Comparative Pharmacology
Head-to-head clinical analysis: PEMAZYRE versus RETEVMO.
Peer-Reviewed Evidence
Head-to-head clinical analysis: PEMAZYRE versus RETEVMO.
PEMAZYRE vs RETEVMO
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selective inhibitor of fibroblast growth factor receptor (FGFR) 1, 2, 3, and 4; binds to and inhibits FGFR kinase activity, leading to decreased tumor cell proliferation and angiogenesis.
RETEVMO (selpercatinib) is a potent and selective RET kinase inhibitor. It inhibits wild-type RET and multiple RET fusions (e.g., KIF5B-RET, CCDC6-RET) and mutations (e.g., M918T, C634W, V804M/L/E) by binding to the ATP-binding site of RET, blocking downstream signaling pathways including MAPK/ERK and PI3K/AKT, thereby inhibiting tumor cell proliferation.
13.5 mg orally once daily continuously until disease progression or unacceptable toxicity.
160 mg orally twice daily
None Documented
None Documented
Terminal elimination half-life is approximately 20 hours (range 14–32 h), supporting once-daily dosing with steady-state reached within 8 days.
18 hours (terminal elimination half-life) supporting twice-daily dosing; steady-state reached within ~3 days.
Primarily hepatobiliary excretion: 72% of the dose recovered in feces (mainly as unchanged drug and metabolites); renal excretion accounts for approximately 17% (less than 1% unchanged).
Primarily biliary/fecal (approximately 75% of administered dose recovered in feces as unchanged drug and metabolites); renal elimination accounts for <10% (mostly metabolites).
Category C
Category C
Kinase Inhibitor
Kinase Inhibitor