NVP-LDE225 is an inhibitor of Smo that prevents hedgehog (Hh) signaling; it exhibits anticancer chemotherapeutic and anti-metastatic activities. NVP-LDE225 is currently approved for the treatment of basal cell carcinoma but is also in clinical trials as a potential treatment for other cancers. In renal cell carcinoma cells, NVP-LDE225 inhibits cellular proliferation, migration, and invasion; in animal models, it increases survival rates and decreases tumor growth. NVP-LDE225 also inhibits cell viability in prostate cancer cells. In animal models of prostate cancer, this compound inhibits the epithelial-to-mesenchymal transition (EMT), induces apoptosis, decreases the expression of Bcl-2, Bcl-xl, XIAP, and survivin, and increases the expression of Bax and Bak; it also inhibits tumor growth. Smo antagonists such as NVP-LDE225 also cause alopecia, likely due to alteration in hair follicle embryology.