sotrastaurin

Sotrastaurin is an orally available small molecule that acts as a potent, selective pan-protein kinase C (PKC) inhibitor, with particular activity against the PKC alpha, beta, and theta isoforms. By inhibiting these PKC isozymes, sotrastaurin blocks T- and B-cell activation through suppression of NF-kappaB signaling pathways. This results in immunosuppressive effects and potential antineoplastic activity by inducing G1 cell cycle arrest and apoptosis in susceptible tumor cells. Sotrastaurin has been investigated primarily for its use as an immunomodulator in organ transplantation to prevent acute rejection and for the treatment of various cancers including uveal melanoma and diffuse large B-cell lymphoma. The drug was developed by Novartis

Other names

sotrastaurin acetate