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. Author manuscript; available in PMC: 2012 Sep 25.
Published in final edited form as: Expert Opin Ther Targets. 2012 Jan 12;16(1):103–119. doi: 10.1517/14728222.2011.645805

Table 3.

MEK inhibitors

Compound Tumor Primary Target(s) Potential side effects
CI-1040 (Pfizer Inc.) Breast cancer, Lung cancer, Pancreatic cancer, Colorectal cancer, Breast Neoplasm, Non small cell lung cancer, Pancreatic Cancers MEK Diarrhea, Asthenia, Rush, Nausea, Vomiting
PD-0325901 (Pfizer Inc.) Carcinoma, Non small cell lung cancer, Melanoma, Breast cancer MEK Diarrhea, Nausea, Fatigue, Rash, Reversible visual disturbances, Vomiting
ARRY-438162 (Array BioPharma) Metastatic Biliary Cancer, and Metastatic Colorectal Cancer MEK Recruiting Phase
AZD6244 (AstraZeneca) Breast cancer, Colon cancer, Lung cancer, Kidney cancer, Metastatic colorectal cancer, Advanced/metastatic Melanoma, Pancreatic cancer, Non small cell lung cancer, Hepatocellular carcinoma MEK Papulopustular rash, Xerosis, Fissures, Pruritus, Telangiectasias, Hyperpigmentation, Dermatitis, Alopecia, Angular chelitis, Paronychea, Fatigue
RDEA119/BAY 86-9766 (Bayer/Ardea Biosciences) Advanced cancer, cancer, Thyroid cancer Pancreatic MEK Low toxicity, further studies are needed
GSK1120212 (GlaxoSmithKline) Solid tumors, Melanoma, Non small cell lung cancer, Pancreatic cancer MEK, C-Raf, B-Raf, V600E, BRAF wt Fatigue, Diarrhea
TAK-733 (Millennium Pharmaceuticals) Advanced Non-hematologic malignancies, Metastatic melanoma MEK Recruiting
GDC-0973/XL581 (Genentech/Exelixis) Metastatic Melanoma, Solid cancers MEK High toxicity, Diarrhea, Fatigue, Rash, Nausea, Vomiting
AZD8330/ARRY-424704 (AstraZeneca) Advanced malignancies MEK Ongoing trial
RO5126766 (Hoffmann-La Roche) Metastatic or advanced solid tumors MEK Recruiting
RO4987655 (Hoffmann-La Roche) Advanced and/or metastatic solid tumors MEK Recruiting
RO5068760 (Hoffmann-La Roche) Melanoma, Colorectal cancer MEK Preclinical Phase Studies
AS703026 (EMD Serono) Acute Myeloid Leukemia, and Hematological Malignancies MEK Recruiting