BRAF-Mutated Advanced Colorectal Cancer: A Rapidly Changing Therapeutic Landscape

Encorafenib Plus Cetuximab as a New Standard of Care for Previously Treated BRAF V600E–Mutant Metastatic Colorectal Cancer: Updated Survival Results and Subgroup Analyses from the BEACON Study

(2021) Josep Tabernero et al.   JOURNAL OF CLINICAL ONCOLOGY

O-10 ANCHOR CRC: Results from a single-arm, phase 2 study of encorafenib, binimetinib plus cetuximab in previously untreated BRAF V600E–mutant metastatic colorectal cancer

(2021) E. Van Cutsem et al.   ANNALS OF ONCOLOGY

Randomized study to investigate FOLFOXIRI plus either bevacizumab or cetuximab as first-line treatment of BRAF V600E-mutant mCRC: The phase-II FIRE-4.5 study (AIO KRK-0116).

(2021) Sebastian Stintzing et al.   JOURNAL OF CLINICAL ONCOLOGY

Overall survival (OS) with encorafenib (enco) + cetuximab (cetux) in BEACON CRC: Effect of prior therapy for BRAF V600E-mutant metastatic colorectal cancer (mCRC).

(2021) Scott Kopetz et al.   JOURNAL OF CLINICAL ONCOLOGY

BRAF-mutant Transcriptional Subtypes Predict Outcome of Combined BRAF, MEK, and EGFR Blockade with Dabrafenib, Trametinib, and Panitumumab in Patients with Colorectal Cancer

(2020) Gary Middleton et al.   CLINICAL CANCER RESEARCH

SO-26 Clinical efficacy of combined BRAF, MEK, and PD-1 inhibition in BRAFV600E colorectal cancer patients

(2020) R. Corcoran et al.   ANNALS OF ONCOLOGY

Interim results from a phase 1/2 precision medicine study of PLX8394- a next generation BRAF inhibitor

(2020) F. Janku et al.   EUROPEAN JOURNAL OF CANCER

Individual Patient Data Meta-Analysis of FOLFOXIRI Plus Bevacizumab Versus Doublets Plus Bevacizumab as Initial Therapy of Unresectable Metastatic Colorectal Cancer

(2020) Chiara Cremolini et al.   JOURNAL OF CLINICAL ONCOLOGY

Inhibitors of BRAF dimers using an allosteric site

(2020) Xiomaris M. Cotto-Rios et al.   Nature Communications

Randomized Trial of Irinotecan and Cetuximab With or Without Vemurafenib in BRAF-Mutant Metastatic Colorectal Cancer (SWOG S1406)

(2020) Scott Kopetz et al.   JOURNAL OF CLINICAL ONCOLOGY

Pembrolizumab in Microsatellite-Instability–High Advanced Colorectal Cancer

(2020) Thierry André et al.   NEW ENGLAND JOURNAL OF MEDICINE

BRAF paradox breakers PLX8394, PLX7904 are more effective against BRAFV600Ε CRC cells compared with the BRAF inhibitor PLX4720 and shown by detailed pathway analysis

(2020) Kassandra Koumaki et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

SHP2 Drives Adaptive Resistance to ERK Signaling Inhibition in Molecularly Defined Subsets of ERK-Dependent Tumors

(2019) Tamer A. Ahmed et al.   Cell Reports

Targeting Alterations in the RAF–MEK Pathway

(2019) Rona Yaeger et al.   Cancer Discovery

Mutational Analysis of Patients With Colorectal Cancer in CALGB/SWOG 80405 Identifies New Roles of Microsatellite Instability and Tumor Mutational Burden for Patient Outcome

(2019) Federico Innocenti et al.   JOURNAL OF CLINICAL ONCOLOGY

Molecular landscape of colorectal cancers harboring R-spondin fusions.

(2019) Andreas Seeber et al.   JOURNAL OF CLINICAL ONCOLOGY

Response to Anti-EGFR Therapy in Patients with BRAF non-V600–Mutant Metastatic Colorectal Cancer

(2019) Rona Yaeger et al.   CLINICAL CANCER RESEARCH

A Phase 1 Study of LY3009120, a Pan-RAF Inhibitor, in Patients with Advanced or Metastatic Cancer

(2019) Ryan J. Sullivan et al.   MOLECULAR CANCER THERAPEUTICS

A First-in-Human Phase I Study to Evaluate the ERK1/2 Inhibitor GDC-0994 in Patients with Advanced Solid Tumors

(2019) Andrea Varga et al.   CLINICAL CANCER RESEARCH

Clinical Sequencing Defines the Genomic Landscape of Metastatic Colorectal Cancer

(2018) Rona Yaeger et al.   CANCER CELL

Treatment and Survival Outcome of BRAF -Mutated Metastatic Colorectal Cancer: A Retrospective Matched Case-Control Study

(2018) Hamzeh Kayhanian et al.   Clinical Colorectal Cancer

Combined BRAF, EGFR, and MEK Inhibition in Patients with BRAF V600E -Mutant Colorectal Cancer

(2018) Ryan B. Corcoran et al.   Cancer Discovery

Type II RAF inhibitor causes superior ERK pathway suppression compared to type I RAF inhibitor in cells expressing different BRAF mutant types recurrently found in lung cancer

(2018) Noeparast Amir et al.   Oncotarget

Health-related quality of life in patients with metastatic colorectal cancer, association with systemic inflammatory response and RAS and BRAF mutation status

(2017) Maria Thomsen et al.   EUROPEAN JOURNAL OF CANCER

Non-V600BRAF Mutations Define a Clinically Distinct Molecular Subtype of Metastatic Colorectal Cancer

(2017) Jeremy C. Jones et al.   JOURNAL OF CLINICAL ONCOLOGY

Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS

(2017) Zhan Yao et al.   NATURE

Mutational landscape of metastatic cancer revealed from prospective clinical sequencing of 10,000 patients

(2017) Ahmet Zehir et al.   NATURE MEDICINE

First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study

(2017) Ryan J. Sullivan et al.   Cancer Discovery

A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic BRAF -Mutant Colorectal Cancer

(2017) Robin M.J.M. van Geel et al.   Cancer Discovery

AACR Project GENIE: Powering Precision Medicine through an International Consortium

(2017)   Cancer Discovery

Outcome according to KRAS-, NRAS- and BRAF-mutation as well as KRAS mutation variants: pooled analysis of five randomized trials in metastatic colorectal cancer by the AIO colorectal cancer study group

(2016) D. P. Modest et al.   ANNALS OF ONCOLOGY

Association of CpG island methylator phenotype and EREG/AREG methylation and expression in colorectal cancer

(2016) Michael S Lee et al.   BRITISH JOURNAL OF CANCER

Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer

(2016) D. Oddo et al.   CANCER RESEARCH

Phase IB Study of Vemurafenib in Combination with Irinotecan and Cetuximab in Patients with Metastatic Colorectal Cancer with BRAFV600E Mutation

(2016) D. S. Hong et al.   Cancer Discovery

LY3009120, a panRAF inhibitor, has significant anti-tumor activity in BRAF and KRAS mutant preclinical models of colorectal cancer

(2016) Eliza Vakana et al.   Oncotarget

BRAFcodons 594 and 596 mutations identify a new molecular subtype of metastatic colorectal cancer at favorable prognosis

(2015) C. Cremolini et al.   ANNALS OF ONCOLOGY

BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition

(2015) Zhan Yao et al.   CANCER CELL

Therapeutic Targeting of Tumor-Derived R-Spondin Attenuates  -Catenin Signaling and Tumorigenesis in Multiple Cancer Types

(2015) C. Chartier et al.   CANCER RESEARCH

Predictive role of BRAF mutations in patients with advanced colorectal cancer receiving cetuximab and panitumumab: A meta-analysis

(2015) Filippo Pietrantonio et al.   EUROPEAN JOURNAL OF CANCER

Phase II Pilot Study of Vemurafenib in Patients With Metastatic BRAF-Mutated Colorectal Cancer

(2015) Scott Kopetz et al.   JOURNAL OF CLINICAL ONCOLOGY

Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600–Mutant Colorectal Cancer

(2015) Ryan B. Corcoran et al.   JOURNAL OF CLINICAL ONCOLOGY

RAF inhibitors that evade paradoxical MAPK pathway activation

(2015) Chao Zhang et al.   NATURE

Distal and proximal colon cancers differ in terms of molecular, pathological, and clinical features

(2014) E. Missiaglia et al.   ANNALS OF ONCOLOGY

BRAF mutation predicts for poor outcomes after metastasectomy in patients with metastatic colorectal cancer

(2014) Rona Yaeger et al.   CANCER

Mismatch Repair Status and BRAF Mutation Status in Metastatic Colorectal Cancer Patients: A Pooled Analysis of the CAIRO, CAIRO2, COIN, and FOCUS Studies

(2014) S. Venderbosch et al.   CLINICAL CANCER RESEARCH

Response to BRAF Inhibition in Melanoma Is Enhanced When Combined with Immune Checkpoint Blockade

(2014) Z. A. Cooper et al.   Cancer Immunology Research

Single agent panitumumab in KRAS wild-type metastatic colorectal cancer patients following cetuximab-based regimens

(2013) Filippo Pietrantonio et al.   CANCER BIOLOGY & THERAPY

PIK3CA, BRAF , and PTEN Status and Benefit from Cetuximab in the Treatment of Advanced Colorectal Cancer—Results from NCIC CTG/AGITG CO.17

(2013) Christos S. Karapetis et al.   CLINICAL CANCER RESEARCH

Discovery of a Selective Kinase Inhibitor (TAK-632) Targeting Pan-RAF Inhibition: Design, Synthesis, and Biological Evaluation of C-7-Substituted 1,3-Benzothiazole Derivatives

(2013) Masanori Okaniwa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Panitumumab–FOLFOX4 Treatment and RAS Mutations in Colorectal Cancer

(2013) Jean-Yves Douillard et al.   NEW ENGLAND JOURNAL OF MEDICINE

Relief of Profound Feedback Inhibition of Mitogenic Signaling by RAF Inhibitors Attenuates Their Activity in BRAFV600E Melanomas

(2012) Piro Lito et al.   CANCER CELL

Addition of cetuximab to chemotherapy as first-line treatment for KRAS wild-type metastatic colorectal cancer: Pooled analysis of the CRYSTAL and OPUS randomised clinical trials

(2012) Carsten Bokemeyer et al.   EUROPEAN JOURNAL OF CANCER

Phase III Trial of Cetuximab With Continuous or Intermittent Fluorouracil, Leucovorin, and Oxaliplatin (Nordic FLOX) Versus FLOX Alone in First-Line Treatment of Metastatic Colorectal Cancer: The NORDIC-VII Study

(2012) Kjell Magne Tveit et al.   JOURNAL OF CLINICAL ONCOLOGY

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR

(2012) Anirudh Prahallad et al.   NATURE

Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors

(2012) A. Gurney et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

EGFR-Mediated Reactivation of MAPK Signaling Contributes to Insensitivity of BRAF -Mutant Colorectal Cancers to RAF Inhibition with Vemurafenib

(2012) Ryan B. Corcoran et al.   Cancer Discovery

Efficacy according to biomarker status of cetuximab plus FOLFOX-4 as first-line treatment for metastatic colorectal cancer: the OPUS study

(2011) C. Bokemeyer et al.   ANNALS OF ONCOLOGY

Impact of BRAF mutation and microsatellite instability on the pattern of metastatic spread and prognosis in metastatic colorectal cancer

(2011) Ben Tran et al.   CANCER

Cetuximab Plus Irinotecan, Fluorouracil, and Leucovorin As First-Line Treatment for Metastatic Colorectal Cancer: Updated Analysis of Overall Survival According to Tumor KRAS and BRAF Mutation Status

(2011) Eric Van Cutsem et al.   JOURNAL OF CLINICAL ONCOLOGY

BRAFMutation in Metastatic Colorectal Cancer

(2009) Jolien Tol et al.   NEW ENGLAND JOURNAL OF MEDICINE

V600EBRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway

(2009) C. A. Pratilas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

R-Spondin Family Members Regulate the Wnt Pathway by a Common Mechanism

(2008) Kyung-Ah Kim et al.   MOLECULAR BIOLOGY OF THE CELL