Comparative Pharmacology
Head-to-head clinical analysis: DASATINIB versus PEMAZYRE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DASATINIB versus PEMAZYRE.
DASATINIB vs PEMAZYRE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Dasatinib is a tyrosine kinase inhibitor that targets BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. It inhibits BCR-ABL autophosphorylation and downstream signaling, leading to apoptosis in Philadelphia chromosome-positive (Ph+) leukemia cells.
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.
140 mg orally once daily; reduce to 100 mg once daily if no cytogenetic response after 3 months or 140 mg once daily with dose escalation to 200 mg once daily as tolerated.
13.5 mg orally once daily continuously until disease progression or unacceptable toxicity.
None Documented
None Documented
Clinical Note
moderateDasatinib + Deslanoside
"Dasatinib may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateDasatinib + Acetyldigitoxin
"Dasatinib may decrease the cardiotoxic activities of Acetyldigitoxin."
Clinical Note
moderateDasatinib + Ouabain
"Dasatinib may decrease the cardiotoxic activities of Ouabain."
Clinical Note
moderateDasatinib + Tenofovir disoproxil
"The metabolism of Tenofovir disoproxil can be decreased when combined with Dasatinib."
Terminal elimination half-life is 3-5 hours. This short half-life supports twice-daily dosing, but active metabolite (N-desmethyl dasatinib) has a similar half-life and contributes to PD activity.
Terminal elimination half-life is approximately 20 hours (range 14–32 h), supporting once-daily dosing with steady-state reached within 8 days.
Approximately 85% of the dose is eliminated via feces (mainly as metabolites), and about 4% via urine (parent drug and metabolites). Less than 1% is excreted unchanged in urine.
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).
Category D/X
Category C
Kinase Inhibitor
Kinase Inhibitor