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refametinib

An orally bioavailable selective MEK inhibitor with potential antineoplastic activity. Refametinib specifically inhibits mitogen-activated protein… Expand
National Institutes of Health

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RDEA 119

Papers overview

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2019
2019
Receptor tyrosine kinase-dependent PI3K activation is an escape mechanism to vertical suppression of the EGFR/RAS/MAPK pathway in KRAS-mutated human colorectal cancer cell lines
BackgroundPrevious studies showed that the combination of an anti-Epidermal growth factor (EGFR) and a MEK-inhibitor is able to… Expand
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2018
2018
Phase II Studies with Refametinib or Refametinib plus Sorafenib in Patients with RAS-Mutated Hepatocellular Carcinoma
Purpose: Refametinib, an oral MEK inhibitor, has demonstrated antitumor activity in combination with sorafenib in patients with… Expand
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2017
2017
A preclinical evaluation of the MEK inhibitor refametinib in HER2-positive breast cancer cell lines including those with acquired resistance to trastuzumab or lapatinib
Purpose The MEK/MAPK pathway is commonly activated in HER2-positive breast cancer, but little investigation of targeting this… Expand
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2016
2016
Phase I/II Study of Refametinib (BAY 86-9766) in Combination with Gemcitabine in Advanced Pancreatic cancer
BackgroundActivating KRAS mutations are reported in up to 90% of pancreatic cancers. Refametinib potently inhibits MEK1/2, part… Expand
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2016
2016
Differences in MEK inhibitor efficacy in molecularly characterized low-grade serous ovarian cancer cell lines.
Advanced or recurrent low-grade serous ovarian cancers (LGSC) are resistant to conventional systemic treatments. LGSC carry… Expand
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2015
2015
A Phase I Study of the Safety, Pharmacokinetics, and Pharmacodynamics of Combination Therapy with Refametinib plus Sorafenib in Patients with Advanced Cancer
Purpose: To assess the safety and tolerability of the small-molecule allosteric MEK inhibitor refametinib combined with sorafenib… Expand
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Highly Cited
2014
Highly Cited
2014
A Phase II Study of the Efficacy and Safety of the Combination Therapy of the MEK Inhibitor Refametinib (BAY 86-9766) Plus Sorafenib for Asian Patients with Unresectable Hepatocellular Carcinoma
Purpose: There is an unmet need for treatment options in hepatocellular carcinoma (HCC). Sorafenib is currently the only approved… Expand
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2014
2014
A phase 1b trial of PI3K inhibitor copanlisib (BAY 80-6946) combined with the allosteric-MEK inhibitor refametinib (BAY 86-9766) in patients with advanced cancer.
2588 Background: Dual inhibition of the PI3K and MAPK signaling pathways is a promising strategy for optimal anticancer therapy… Expand
Review
2013
Review
2013
MEK and the inhibitors: from bench to bedside
Four distinct MAP kinase signaling pathways involving 7 MEK enzymes have been identified. MEK1 and MEK2 are the prototype members… Expand
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2013
2013
Allosteric MEK1/2 inhibitor refametinib (BAY 86-9766) in combination with sorafenib exhibits antitumor activity in preclinical murine and rat models of hepatocellular carcinoma.
OBJECTIVE The objectives of the study were to evaluate the allosteric mitogen-activated protein kinase kinase (MEK) inhibitor BAY… Expand
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