Discovery and preclinical development of vismodegib

Hedgehog Pathway Inhibitor HhAntag691 Is a Potent Inhibitor of ABCG2/BCRP and ABCB1/Pgp

(2015) Yimao Zhang et al.   NEOPLASIA

Abstract PR05: Resistance to Hedgehog inhibitor through Smoothened receptor mutation in basal cell carcinoma.

(2014) P. Bossi et al.   MOLECULAR CANCER THERAPEUTICS

Hedgehog pathway inhibitors: a patent review (2009 – present)

(2013) Matthew Kyle Hadden   EXPERT OPINION ON THERAPEUTIC PATENTS

Oxysterol binding to the extracellular domain of Smoothened in Hedgehog signaling

(2013) Daniel Nedelcu et al.   Nature Chemical Biology

Molecular subgroups of medulloblastoma: an international meta-analysis of transcriptome, genetic aberrations, and clinical data of WNT, SHH, Group 3, and Group 4 medulloblastomas

(2012) Marcel Kool et al.   ACTA NEUROPATHOLOGICA

Single and multiple dose intravenous and oral pharmacokinetics of the hedgehog pathway inhibitor vismodegib in healthy female subjects

(2012) Richard A. Graham et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

A Phase II, Randomized, Placebo-Controlled Study of Vismodegib as Maintenance Therapy in Patients with Ovarian Cancer in Second or Third Complete Remission

(2012) S. B. Kaye et al.   CLINICAL CANCER RESEARCH

A Randomized Phase II Trial of Vismodegib versus Placebo with FOLFOX or FOLFIRI and Bevacizumab in Patients with Previously Untreated Metastatic Colorectal Cancer

(2012) J. Berlin et al.   CLINICAL CANCER RESEARCH

Antitumor Activity of Targeted and Cytotoxic Agents in Murine Subcutaneous Tumor Models Correlates with Clinical Response

(2012) H. Wong et al.   CLINICAL CANCER RESEARCH

An oxysterol ligand for Smoothened

(2012) Hayley J Sharpe et al.   Nature Chemical Biology

Efficacy and Safety of Vismodegib in Advanced Basal-Cell Carcinoma

(2012) Aleksandar Sekulic et al.   NEW ENGLAND JOURNAL OF MEDICINE

The Hedgehog Signal Transduction Network

(2012) D. J. Robbins et al.   Science Signaling

Phase I Trial of Hedgehog Pathway Inhibitor Vismodegib (GDC-0449) in Patients with Refractory, Locally Advanced or Metastatic Solid Tumors

(2011) P. M. LoRusso et al.   CLINICAL CANCER RESEARCH

Targeting Superficial or Nodular Basal Cell Carcinoma with Topically Formulated Small Molecule Inhibitor of Smoothened

(2011) T. Tang et al.   CLINICAL CANCER RESEARCH

Pharmacokinetic-Pharmacodynamic Analysis of Vismodegib in Preclinical Models of Mutational and Ligand-Dependent Hedgehog Pathway Activation

(2011) H. Wong et al.   CLINICAL CANCER RESEARCH

Absorption, Distribution, Metabolism, and Excretion of [14C]GDC-0449 (Vismodegib), an Orally Active Hedgehog Pathway Inhibitor, in Rats and Dogs: A Unique Metabolic Pathway via Pyridine Ring Opening

(2011) Q. Yue et al.   DRUG METABOLISM AND DISPOSITION

Identification, Characterization, and Implications of Species-Dependent Plasma Protein Binding for the Oral Hedgehog Pathway Inhibitor Vismodegib (GDC-0449)

(2011) Anthony M. Giannetti et al.   JOURNAL OF MEDICINAL CHEMISTRY

The controversial role of the Hedgehog pathway in normal and malignant hematopoiesis

(2011) B G Mar et al.   LEUKEMIA

Cyclopamine and Hedgehog Signaling: Chemistry, Biology, Medical Perspectives

(2010) Philipp Heretsch et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance

(2010) Gerrit J. P. Dijkgraaf et al.   CANCER RESEARCH

Hedgehog signaling regulates the generation of ameloblast progenitors in the continuously growing mouse incisor

(2010) K. Seidel et al.   DEVELOPMENT

Interplay of Dissolution, Solubility, and Nonsink Permeation Determines the Oral Absorption of the Hedgehog Pathway Inhibitor GDC-0449 in Dogs: An Investigation Using Preclinical Studies and Physiologically Based Pharmacokinetic Modeling

(2010) H. Wong et al.   DRUG METABOLISM AND DISPOSITION

Determination of GDC-0449, a small-molecule inhibitor of the Hedgehog signaling pathway, in human plasma by solid phase extraction-liquid chromatographic-tandem mass spectrometry

(2010) X. Ding et al.   JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES

GDC-0449—A potent inhibitor of the hedgehog pathway

(2009) Kirk D. Robarge et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Hedgehog Signaling Is Dispensable for Adult Murine Hematopoietic Stem Cell Function and Hematopoiesis

(2009) Inga Hofmann et al.   Cell Stem Cell

Treatment of Medulloblastoma with Hedgehog Pathway Inhibitor GDC-0449

(2009) Charles M. Rudin et al.   NEW ENGLAND JOURNAL OF MEDICINE

Inhibition of the Hedgehog Pathway in Advanced Basal-Cell Carcinoma

(2009) Daniel D. Von Hoff et al.   NEW ENGLAND JOURNAL OF MEDICINE

Smoothened Mutation Confers Resistance to a Hedgehog Pathway Inhibitor in Medulloblastoma

(2009) R. L. Yauch et al.   SCIENCE

Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor

(2009) H. Wong et al.   XENOBIOTICA

Hedgehog: functions and mechanisms

(2008) M. Varjosalo et al.   GENES & DEVELOPMENT

Potent Inhibitors of the Hedgehog Signaling Pathway

(2008) Shirley A. Brunton et al.   JOURNAL OF MEDICINAL CHEMISTRY

A paracrine requirement for hedgehog signalling in cancer

(2008) Robert L. Yauch et al.   NATURE