Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer.

PubWeight™: 2.22‹?› | Rank: Top 2%

🔗 View Article (PMID 22180495)

Published in Cancer Res on December 16, 2011

Authors

Hong Yang1, Brian Higgins, Kenneth Kolinsky, Kathryn Packman, William D Bradley, Richard J Lee, Kathleen Schostack, Mary Ellen Simcox, Scott Kopetz, David Heimbrook, Brian Lestini, Gideon Bollag, Fei Su

Author Affiliations

1: Roche Pharmaceuticals, Nutley, New Jersey 07110, USA.

Articles citing this

Tumor adaptation and resistance to RAF inhibitors. Nat Med (2013) 3.11

Vemurafenib: the first drug approved for BRAF-mutant cancer. Nat Rev Drug Discov (2012) 3.09

Phase II Pilot Study of Vemurafenib in Patients With Metastatic BRAF-Mutated Colorectal Cancer. J Clin Oncol (2015) 2.33

Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascade inhibitors: how mutations can result in therapy resistance and how to overcome resistance. Oncotarget (2012) 1.96

Resistance to BRAF inhibition in BRAF-mutant colon cancer can be overcome with PI3K inhibition or demethylating agents. Clin Cancer Res (2012) 1.92

Clonal evolution in hematological malignancies and therapeutic implications. Leukemia (2013) 1.50

Concomitant BRAF and PI3K/mTOR blockade is required for effective treatment of BRAF(V600E) colorectal cancer. Clin Cancer Res (2013) 1.21

Identification of recurrent SMO and BRAF mutations in ameloblastomas. Nat Genet (2014) 1.20

The B-Raf(V600E) inhibitor dabrafenib selectively inhibits RIP3 and alleviates acetaminophen-induced liver injury. Cell Death Dis (2014) 1.14

B-Raf and the inhibitors: from bench to bedside. J Hematol Oncol (2013) 1.14

Molecular dissection of microsatellite instable colorectal cancer. Cancer Discov (2013) 1.10

Toward a Molecular Classification of Colorectal Cancer: The Role of BRAF. Front Oncol (2013) 1.02

Evolving approaches to patients with advanced differentiated thyroid cancer. Endocr Rev (2013) 1.02

Shimmer: detection of genetic alterations in tumors using next-generation sequence data. Bioinformatics (2013) 1.02

Differential expression of IL-17, 22 and 23 in the progression of colorectal cancer in patients with K-ras mutation: Ras signal inhibition and crosstalk with GM-CSF and IFN-γ. PLoS One (2013) 0.95

Primary and acquired resistance to EGFR-targeted therapies in colorectal cancer: impact on future treatment strategies. J Mol Med (Berl) (2014) 0.91

Applications of nanotechnology for melanoma treatment, diagnosis, and theranostics. Int J Nanomedicine (2013) 0.90

Biology of colorectal cancer. Ecancermedicalscience (2015) 0.90

Strategies to overcome resistance to epidermal growth factor receptor monoclonal antibody therapy in metastatic colorectal cancer. World J Gastroenterol (2014) 0.88

Receptor tyrosine kinases in cancer escape from BRAF inhibitors. Cell Res (2012) 0.88

Cordycepin induced MA-10 mouse Leydig tumor cell apoptosis by regulating p38 MAPKs and PI3K/AKT signaling pathways. Sci Rep (2015) 0.88

Immunohistochemistry of colorectal cancer biomarker phosphorylation requires controlled tissue fixation. PLoS One (2014) 0.86

HDAC Inhibition Overcomes Acute Resistance to MEK Inhibition in BRAF-Mutant Colorectal Cancer by Downregulation of c-FLIPL. Clin Cancer Res (2015) 0.86

Optimising the combination dosing strategy of abemaciclib and vemurafenib in BRAF-mutated melanoma xenograft tumours. Br J Cancer (2016) 0.86

Phase IB Study of Vemurafenib in Combination with Irinotecan and Cetuximab in Patients with Metastatic Colorectal Cancer with BRAFV600E Mutation. Cancer Discov (2016) 0.86

Cross-resistance to clinically used tyrosine kinase inhibitors sunitinib, sorafenib and pazopanib. Cell Oncol (Dordr) (2015) 0.84

Vemurafenib and panitumumab combination tailored therapy in BRAF-mutated metastatic colorectal cancer: a case report. Cancer Biol Ther (2014) 0.83

Similar but different: distinct roles for KRAS and BRAF oncogenes in colorectal cancer development and therapy resistance. Oncotarget (2015) 0.82

Personalized treatment for colorectal cancer: novel developments and putative therapeutic strategies. Langenbecks Arch Surg (2015) 0.82

BRAF inhibitors: experience in thyroid cancer and general review of toxicity. Horm Cancer (2014) 0.82

Genetic targeting of B-RafV600E affects survival and proliferation and identifies selective agents against BRAF-mutant colorectal cancer cells. Mol Cancer (2014) 0.81

Advances in targeted and immunobased therapies for colorectal cancer in the genomic era. Onco Targets Ther (2016) 0.81

Personalizing colon cancer therapeutics: targeting old and new mechanisms of action. Pharmaceuticals (Basel) (2013) 0.81

SK3/TRPC1/Orai1 complex regulates SOCE-dependent colon cancer cell migration: a novel opportunity to modulate anti-EGFR mAb action by the alkyl-lipid Ohmline. Oncotarget (2016) 0.79

Molecular Subtypes and Personalized Therapy in Metastatic Colorectal Cancer. Curr Colorectal Cancer Rep (2016) 0.78

Application of genomic principles to pharmacotherapy of cancer. Am J Pharm Educ (2014) 0.78

BRAF mutant colorectal cancer as a distinct subset of colorectal cancer: clinical characteristics, clinical behavior, and response to targeted therapies. J Gastrointest Oncol (2015) 0.78

Serrated colorectal cancer: Molecular classification, prognosis, and response to chemotherapy. World J Gastroenterol (2016) 0.77

Synergistic combination of novel tubulin inhibitor ABI-274 and vemurafenib overcome vemurafenib acquired resistance in BRAFV600E melanoma. Mol Cancer Ther (2013) 0.77

Reactivation of ERK and Akt confers resistance of mutant BRAF colon cancer cells to the HSP90 inhibitor AUY922. Oncotarget (2016) 0.77

A Phase 1b Dose-Escalation Study of Encorafenib (LGX818) and Cetuximab With or Without Alpelisib in Metastatic BRAF-Mutant Colorectal Cancer. Cancer Discov (2017) 0.76

LY3009120, a panRAF inhibitor, has significant anti-tumor activity in BRAF and KRAS mutant preclinical models of colorectal cancer. Oncotarget (2017) 0.76

The role of EGFR monoclonal antibodies (MoABs) cetuximab/panitumab, and BRAF inhibitors in BRAF mutated colorectal cancer. J Gastrointest Oncol (2013) 0.76

Molecular profiling in the treatment of colorectal cancer: focus on regorafenib. Onco Targets Ther (2015) 0.76

Single-Cell Sequencing Technology in Oncology: Applications for Clinical Therapies and Research. Anal Cell Pathol (Amst) (2016) 0.76

Precision Medicine and Non-Colorectal Cancer Liver Metastases: Fiction or Reality? Viszeralmedizin (2015) 0.75

BRAF-Directed Therapy in Metastatic Colorectal Cancer. Cancer J (2016) 0.75

Gastrointestinal cancer: Combine and conquer. Nat Rev Clin Oncol (2012) 0.75

Cancer in silico drug discovery: a systems biology tool for identifying candidate drugs to target specific molecular tumor subtypes. Mol Cancer Ther (2014) 0.75

BRAFV600 mutant non-small-cell lung cancer resistant to Vemurafenib. Int J Clin Exp Pathol (2015) 0.75

Report on the use of non-clinical studies in the regulatory evaluation of oncology drugs. Cancer Sci (2016) 0.75

Beyond RAS and BRAF: a target rich disease that is ripe for picking. J Gastrointest Oncol (2016) 0.75

Recent Advances in Targeting the EGFR Signaling Pathway for the Treatment of Metastatic Colorectal Cancer. Int J Mol Sci (2017) 0.75

Concomitant inhibition of receptor tyrosine kinases and downstream AKT synergistically inhibited growth of KRAS/BRAF mutant colorectal cancer cells. Oncotarget (2017) 0.75

Present and future of metastatic colorectal cancer treatment: A review of new candidate targets. World J Gastroenterol (2017) 0.75

Non-V600 BRAF mutations recurrently found in lung cancer predict sensitivity to the combination of Trametinib and Dabrafenib. Oncotarget (2016) 0.75

Articles by these authors

Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med (2011) 45.46

Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med (2010) 36.57

BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res (2004) 21.36

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A (2008) 17.41

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature (2010) 17.31

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature (2010) 16.12

Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N Engl J Med (2012) 13.17

Nivolumab versus Docetaxel in Advanced Squamous-Cell Non-Small-Cell Lung Cancer. N Engl J Med (2015) 11.98

Hyperactive Ras in developmental disorders and cancer. Nat Rev Cancer (2007) 10.27

Isolation of circulating tumor cells using a microvortex-generating herringbone-chip. Proc Natl Acad Sci U S A (2010) 7.77

RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors. N Engl J Med (2012) 6.93

The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner. Proc Natl Acad Sci U S A (2010) 6.54

Inertial focusing for tumor antigen-dependent and -independent sorting of rare circulating tumor cells. Sci Transl Med (2013) 4.74

RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res (2010) 4.70

Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy. Proc Natl Acad Sci U S A (2006) 4.68

Germline KRAS mutations cause Noonan syndrome. Nat Genet (2006) 4.48

Pathologic response to preoperative chemotherapy: a new outcome end point after resection of hepatic colorectal metastases. J Clin Oncol (2008) 4.37

Targeting ligand-activated ErbB2 signaling inhibits breast and prostate tumor growth. Cancer Cell (2002) 4.34

Isolation and characterization of circulating tumor cells from patients with localized and metastatic prostate cancer. Sci Transl Med (2010) 3.90

17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts. Clin Cancer Res (2002) 3.72

Towards the introduction of the 'Immunoscore' in the classification of malignant tumours. J Pathol (2014) 3.21

Cancer classification using the Immunoscore: a worldwide task force. J Transl Med (2012) 2.88

Androgen receptor signaling in circulating tumor cells as a marker of hormonally responsive prostate cancer. Cancer Discov (2012) 2.76

Impact of BRAF mutation and microsatellite instability on the pattern of metastatic spread and prognosis in metastatic colorectal cancer. Cancer (2011) 2.68

CCAT2, a novel noncoding RNA mapping to 8q24, underlies metastatic progression and chromosomal instability in colon cancer. Genome Res (2013) 2.57

Preoperative bevacizumab does not significantly increase postoperative complication rates in patients undergoing hepatic surgery for colorectal cancer liver metastases. J Clin Oncol (2008) 2.52

A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design. Nat Biotechnol (2005) 2.51

Pharmacodynamic effects and mechanisms of resistance to vemurafenib in patients with metastatic melanoma. J Clin Oncol (2013) 2.51

ALDH activity selectively defines an enhanced tumor-initiating cell population relative to CD133 expression in human pancreatic adenocarcinoma. PLoS One (2011) 2.49

Use of research biopsies in clinical trials: are risks and benefits adequately discussed? J Clin Oncol (2012) 2.43

Prostate cancer, version 2.2014. J Natl Compr Canc Netw (2014) 2.40

Association of computed tomography morphologic criteria with pathologic response and survival in patients treated with bevacizumab for colorectal liver metastases. JAMA (2009) 2.35

High survival rate after two-stage resection of advanced colorectal liver metastases: response-based selection and complete resection define outcome. J Clin Oncol (2011) 2.28

Blood neutrophil-to-lymphocyte ratio predicts survival in patients with colorectal liver metastases treated with systemic chemotherapy. Ann Surg Oncol (2009) 2.27

Stapled α-helical peptide drug development: a potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy. Proc Natl Acad Sci U S A (2013) 2.22

Marked, homogeneous, and early [18F]fluorodeoxyglucose-positron emission tomography responses to vemurafenib in BRAF-mutant advanced melanoma. J Clin Oncol (2012) 2.21

CSF1R signaling blockade stanches tumor-infiltrating myeloid cells and improves the efficacy of radiotherapy in prostate cancer. Cancer Res (2013) 2.19

Quantified pathologic response assessed as residual tumor burden is a predictor of recurrence-free survival in patients with rectal cancer who undergo resection after neoadjuvant chemoradiotherapy. Cancer (2013) 2.09

Tyrosine kinase inhibitors reverse type 1 diabetes in nonobese diabetic mice. Proc Natl Acad Sci U S A (2008) 2.06

PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas. Pigment Cell Melanoma Res (2010) 2.02

Small-molecule MAPK inhibitors restore radioiodine incorporation in mouse thyroid cancers with conditional BRAF activation. J Clin Invest (2011) 1.97

Resistance to BRAF inhibition in BRAF-mutant colon cancer can be overcome with PI3K inhibition or demethylating agents. Clin Cancer Res (2012) 1.92

Phase II study of capecitabine and oxaliplatin for advanced adenocarcinoma of the small bowel and ampulla of Vater. J Clin Oncol (2009) 1.88

Prostate cancer, Version 3.2012: featured updates to the NCCN guidelines. J Natl Compr Canc Netw (2012) 1.84

Structural basis for the activity of drugs that inhibit phosphodiesterases. Structure (2004) 1.84

Optimizing targeted therapeutic development: analysis of a colorectal cancer patient population with the BRAF(V600E) mutation. Int J Cancer (2011) 1.84

Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor. N Engl J Med (2015) 1.75

GTPase activating proteins: critical regulators of intracellular signaling. Biochim Biophys Acta (2002) 1.74

Resistance to selective BRAF inhibition can be mediated by modest upstream pathway activation. Cancer Res (2011) 1.73

EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation. Chem Biol (2014) 1.69

MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models. Cancer Res (2013) 1.68

Application of a fracture risk algorithm to men treated with androgen deprivation therapy for prostate cancer. J Urol (2010) 1.66

A glutamine switch mechanism for nucleotide selectivity by phosphodiesterases. Mol Cell (2004) 1.64

Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. J Med Chem (2013) 1.63

Surgical strategies for synchronous colorectal liver metastases in 156 consecutive patients: classic, combined or reverse strategy? J Am Coll Surg (2010) 1.60

Cytostatic activity of adenosine triphosphate-competitive kinase inhibitors in BRAF mutant thyroid carcinoma cells. J Clin Endocrinol Metab (2009) 1.59

Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties. Cancer Res (2009) 1.58

Recurrent BRAF kinase fusions in melanocytic tumors offer an opportunity for targeted therapy. Pigment Cell Melanoma Res (2013) 1.56

Beyond VEGF: inhibition of the fibroblast growth factor pathway and antiangiogenesis. Clin Cancer Res (2011) 1.49

Deregulated Ras signaling in developmental disorders: new tricks for an old dog. Curr Opin Genet Dev (2007) 1.48

Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma. Neoplasia (2010) 1.48

Antitumor activity of erlotinib (OSI-774, Tarceva) alone or in combination in human non-small cell lung cancer tumor xenograft models. Anticancer Drugs (2004) 1.47

Clinical responses to vemurafenib in patients with metastatic papillary thyroid cancer harboring BRAF(V600E) mutation. Thyroid (2013) 1.45

The phosphodiesterase PDE4B limits cAMP-associated PI3K/AKT-dependent apoptosis in diffuse large B-cell lymphoma. Blood (2004) 1.43

Extended preoperative chemotherapy does not improve pathologic response and increases postoperative liver insufficiency after hepatic resection for colorectal liver metastases. Ann Surg Oncol (2010) 1.42

Biochemical and functional characterization of germ line KRAS mutations. Mol Cell Biol (2007) 1.41

Analysis of dermatologic events in vemurafenib-treated patients with melanoma. Oncologist (2013) 1.41

Identification of the MEK1(F129L) activating mutation as a potential mechanism of acquired resistance to MEK inhibition in human cancers carrying the B-RafV600E mutation. Cancer Res (2011) 1.40

The Abl-related gene tyrosine kinase acts through p190RhoGAP to inhibit actomyosin contractility and regulate focal adhesion dynamics upon adhesion to fibronectin. Mol Biol Cell (2007) 1.39