Dasatinib
Tyrosine kinase inhibitors
MECHANISM OF ACTION
BCR-ABL cellular tyrosine kinase inhibitor
MECHANISM OF KIDNEY INJURY
Water/electrolyte disturbances
CLINICAL KIDNEY SYNDROME
TMA extremely rare. Appears to be one case with dasatinib induced nephrotic syndrome.
CARDIOVASCULAR ADVERSE EFFECTS
edema, hypertension, arrhythmia, cardiomyopathy (CHF)
LYTE ABNORMALITIES
unclear. One case of nephrotic syndrome.
RISK FACTORS
MITIGATION STRATEGIES
unclear
SUGGESTIONS
Check UA with urine culture, Check urine analysis for cyrstals, WBC, RBC, etc, Check urine protein creatinine ratio
NOTES/COMMENTS
Dasatinib 96%; active metabolite 93%
PHARMACOKINETICS
Molecular Weight
488.01 g/mol
Volume of Distribution
2505 L
Plasma Protein Binding
Metabolism
Hepatic: via CYP3A4 (primarily), FOM-3 and UFT to an active metabolite (plays only a minor role in pharmacology of dasatinib) and other inactive metabolites
Bioavailability
14 to 34%
Half-life elimination
3 to 5 hours
Time to peak
0.5 to 6 hours
Excretion
Feces (85%. 19% as unchanged drug); urine (4%, 0.1% as unchanged drug)
Dialyzable?
Unknown
REF:
PATHOLOGY SLIDES:
ENTRY UPDATES:
Raad Chowdhury
MN/USA
Sep 25, 2022