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dasatinib (Sprycel)

Tradename: Sprycel Indications: 1) chronic myeloid leukemia (CML) 2) Philadelphia chromosome + acute lymphoblastic leukemia (ALL) 3) for patients not responding to other therapies Dosage: usual dose is 70 mg PO BID Tabs: 20, 50, 70, 80, 100, 140 mg [5] Pharmacokinetics: - metabolized by CYP3A4 Adverse effects: 1) bleeding 2) diarrhea 3) skin rash 4) infections 5) headache 6) fatigue 7) edema 8) nausea 9) anemia 10) neutropenia 11) thrombocytopenia 12) abnormal liver function tests 13) pulmonary hypertension (rare) [3,4] 14) pericardial effusion [4] 15) pleural effusion [4] Drug interactions: 1) levels may be increased by drugs that inhibit cyt P450 3A4 2) levels may be decreased by drugs that induce cyt P450 3A4 - St John's wort, carbamazepine, phenobarbital, phenytoin, primidone, others 3) proton pump inhibitors may decrease absorption of dasatinib Mechanism of action: 1) tyrosine kinase inhibitor 2) inhibits proliferation of abnormal leukocytes 3) said to act similarly to imatinib (Gleevec) 4) may inhibit bcl-abl 5) inhibits CSF1R Bristol-Myers Squibb Cost $5000/month 2006

Interactions

drug adverse effects of tyrosine kinase inhibitor(s)

General

antineoplastic tyrosine kinase inhibitor small inhibitory antineoplastic agent (ib drug)

Properties

INHIBITS: protein kinase

Database Correlations

PUBCHEM cid=3062316

References

  1. Prescriber's Letter 13(8): 2006 FDA Approves Sprycel, a New Treatment for a Rare Type of Leukemia Detail-Document#: 220812 (subscription needed) http://www.prescribersletter.com
  2. Cortes JE et al Results of dasatinib therapy in patients with early chronic- phase chronic myeloid leukemia. J Clin Oncol 2010 Jan 20; 28:398. PMID: 20008620
  3. FDA MedWatch: 10/11/2011 Sprycel (dasatinib): Drug Safety Communication - Risk of Pulmonary Arterial Hypertension http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm275176.htm
  4. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
  5. dasatinib (Rx) Medscape https://reference.medscape.com/drug/sprycel-dasatinib-342199