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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

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