Comparative Pharmacology
Head-to-head clinical analysis: MEKINIST versus MEKTOVI.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MEKINIST versus MEKTOVI.
MEKINIST vs MEKTOVI
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Reversible, selective inhibitor of MEK1 and MEK2, which are downstream kinases in the RAS/RAF/MEK/ERK signaling pathway. Inhibition prevents phosphorylation and activation of ERK, thereby reducing cell proliferation in BRAF V600 mutant tumors.
MEKTOVI (binimetinib) is a reversible, non-competitive inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2. It inhibits the MAPK/ERK pathway, which is activated in tumors with BRAF mutations.
2 mg orally once daily, at least 1 hour before or 2 hours after a meal.
45 mg orally twice daily, approximately 12 hours apart
None Documented
None Documented
Terminal half-life of 3.9 days (93.6 hours) in patients; supports once-daily dosing and steady-state achieved in ~19 days
Terminal elimination half-life is approximately 3.7 days (range 2.5–6.3 days) in patients with advanced solid tumors. This long half-life supports once-daily dosing.
Fecal (80% as unchanged drug and metabolites), renal (<1% unchanged)
Primarily fecal (94% of total radioactivity) with minimal renal excretion (4% of total radioactivity). Unchanged drug accounts for approximately 27% of the dose in feces.
Category C
Category C
MEK Inhibitor
MEK Inhibitor