PD-0325901 (Not yet branded)

Other Medications

US Experimental EU Experimental ES Not available Oral 3 Clinical Trials
MEK1 MEK2

Description

PD-0325901 is a potent, selective MEK inhibitor that targets the mitogen-activated protein kinase (MAPK) signaling pathway in colorectal cancer. This compound has been evaluated specifically in combination therapies for KRAS-mutant colorectal cancers, where aberrant MEK signaling drives tumor growth. It represents a targeted approach to block downstream effects of KRAS mutations, which occur in approximately 40-50% of colorectal cancer patients and confer resistance to EGFR-targeted therapies.

Mechanism of Action

PD-0325901 works by selectively inhibiting MEK1 and MEK2, which are critical kinases in the RAS/RAF/MEK/ERK signaling cascade. By blocking MEK activity, the drug prevents phosphorylation and activation of ERK, thereby disrupting cellular proliferation, survival signals, and tumor growth in KRAS-mutant cancer cells.

Molecular Targets

Side Effects

Diarrhea Skin rash Fatigue Nausea Peripheral edema Blurred vision Decreased ejection fraction Elevated liver enzymes

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

Clinical Trials

NCT02510001 Phase 1
Archived
MEK and MET Inhibition in Colorectal Cancer
United Kingdom
NCT02039336 Phase 1
Archived
Dacomitinib Plus PD-0325901 in Advanced KRAS Mutant NSCLC
Netherlands
NCT00147550 Phase 1
Archived
MEK Inhibitor PD-325901 To Treat Advanced Breast Cancer, Colon Cancer, And Melanoma.
United States