 2007 former PRIDE and UFC fighter Phil Baroni tested positive for boldenone, as well as stanozolol .  At a K-1 WGP event in Las Vegas on August 17, 2007 two fighters, Rickard Nordstrand and Zabit Samedov , both tested positive for boldenone.  Alexandre Franca Nogueira tested positive for boldenone in July 2008.