Active Ingredient History
Binimetinib (MEK162) is an oral small-molecule with potential antineoplastic activity. It is a selective mitogen-activated protein kinase 1 and 2 (MEK1/2) inhibitor, a key protein kinase in the RAS/RAF/MEK/ERK pathway, which regulates several key cellular activities including proliferation, differentiation, migration, survival and angiogenesis. Inappropriate activation of this pathway has been shown to occur in many cancers, in particular through mutations in BRAF, KRAS and NRAS. MEK162 at 6 mg/kg, BID combined with BEZ235 (dual PI3K/mTOR inhibitor) resulted in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells. There are three ongoing Phase 3 trials with binimetinib in advanced cancer patients: NEMO (NRAS-mutant melanoma), COLUMBUS (encorafenib in combination with binimetinib in BRAF-mutant melanoma) and BEACON CRC (encorafenib, binimetinib and cetuximab in BRAF-mutant colorectal cancer). NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Melanoma (approved 2018)
Adenocarcinoma of Lung (Early Phase 1)
Arthritis, Rheumatoid (Phase 2)
Astrocytoma (Phase 2)
Bile Duct Neoplasms (Phase 2)
Biliary Tract Neoplasms (Phase 2)
Brain Neoplasms (Phase 2)
Breast Neoplasms (Phase 2)
Carcinoma (Phase 2)
Carcinoma, Non-Small-Cell Lung (Phase 2)
Carcinoma, Ovarian Epithelial (Phase 2)
Cardiomegaly (Phase 2)
Cholangiocarcinoma (Phase 2)
Colonic Neoplasms (Phase 2)
Colorectal Neoplasms (Phase 3)
Craniopharyngioma (Phase 2)
Endometrial Neoplasms (Phase 2)
Esophageal Neoplasms (Phase 2)
Fallopian Tube Neoplasms (Phase 3)
Gallbladder Neoplasms (Phase 2)
Gastrointestinal Stromal Tumors (Phase 1/Phase 2)
Glioblastoma (Phase 2)
Glioma (Phase 2)
Gliosarcoma (Phase 2)
Hamartoma (Phase 3)
Immunotherapy (Phase 2)
Intestinal Neoplasms (Phase 1/Phase 2)
Kidney Neoplasms (Phase 2)
Leukemia (Phase 1/Phase 2)
Leukemia, Hairy Cell (Phase 2)
Leukemia, Monocytic, Acute (Phase 1)
Leukemia, Myeloid, Acute (Phase 1/Phase 2)
Leukemia, Myelomonocytic, Acute (Phase 1)
Liver Diseases (Phase 1)
Liver Neoplasms (Phase 2)
Lung Neoplasms (Phase 2)
Lymphoma (Phase 2)
Lymphoma, Large-Cell, Anaplastic (Phase 1/Phase 2)
Melanoma (Phase 3)
Multiple Myeloma (Phase 2)
Mutation (Phase 2)
Myelodysplastic Syndromes (Phase 1/Phase 2)
Neoplasm Metastasis (Phase 2)
Neoplasms (Phase 4)
Neurofibroma, Plexiform (Phase 2)
Neurofibromatosis 1 (Phase 2)
Oncogene Proteins (Phase 1/Phase 2)
Oncogenes (Phase 1)
Ovarian Neoplasms (Phase 3)
Pancreatic Neoplasms (Phase 2)
Prostatic Neoplasms (Phase 2)
Proto-Oncogene Proteins B-raf (Phase 2)
Proto-Oncogene Proteins c-met (Phase 1/Phase 2)
Skin Neoplasms (Phase 2)
Soft Tissue Neoplasms (Phase 1/Phase 2)
Squamous Cell Carcinoma of Head and Neck (Phase 2)
Stomach Neoplasms (Phase 2)
Thyroid Neoplasms (Phase 2)
Triple Negative Breast Neoplasms (Phase 1/Phase 2)
Urinary Bladder Neoplasms (Phase 2)
Uterine Cervical Neoplasms (Phase 2)
| Trial | Phase | Start Date | Organizations | Indications |
|---|
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