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Ulixertinib

Known as: 1H-Pyrrole-2-carboxamide, 4-(5-chloro-2-((1-methylethyl)amino)-4-pyridinyl)-N-((1S)-1-(3-chlorophenyl)-2-hydroxyethyl)- 
An orally available inhibitor of extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity. Upon oral… 
National Institutes of Health

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BVD-523
NCIt Antineoplastic Agent Terminology

Papers overview

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2020
2020
Pharmacokinetics and bioavailability of ipatasertib in dog plasma by LC/MS/MS.
A rapid, sensitive and reliable liquid chromatography-tandem mass spectrometric method was established to quantify ipatasertib in… 
2019
2019
Abstract 4732: CDK4/6 inhibition with lerociclib (G1T38) enhances response to PI3K or ERK inhibitors in high-throughput, ex vivo pancreatic PDX screens
Introduction: In pancreatic ductal adenocarcinoma (PDAC), mutations in KRAS and deletion or promoter methylation of the CDKN2A… 
2018
2018
Abstract 2375: Concurrent HER or PI3K inhibition potentiates the anti-tumor effect of ERK inhibitor BVD-523 (ulixertinib) in preclinical pancreatic cancer models
To date, effective treatments for inoperable pancreatic ductal adenocarcinoma (PDAC) remain elusive. Targeting KRAS, the gene… 
2017
2017
First-in-class oral ERK1/2 inhibitor Ulixertinib (BVD-523) in patients with advanced solid tumors: Final results of a phase I dose escalation and expansion study.
2508Background: Aberrant MAPK pathway activation is known to be an oncogenic driver in many solid tumors, making ERK inhibition… 
2017
2017
Chemical-biology approach to delineate the mechanism of action of HIV-1 latency reversing agents
Prostratin exhibits potent HIV-1 latency reversing activity, yet its molecular mechanism of action has not been defined in detail… 
2016
2016
Acquisition of BTK C481S Produces Resistance to Ibrutinib in MYD88 Mutated WM and ABC DLBCL Cells That Is Accompanied By ERK1/2 Hyperactivation, and Is Targeted By the Addition of the ERK1/2…
Activating mutations in MYD88 mutations trigger BTK (Yang et al, Blood 2013; Wilson et al, Nat. Med. 2015) and HCK (Yang et al… 
2015
2015
Dose escalation stage of a first-in-class phase I study of the novel oral ERK 1/2 kinase inhibitor BVD-523 (ulixertinib) in patients with advanced solid tumors.
2506 Background: Aberrant MAPK pathway signaling and resultant ERK kinase activity is evident in many oncogene-dependent cancers… 
2015
2015
Abstract 4693: The selective ERK inhibitor BVD-523 is active in models of MAPK pathway-dependent cancers, including those with intrinsic and acquired drug resistance
The MAPK (RAS-RAF-MEK-ERK) pathway is activated in many cancers, and the clinical efficacy of BRAF and MEK inhibitors in melanoma… 
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