VTX-27 is a selective inhibitor of protein kinase C θ (PKC θ) (Kis: 0.08 nM and 16 nM for PKC θ and PKC δ).

PKCθ:0.08 nM (ki), PKCδ:16 nM (ki), PKCα:356 nM (ki)

It has also been found that VTX-27 has good selectivity to other PKC family members, especially the classic isoforms (except for PKCβI, >1000 times, 200 times) and atypical isoforms (>10000 times). As expected, it is more challenging to obtain selectivity for more closely related novel PKC family members, which is 200 times more selective than PKCδ.

VTX-27 demonstrates a superior PK profile characterized by low clearance (7 mL/min/kg), high oral bioavailability (65%), and a prolonged half-life (4.7 h). Following a single oral administration at doses of 6.25, 12.5, 25, and 50 mg/kg (e.g., at 25 mg/kg Cmax concentration 700 ng/mL), it effectively inhibits IL-2 production in a potent dose-dependent manner.