Comparative Pharmacology
Head-to-head clinical analysis: CAPRELSA versus DASATINIB.
Head-to-head clinical analysis: CAPRELSA versus DASATINIB.
CAPRELSA vs DASATINIB
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Inhibits multiple receptor tyrosine kinases involved in tumor angiogenesis and oncogenesis, including VEGFR2, EGFR, and RET.
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.
300 mg orally once daily, with or without food.
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.
None Documented
None Documented
Terminal half-life approximately 90 hours (range 30–150 hours), supporting once-daily dosing; steady-state achieved by day 15.
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.
Primarily fecal (approximately 75% of administered dose, mainly as unchanged drug and metabolites); renal excretion accounts for about 25% (less than 1% unchanged).
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.
Category C
Category D/X
Kinase Inhibitor
Kinase Inhibitor