Glasdegib, also known as PF-04449913, is an orally bioavailable small-molecule inhibitor of the Hedgehog (Hh) signaling pathway with potential antineoplastic activity. Hedgehog inhibitor PF-04449913 appears to inhibit Hh pathway signaling. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Constitutive activation of Hh pathway signaling has been observed in various types of malignancies. Glasdegib (PF-04449913) is an FDA approved cancer drug developed by Pfizer. It is a small molecule inhibitor of sonic hedgehog, which is a protein overexpressed in many types of cancer. It inhibits the sonic hedgehog receptor smoothened (SMO), as do most drugs in its class.
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Munchhof, Michael J.; Li, Qifang; Shavnya, Andrei; Borzillo, Gary V.; Boyden, Tracey L.; Jones, Christopher S.; LaGreca, Susan D.; Martinez-Alsina, Luis; Patel, Nandini; Pelletier, Kathleen; Reiter, Larry A.; Robbins, Michael D.; Tkalcevic, George T. Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened. ACS Medicinal Chemistry Letters. Volume 3. Issue 2. Pages 106-111. Journal; Online Computer File. (2012).
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