Lomitapide

Sotrastaurin (AEB071) is a specific inhibitor of protein kinase C that prevents T-cell activation. Sotrastaurin at low micromolar concentrations significantly inhibited the growth of uveal melanoma cells harboring GNAQ mutations through induction of G(1) arrest and apoptosis. AEB071 markedly inhibited in situ PKCθ catalytic activity and selectively affected both the canonical nuclear factor-κB and nuclear factor of activated T cells transactivation pathways. In primary human and mouse T cells, AEB071 treatment effectively abrogated at low nanomolar concentration markers of early T-cell activation. The PKC inhibitor sotrastaurin (AEB071) is currently in phase II clinical trials.