Comparative Pharmacology
Head-to-head clinical analysis: MEKINIST versus TRAMETINIB DIMETHYL SULFOXIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MEKINIST versus TRAMETINIB DIMETHYL SULFOXIDE.
MEKINIST vs TRAMETINIB DIMETHYL SULFOXIDE
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.
Trametinib is a reversible, selective inhibitor of MEK1 and MEK2, downstream effectors of the RAS/RAF/MEK/ERK signaling pathway, thereby inhibiting cell proliferation.
2 mg orally once daily, at least 1 hour before or 2 hours after a meal.
2 mg orally once daily.
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 approximately 5.3 days (127 hours); supports once-daily dosing with steady-state achieved in ~21 days.
Fecal (80% as unchanged drug and metabolites), renal (<1% unchanged)
Primarily fecal (80%), with 20% excreted in urine; less than 0.1% recovered unchanged in urine.
Category C
Category C
MEK Inhibitor
MEK Inhibitor