Active Ingredient History
Cobimetinib is an orally active, potent and highly selective small molecule inhibiting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), and central components of the RAS/RAF/MEK/ERK signal transduction pathway. It has been approved in Switzerland and the US, in combination with vemurafenib for the treatment of patients with unresectable or metastatic BRAF V600 mutation-positive melanoma. Preclinical studies have demonstrated that Cobimetinib is effective in inhibiting the growth of tumor cells bearing a BRAF mutation, which has been found to be associated with many tumor types. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signalling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases. Cobimetinib is used in combination with vemurafenib because the clinical benefit of a BRAF inhibitor is limited by intrinsic and acquired resistance. Reactivation of the MAPK pathway is a major contributor to treatment failure in BRAF-mutant melanomas, approximately ~80% of melanoma tumors becomes BRAF-inhibitor resistant due to reactivation of MAPK signalling. BRAF-inhibitor resistant tumor cells are sensitive to MEK inhibition, therefore cobimetinib and vemurafenib will result in dual inhibition of BRAF and its downstream target, MEK. Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Cobimetinib and vemurafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. Cobimetinib is used for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation. Cobimetinib is used in combination with vemurafenib, a BRAF inhibitor. Cobimetinib is marketed under the trade name Cotellic. 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 |
|---|
Adenocarcinoma (Phase 2)
Bile Duct Neoplasms (Phase 2)
Biliary Tract Neoplasms (Phase 2)
Brain Neoplasms (Phase 2)
Breast Neoplasms (Phase 2)
Carcinoma, Non-Small-Cell Lung (Phase 2/Phase 3)
Carcinoma, Squamous Cell (Phase 2)
Cholangiocarcinoma (Phase 2)
Colorectal Neoplasms (Phase 3)
Craniopharyngioma (Phase 2)
Endometrial Neoplasms (Phase 1)
Erdheim-Chester Disease (Phase 2/Phase 3)
Esophageal Neoplasms (Phase 1/Phase 2)
Fallopian Tube Neoplasms (Phase 2)
Gallbladder Neoplasms (Phase 2)
Gastrointestinal Neoplasms (Phase 2)
Glioma (Phase 2/Phase 3)
Hamartoma (Phase 2)
Healthy Volunteers (Phase 1)
Histiocytic Disorders, Malignant (Phase 2)
Histiocytic Sarcoma (Phase 2)
Histiocytosis (Phase 3)
Histiocytosis, Sinus (Phase 2)
Intestinal Neoplasms (Phase 2)
Laryngeal Neoplasms (Phase 2/Phase 3)
Leukemia, Myeloid, Acute (Phase 1/Phase 2)
Leukemia, Myelomonocytic, Chronic (Phase 2)
Lymphoma, Non-Hodgkin (Phase 2)
Melanoma (Phase 3)
Multiple Myeloma (Phase 2/Phase 3)
Mutation (Phase 2)
Neoplasm Metastasis (Phase 2)
Neoplasms ()
Neoplastic Syndromes, Hereditary (Phase 2)
Neurodegenerative Diseases (Phase 2)
Ovarian Neoplasms (Phase 2/Phase 3)
Pancreatic Neoplasms (Phase 2)
Prostatic Neoplasms (Phase 2)
Sarcoma (Phase 2)
Sarcoma, Clear Cell (Phase 2)
Skin Neoplasms (Phase 1)
Thyroid Cancer, Papillary (Phase 2/Phase 3)
Thyroid Carcinoma, Anaplastic (Phase 2/Phase 3)
Thyroid Neoplasms (Phase 2)
Triple Negative Breast Neoplasms (Phase 1/Phase 2)
Urinary Bladder Neoplasms (Phase 2)
Venous Cutdown (Phase 2)
Xanthogranuloma, Juvenile (Phase 2)
| Trial | Phase | Start Date | Organizations | Indications |
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