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dasatinib (Rx)Brand and Other Names:Sprycel

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 20mg
  • 50mg
  • 70mg
  • 80mg
  • 100mg
  • 140mg
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CML, Chronic Phase (Newly Diagnosed)

Indicated for newly diagnosed adults with Philadelphia chromosome-positive chronic phase chronic myeloid leukemia (Ph+ CP-CML)

Start 100 mg PO qDay (morning or evening)

May increase to 140 mg qDay if inadequate response

CML, Advanced

Indicated for treatment of chronic, accelerated, or myeloid or lymphoid blast phase Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) with resistance or intolerance to prior therapy including imatinib

Start 140 mg PO qDay

May increase to 180 mg qDay if inadequate response

ALL, Ph+

Indicated for Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL) with resistance or intolerance to prior therapy

Start 140 mg PO qDay

May increase to 180 mg PO qDay if inadequate response

Hepatic Impairment

Dose adjustment not necessary

Administration

Take with or without meals

Swallow tablet whole; do not cut, crush, or chew

Dose Modification

Myelosuppression: Reduce/interrupt dose, see Manufacturer's PI

Monitor: CBC qWeek for 2 months, THEN qMonth

Concomitant Strong CYP3A4 Inducers/Inhibitors

  • Avoid or modify dose
  • Concomitant strong CYP3A4 inducers: May decrease dasatinib plasma concentrations; consider increasing dose (monitor for toxicity)
  • Concomitant strong CYP3A4 inhibitors: May increase dasatinib plasma concentrations; decrease to 20 mg/day if taking 100 mg/day; decrease to 40 mg/day if taking 140 mg/day
  • If not tolerated despite dose reduction, discontinue strong CYP3A4 inhibitor and allow washout of 1 week before dasatinib dose increased, OR
  • Discontinue dasatinib until treatment with CYP3A4 inhibitor ceased

<18 years: Safety and efficacy not established

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Interactions

Interaction Checker

dasatinib and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Fluid retention, incl CHF, pulm edema, pleural effusion (50%)

            Diarrhea (49%)

            Headache (40%)

            Hemorrhage (40%)

            Fatigue (39%)

            Pyrexia (39%)

            Skin rash (35%)

            Infection (34%)

            Nausea (34%)

            Dyspnea (32%)

            Cough (28%)

            Pain (26%)

            Abdominal pain (25%)

            Vomiting (22%)

            Anorexia (19%)

            Arthralgia (19%)

            Asthenia (19%)

            Constipation (14%)

            Dizziness (14%)

            Musculoskeletal pain (14%)

            Weight loss (14%)

            Chest pain (13%)

            Neuropathy (13%)

            Myalgia (12%)

            Abdominal distention (11%)

            Arrhythmia (11%)

            Chills (11%)

            Pneumonia (11%)

            Pruritus (11%)

            Weight gain (11%)

            1-10% (selected)

            Anemia

            Febrile neutropenia

            Thrombocytopenia

            Mucosal inflammation

            Postmarketing Reports

            Cardiac disorders: Atrial fibrillation/atrial flutter

            Vascular disorders: Thrombosis/embolism (including pulmonary embolism, deep vein thrombosis)

            Respiratory, thoracic, and mediastinal disorders: Interstitial lung disease, pulmonary arterial hypertension

            Dermatologic reactions: Stevens-Johnson syndrome, erythema multiforme

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            Warnings

            Contraindications

            None

            Cautions

            Myelosuppression including severe thrombocytopenia, neutropenia and anemia may occur; may manage by dose interruption, dose reduction, or discontinuation of therapy; hematopoietic growth factor has been used with resistant myelosuppression

            In patients with chronic phase CML, perform complete blood counts (CBCs) every 2 weeks for 12 weeks, then every 3 months thereafter, or as clinically indicated; perform CBCs weekly for the first 2 months and then monthly thereafter, or as clinically indicated in patients with advanced phase CML or Ph+ ALL

            CNS and gastrointestinal hemorrhages, including fatalities have occurred; severe hemorrhage may require treatment interruption and transfusion

            Increased risk of developing pulmonary arterial hypertension (PAH); may be reversible on discontinuation; evaluate patients for signs and symptoms of underlying cardiopulmonary disease prior to initiation and during treatment; if PAH confirmed permanently discontinue therapy

            Hypokalemia, hypomagnesemia, congenital QT interval prolongation, hepatic impairment

            Use with caution in patients who have or may develop prolongation of QT interval

            Cardiac adverse reactions were reported in 5.8% of 258 patients including cardiomyopathy (1.6%), congestive heart failure, diastolic dysfunction, fatal myocardial infarction, and left ventricular dysfunction

            Cases of severe mucocutaneous dermatologic reactions, including Stevens-Johnson syndrome and erythema multiforme, reported; discontinue permanently in patients who experience severe mucocutaneous reaction during treatment if no other etiology can be identified

            Risk of tumor lysis syndrome

            Risk of fluid retention and pleural/pericardial effusion

            Embryofetal toxicity reported; advise female patients of reproductive potential to avoid pregnancy during treatment

            Avoid concomitant CYP3A4 inducers/inhibitors

            • If unavoidable, consider dose modification as appropriate
            • Decrease from 100 mg/day to 20 mg/day if concomitant strong CYP3A4 inhibitor
            • Decrease from 140 mg/day to 40 mg/day if concomitant strong CYP3A4 inhibitor
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            Pregnancy & Lactation

            Pregnancy Category: D

            Transplacental transfer of dasatinib reported; dasatinib has been measured in fetal plasma and amniotic fluid and concentrations were found to be comparable to those in maternal plasma

            Hydrops fetalis and fetal bicytopenia have been reported with maternal exposure to dasatinib

            Lactation: not known if excreted in breast milk; do not nurse

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Multi-kinase inhibitor that inhibits BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-Kit, EPHA2 and PDGFR-beta kinases; tyrosine kinase inhibition possibly blocks angiogenesis and cellular proliferation

            Absorption

            Peak Plasma Time: 0.5-6 hr

            Distribution

            Protein Bound: 96%

            Vd: 2505 L

            Metabolism

            Metabolism: extensively metabolized primarily by CYP3A4

            Enzymes inhibited: CYP3A4 (weak)

            Elimination

            Half-Life: 3-5 hr

            Excretion: Feces 85%; urine 4%

            Pharmacogenomics

            Tyrosine kinase inhibitors (TKIs) inhibit activity of BCR-ABL fusion protein, resulting in both hematologic response (ie, normal cell counts in the peripheral blood and normal bone marrow morphology), as well as cytogenetic response (ie, disappearance or reduction of the Philadelphia [Ph] chromosome)

            NCCN clinical practice guidelines recommends TKIs in CML with confirmed BCR-ABL transcripts in bone marrow or evidence of translocation on cytogenetics

            Genetic testing laboratories

            • The following companies currently offer FISH and/or transcript quantification testing for BCR-ABL
            • Asuragen (http://www.asuragen.com/)
            • Dako (http://www.dakousa.com/)
            • Invitrogen (http://www.invitrogen.com/)
            • Ipsogen (http://www.ipsogen.com)
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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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