Vismodegib

Vismodegib (GDC-0449) is a more potent novel and specific synthetic oral hedgehog pathway inhibitor with an IC50 of 3 nM; also inhibits P-gp with IC50 of 3.0 μM. (In Vitro) :Vismodegib (HhAntag691) is an ABCG2 inhibitor and can increase the effective intracellular concentration of NSC 279836, another ABCG2 substrate, through blocking its export in HEK293 cells. Vismodegib (HhAntag691, 10 μM), resensitizes MDCKII/Pgp cells and MDCKII/MRP1 cells to NSC757 treatment. Vismodegib (25 μM or 50 μM) concentration dependently inhibits HCC and H1339 cells. (In Vivo) :Vismodegib is a novel small molecule HPI, often used for clinical trials. Vismodegib (0.3 to 75 mg/kg, p.o.) is highly efficacious in medulloblastoma allograft tumors. Vismodegib (> 46 mg/kg, p.o.) causes growth delay in patient-derived colorectal xenografts.