VTP-27999 (VTP27999) is a potent, highly selective renin inhibitor with IC50 of 0.47 nM.
VTP-27999 displays >1000-fold selectivity for renin over a panel of >150 receptors, ion channels, and enzymes, and has an IC50 value >30 uM against CYP3A4.
VTP-27999 demonstrates >15% oral bioavailability in three species, oral efficacy in a double transgenic rat model of hypertension, and good exposure in humans.
