MEK inhibitors: a patent review 2008 – 2010

Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer

(2011) Qing Dong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition

(2011) A. G. Gilmartin et al.   CLINICAL CANCER RESEARCH

Antitumour activity of a potent MEK inhibitor RDEA119/BAY 869766 combined with rapamycin in human orthotopic primary pancreatic cancer xenografts

(2010) Qing Chang et al.   BMC CANCER

Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo

(2010) Kihyun Kim et al.   BRITISH JOURNAL OF HAEMATOLOGY

MEK1/2 Inhibitors AS703026 and AZD6244 May Be Potential Therapies forKRASMutated Colorectal Cancer That Is Resistant to EGFR Monoclonal Antibody Therapy

(2010) Juyong Yoon et al.   CANCER RESEARCH

A Phase II Study of PD-0325901, an Oral MEK Inhibitor, in Previously Treated Patients with Advanced Non-Small Cell Lung Cancer

(2010) E. B. Haura et al.   CLINICAL CANCER RESEARCH

The First-in-Human Study of the Hydrogen Sulfate (Hyd-Sulfate) Capsule of the MEK1/2 Inhibitor AZD6244 (ARRY-142886): A Phase I Open-Label Multicenter Trial in Patients with Advanced Cancer

(2010) U. Banerji et al.   CLINICAL CANCER RESEARCH

Emerging MEK inhibitors

(2010) James A McCubrey et al.   EXPERT OPINION ON EMERGING DRUGS

The Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Oral Doses of RO5068760, an MEK Inhibitor, in Healthy Volunteers: Assessment of Target Suppression

(2010) Lucy Lee et al.   JOURNAL OF CLINICAL PHARMACOLOGY

A Phase II, Open-Label, Randomized Study to Assess the Efficacy and Safety of AZD6244 (ARRY-142886) Versus Pemetrexed in Patients with Non-small Cell Lung Cancer Who Have Failed One or Two Prior Chemotherapeutic Regimens

(2010) John D. Hainsworth et al.   Journal of Thoracic Oncology

Preclinical In vivo Evaluation of Efficacy, Pharmacokinetics, and Pharmacodynamics of a Novel MEK1/2 Kinase Inhibitor RO5068760 in Multiple Tumor Models

(2010) S. Daouti et al.   MOLECULAR CANCER THERAPEUTICS

Detection of BRAF mutations in the tumour and serum of patients enrolled in the AZD6244 (ARRY-142886) advanced melanoma phase II study

(2009) R E Board et al.   BRITISH JOURNAL OF CANCER

RDEA119/BAY 869766: A Potent, Selective, Allosteric Inhibitor of MEK1/2 for the Treatment of Cancer

(2009) C. Iverson et al.   CANCER RESEARCH

The Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Single Oral Doses of CH4987655 in Healthy Volunteers: Target Suppression Using a Biomarker

(2009) L. Lee et al.   CLINICAL CANCER RESEARCH

Recent Developments in Anti-Cancer Agents Targeting the Ras/Raf/ MEK/ERK Pathway

(2009) Kwong-Kwok Wong   Recent Patents on Anti-Cancer Drug Discovery

2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles—O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase)

(2008) Joseph S. Warmus et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901

(2008) Stephen D. Barrett et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Putative allosteric MEK1 and MEK2 inhibitors

(2008) Steve Price   EXPERT OPINION ON THERAPEUTIC PATENTS

Phase I Pharmacokinetic and Pharmacodynamic Study of the Oral, Small-Molecule Mitogen-Activated Protein Kinase Kinase 1/2 Inhibitor AZD6244 (ARRY-142886) in Patients With Advanced Cancers

(2008) Alex A. Adjei et al.   JOURNAL OF CLINICAL ONCOLOGY