Trametinib in the treatment of melanoma

R Thota, DB Johnson, JA Sosman - Expert opinion on biological …, 2015 - Taylor & Francis
Introduction: Aberrant MAPK pathway signaling is a hallmark of melanoma.
Mitogen/extracellular signal-regulated kinase (MEK) 1/2 are integral components of MAPK …

Adaptive resistance to RAF inhibitors in melanoma

CH Kugel III, AE Aplin - Pigment cell & melanoma research, 2014 - Wiley Online Library
The discovery of activating mutations in BRAF at high frequency in cutaneous melanoma
opened the door to new treatment options, which have resulted in significantly better patient …

Contribution of MEK Inhibition to BRAF/MEK Inhibitor Combination Treatment of BRAF-Mutant Melanoma: Part 2 of the Randomized, Open-Label, Phase III …

PA Ascierto, R Dummer, HJ Gogas, A Arance… - Journal of Clinical …, 2023 - ascopubs.org
PURPOSE In COLUMBUS part 1, patients with advanced BRAF V600-mutant melanoma
were randomly assigned 1: 1: 1 to encorafenib 450 mg once daily plus binimetinib 45 mg …

Update on the targeted therapy of melanoma

DB Johnson, JA Sosman - Current treatment options in oncology, 2013 - Springer
Opinion statement Melanoma is the most aggressive of the cutaneous malignancies,
causing more than 9,000 deaths in the past year in the United States. Historically, systemic …

Antiproliferative effects of continued mitogen-activated protein kinase pathway inhibition following acquired resistance to BRAF and/or MEK inhibition in melanoma

MS Carlino, K Gowrishankar, CAB Saunders… - Molecular cancer …, 2013 - AACR
Inhibitors of the mitogen-activated protein kinases (MAPK), BRAF, and MAP–ERK kinase
(MEK) induce tumor regression in the majority of patients with BRAF-mutant metastatic …

Preexisting MEK1 Exon 3 Mutations in V600E/KBRAF Melanomas Do Not Confer Resistance to BRAF Inhibitors

H Shi, G Moriceau, X Kong, RC Koya, R Nazarian… - Cancer discovery, 2012 - AACR
BRAF inhibitors (BRAFi) induce antitumor responses in nearly 60% of patients with
advanced V600E/K BRAF melanomas. Somatic activating MEK1 mutations are thought to be …

Role of the MEK inhibitor trametinib in the treatment of metastatic melanoma

JW King, PD Nathan - Future Oncology, 2014 - Taylor & Francis
Approximately 50% of patients with cutaneous metastatic melanoma harbor a somatic BRAF
mutation. BRAF inhibitors are now established in the treatment paradigm of BRAF mutant …

BRAF inhibitors and melanoma

KT Flaherty - The Cancer Journal, 2011 - journals.lww.com
Selective BRAF inhibitors have recently emerged as a new standard treatment for patients
with metastatic melanoma harboring activating BRAF mutations. Inhibition of the MAP kinase …

Dissecting therapeutic resistance to ERK inhibition

S Jha, EJ Morris, A Hruza, MS Mansueto… - Molecular cancer …, 2016 - AACR
The MAPK pathway is frequently activated in many human cancers, particularly melanomas.
A single-nucleotide mutation in BRAF resulting in the substitution of glutamic acid for valine …

Efficacy, Safety, and Tolerability of Approved Combination BRAF and MEK Inhibitor Regimens for BRAF-Mutant Melanoma

O Hamid, CL Cowey, M Offner, M Faries, RD Carvajal - Cancers, 2019 - mdpi.com
No head-to-head studies exist comparing BRAF inhibitor/MEK inhibitor (BRAFi/MEKi)
combination treatments for BRAF-mutant melanoma. A side-by-side analysis of randomized …