Efficacy of intermittent combined RAF and MEK inhibition in a patient with concurrent BRAF-and NRAS-mutant malignancies

O Abdel-Wahab, VM Klimek, AA Gaskell, A Viale… - Cancer discovery, 2014 - AACR
Vemurafenib, a RAF inhibitor, extends survival in patients with BRAFV600-mutant
melanoma but activates extracellular signal–regulated kinase (ERK) signaling in RAS …

Progression of RAS-mutant leukemia during RAF inhibitor treatment

MK Callahan, R Rampal, JJ Harding… - … England Journal of …, 2012 - Mass Medical Soc
Vemurafenib, a selective RAF inhibitor, extends survival among patients with BRAF V600E–
mutant melanoma. Vemurafenib inhibits ERK signaling in BRAF V600E–mutant cells but …

[HTML][HTML] BRAF inhibitor–associated ERK activation drives development of chronic lymphocytic leukemia

N Yaktapour, F Meiss, J Mastroianni… - The Journal of …, 2014 - Am Soc Clin Investig
Patients with BRAFV600E/K-driven melanoma respond to the BRAF inhibitor vemurafenib
due to subsequent deactivation of the proliferative RAS/RAF/MEK/ERK pathway. In BRAF …

Vemurafenib

C Garbe, TK Eigentler - Small Molecules in Oncology, 2018 - Springer
The activating BRAF mutation V600E and related mutations in this codon are most important
for the activation of the RAS/RAF/MEK/ERK mitogen-activated protein kinase (MAPK) …

Vemurafenib

C Garbe, S Abusaif, TK Eigentler - Small Molecules in Oncology, 2014 - Springer
The activating BRAF mutation V600E and related mutations in this codon are most important
for the activation of the RAS/RAF/MEK/ERK mitogen-activated protein kinase (MAPK) …

Pan-erbB inhibition potentiates BRAF inhibitors for melanoma treatment

YK Ng, JY Lee, KM Supko, A Khan, SM Torres… - Melanoma …, 2014 - journals.lww.com
The BRAF inhibitor vemurafenib is currently used for treating patients with BRAF V600E
mutant melanoma. However, the responses to vemurafenib are generally partial and of …

BRAF inhibitors amplify the proapoptotic activity of MEK inhibitors by inducing ER stress in NRAS-mutant melanoma

H Niessner, T Sinnberg, C Kosnopfel… - Clinical Cancer …, 2017 - AACR
Purpose: NRAS mutations in malignant melanoma are associated with aggressive disease
requiring rapid antitumor intervention, but there is no approved targeted therapy for this …

Selective RAF inhibitor impairs ERK 1/2 phosphorylation and growth in mutant NRAS, vemurafenib‐resistant melanoma cells

K Le, ES Blomain, U Rodeck… - Pigment cell & melanoma …, 2013 - Wiley Online Library
The RAF inhibitor vemurafenib achieves remarkable clinical responses in mutant BRAF
melanoma patients. However, vemurafenib is burdened by acquired drug resistance and by …

[HTML][HTML] Combination therapies to inhibit the RAF/MEK/ERK pathway in melanoma: we are not done yet

GA McArthur - Frontiers in oncology, 2015 - frontiersin.org
The discovery and development of small molecule inhibitors of mutant BRAF kinase and
MEK kinase have revolutionized the care of patients with melanoma. When used as single …

[HTML][HTML] Combination of RAF and MEK inhibition for the treatment of BRAF-mutated melanoma: feedback is not encouraged

PB Chapman, DB Solit, N Rosen - Cancer cell, 2014 - cell.com
In BRAF V600E melanoma patients, RAF inhibitor treatment causes a MEK-inhibitor-
sensitive, RAF-inhibitor-resistant adaptive reactivation of ERK signaling. In clinical trials …