Ci-1040 (Not yet branded)

Other Medications

US Experimental EU Experimental ES Not available Oral 2 Clinical Trials
MEK1 MEK2

Description

CI-1040 is a small molecule MEK inhibitor that targets the mitogen-activated protein kinase (MAPK) pathway in colorectal cancer treatment. This compound specifically inhibits MEK1 and MEK2 kinases, which are critical components of the RAS/RAF/MEK/ERK signaling cascade frequently dysregulated in colorectal malignancies. CI-1040 was developed to block tumor cell proliferation and survival signals in advanced colorectal cancer patients, particularly those with RAS pathway mutations.

Mechanism of Action

CI-1040 works by selectively binding to and inhibiting MEK1 and MEK2 kinases, preventing the phosphorylation and activation of downstream ERK1/2 proteins. This inhibition disrupts the RAS/RAF/MEK/ERK signaling pathway, leading to decreased tumor cell proliferation, increased apoptosis, and reduced angiogenesis in colorectal cancer cells with aberrant MAPK pathway activation.

Molecular Targets

Side Effects

Diarrhea Fatigue Nausea Rash Peripheral edema Visual disturbances Elevated liver enzymes Decreased ejection fraction

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT00033384 Phase 2
Archived
CI-1040 in Treating Patients With Advanced Breast, Colon, Pancreatic, or Non-Small Cell Lung Cancer
United States
NCT00034827 Phase 2
Archived
A Multicenter Phase 2 Study of CI-1040 in Patients With Advanced Nonsmall-Cell Lung, Breast, Colon and Pancreatic Cancer
United States