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Novartis AG

Drug Names(s): erismodegib, sonidegib, LDE225, LDE-225, NVP-LDE225

Description: LDE225 is a selective, orally bioavailable Smoothened (Smo) antagonist from a novel structural class and has been shown to potentially inhibit Hedgehog-(HH) and Smo-dependent proliferation in vivo. Smoothened is a GPCR-like (G protein-coupled receptor) molecule that positively regulates Hedgehog (HH) signal transduction, a signalling pathway that plays a critical role in the development and homeostasis of many organs and tissues. The HH pathway is inactive in the absence of ligands as Smo is inhibited by the receptor Patched (Ptch). When Ptch is bound by one of the HH family of ligands, such as Sonic Hedgehog (SHH), Desert Hedgehog (DHH), and Indian Hedgehog (IHH), activation occurs. Genetic activation of the HH pathway at or upstream of Smo is linked to tumorigenesis of several cancers.

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