ATP synthase related toxicity is unlikely

Wednesday, December 31th, 2008 by hinrich

Structure of TMC207/R207910

A recent study by Haagsma et al. has shown that TMC207/R207910 is very specific in inhibiting the mycobacterial ATP synthase. This is an important finding as it makes it unlikely that we will see toxic effects of the compound that would be caused by affecting the human ATP synthase.

In the article the authors demonstrate that sensitivity of the human form of the enzyme to TMC207/R207910 is approximately 20,000 fold lower. Tests using other eukaryotic forms of the ATP synthase (namely those from mouse liver and bovine heart) also exhibited much lower sensitivity as compared to the effect of the compound on the mycobacterial ATP synthase.

You can read the abstract of the paper here.

Posted in Tuberculosis