Abstract
Aberrant Hedgehog (Hh) pathway signaling has been suggested to play a role in the development of multiple solid tumors and hematologic malignancies. GDC-0449 is a novel first-in-human, first-in-class smoothened (SMO) inhibitor, which has completed its phase I evaluation and achieved proof of concept in tumors with Hh pathway mutations.
©2011 AACR.
MeSH terms
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Anilides / metabolism
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Anilides / pharmacokinetics
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Anilides / therapeutic use*
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Dose-Response Relationship, Drug
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Gene Expression Regulation, Neoplastic / drug effects
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Hedgehog Proteins / antagonists & inhibitors*
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Hedgehog Proteins / metabolism
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Humans
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Metabolic Clearance Rate
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Neoplasm Metastasis
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Neoplasms / drug therapy*
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Neoplasms / metabolism
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Neoplasms / pathology
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Orosomucoid / metabolism
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Protein Binding
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Pyridines / metabolism
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Pyridines / pharmacokinetics
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Pyridines / therapeutic use*
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Signal Transduction / drug effects*
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Transcription Factors / genetics
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Treatment Outcome
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Zinc Finger Protein GLI1
Substances
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Anilides
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GLI1 protein, human
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Hedgehog Proteins
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HhAntag691
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Orosomucoid
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Pyridines
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Transcription Factors
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Zinc Finger Protein GLI1