gemtuzumab (Rx)

Brand and Other Names:Mylotarg
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injection, lyophilized cake powder for reconstitution

  • 4.5 mg/single-dose vial

Acute Myeloid Leukemia

Newly Diagnosed CD33-positive AML

  • Indicated for newly diagnosed CD33-positive AML in adults
  • Combination regimen
    • Induction cycle: 3 mg/m2 IV (up to one 4.5-mg vial) on Days 1, 4, and 7 in combination with daunorubicin and cytarabine
    • For patients requiring a second induction cycle, do not administer gemtuzumab during second induction cycle
    • Consolidation: 3 mg/m2 IV on Day 1 (up to one 4.5-mg vial) in combination with daunorubicin and cytarabine
  • Monotherapy
    • Treatment course consists of 1 cycle of induction and up to 8 cycles of continuation therapy
    • Induction: 6 mg/m2 IV on Day 1, and 3 mg/m2 on Day 8
    • Continuation therapy: 2 mg/m2 IV on Day 1 q4weeks

Relapsed or Refractory CD33-positive AML

  • Indicated for relapsed/refractory CD33-positive AML
  • 3 mg/m2 on Days 1, 4, and 7 for 1 cycle

Dosing Modifications

Veno-occlusive disease (VOD): Discontinue treatment

Renal impairment

  • Mild-moderate (CrCl: 30-89 mL/min): No dosage adjustment necessary
  • Severe (CrCl: 15-29 mL/min): Safety and efficacy unknown

Hepatic impairment

  • Mild (total bilirubin <1.5X ULN): No dosage adjustment necessary
  • Moderate (total bilirubin >1.5-3x ULN) or severe (total bilirubin >3x ULN): Unknown

Total bilirubin >2x ULN, or AST and/or ALT >2.5x ULN

  • Hold treatment until total bilirubin to ≤2x ULN and AST/ALT to ≤2.5x ULN prior to each dose
  • Omit scheduled dose if delayed >2 days between sequential infusions

Infusion-related reactions

  • Interrupt infusion and institute appropriate medical management
  • Administer acetaminophen, diphenhydramine, and/or methylprednisolone, if needed
  • Provide supportive care measures as needed
  • Consider resuming the infusion at less than or half the rate at which the reaction occurred once symptoms resolve
  • Repeat the procedure above in the event of recurrence of symptoms
  • Permanently discontinue gemtuzumab if a severe infusion reaction occurs or for any life-threatening infusion reaction

Other severe/life-threatening nonhematologic toxicities

  • Hold treatment until reaction severity is no more than mild
  • Omit scheduled dose if delayed more than 2 days between sequential infusions

Combination therapy only

  • Persistent thrombocytopenia
    • If platelet count does not recover to >100 Gi/L within14 days following the planned start date of the consolidation cycle (14 days after hematologic recovery following previous cycle), discontinue gemtuzumab
    • Do not administer gemtuzumab in the consolidation cycle
  • Persistent neutropenia
    • If neutrophil count does not recover to >0.5 Gi/L within14 days following the planned start date of the consolidation cycle (14 days after hematologic recovery following previous cycle), discontinue gemtuzumab
    • Do not administer gemtuzumab in the consolidation cycle

Dosing Considerations

Use appropriate measures to prevent tumor lysis syndrome

Patients with hyperleukocytosis (leukocyte count ≥30 Gi/L): Cytoreduction is recommended prior to gemtuzumab administration

Monitor blood cell counts frequently through resolution of cytopenias

Monitor blood cell counts and chemistries <3X/week through recovery from treatment-related toxicities

Dosage Forms & Strengths

injection, lyophilized cake powder for reconstitution

  • 4.5-mg/single-dose vial

Newly Diagnosed Acute Myeloid Leukemia

Indicated for newly-diagnosed CD33-positive acute myeloid leukemia (AML) in adults and pediatric patients aged ≥1 month

<1 month: Safety and efficacy not established

≥1 month

  • Body surface area (BSA) <0.6 m2: 0.1 mg/kg IV
  • BSA ≥0.6 m2: 3 mg/m2 IV
  • First induction cycle: Give once in combination with standard chemotherapy
  • Second induction cycle: No gemtuzumab given
  • First intensification cycle: No gemtuzumab given
  • Second intensification cycle: Give once in combination with standard chemotherapy; consider risks and potential benefits before giving gemtuzumab
  • Third intensification cycle: No gemtuzumab given

Relapse or refractory AML

Indicated for relapsed or refractory CD33-positive AML in adults and pediatric patients ≥2 years

3 mg/m2 (up to one 4.5-mg vial) on Days 1, 4, and 7 for 1 cycle

Dosing Modifications

Veno-occlusive disease (VOD): Discontinue treatment

Renal impairment

  • Mild-moderate (CrCl: 30-89 mL/min): No dosage adjustment necessary
  • Severe (CrCl: 15-29 mL/min): Safety and efficacy unknown

Hepatic impairment

  • Mild (total bilirubin <1.5x ULN): No dosage adjustment necessary
  • Moderate (total bilirubin >1.5-3x ULN) or severe (total bilirubin >3x ULN): Unknown

Combination therapy only

  • Persistent thrombocytopenia
    • Platelet count should be at least 75 Gi/L before the next cycle (induction or intensification)
  • Persistent neutropenia
    • Neutrophil count should be at least 1 Gi/L before the next cycle (induction or intensification)

Total bilirubin >2x ULN, or AST and/or ALT >2.5X ULN

  • Hold treatment until total bilirubin improves to ≤2x ULN and AST/ALT to ≤2.5x ULN prior to each dose
  • Omit scheduled dose if delayed >2 days between sequential infusions

Infusion-related reactions

  • Interrupt infusion and institute appropriate medical management
  • Administer acetaminophen, diphenhydramine, and/or methylprednisolone, if needed
  • Provide supportive care measures as needed
  • Consider resuming the infusion at less than or half the rate at which the reaction occurred once symptoms resolve
  • Repeat the procedure above in the event of recurrence of symptoms
  • Permanently discontinue gemtuzumab if a severe infusion reaction occurs or for any life-threatening infusion reaction

Other severe/life-threatening nonhematologic toxicities

  • Hold treatment until reaction severity is no more than mild
  • Omit scheduled dose if delayed more than 2 days between sequential infusions

Dosing Considerations

Use appropriate measures to prevent tumor lysis syndrome

Patients with hyperleukocytosis (leukocyte count ≥30 Gi/L): Cytoreduction is recommended prior to gemtuzumab administration

Monitor blood cell counts frequently through resolution of cytopenias

Monitor blood cell counts and chemistries <3X/week through recovery from treatment-related toxicities

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Interactions

Interaction Checker

and gemtuzumab

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            Contraindicated (0)

              Serious - Use Alternative (14)

              • bedaquiline

                bedaquiline and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug.

              • desflurane

                desflurane and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug.

              • efavirenz

                efavirenz and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug.

              • encorafenib

                encorafenib and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug.

              • entrectinib

                gemtuzumab and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

              • fexinidazole

                fexinidazole and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels or prolong QT interval.

              • glasdegib

                gemtuzumab and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.

              • hydroxychloroquine sulfate

                hydroxychloroquine sulfate and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug.

              • ivosidenib

                ivosidenib and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of QTc prolonging drugs with ivosidenib or replace with alternate therapies. If coadministration of a QTc prolonging drug is unavoidable, monitor for increased risk of QTc interval prolongation.

              • lefamulin

                lefamulin and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug.

              • macimorelin

                macimorelin and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug. Macimorelin causes an increase of ~11 msec in the corrected QT interval. Avoid coadministration with drugs that prolong QT interval, which could increase risk for developing torsade de pointes-type ventricular tachycardia. Allow sufficient washout time of drugs that are known to prolong the QT interval before administering macimorelin.

              • mobocertinib

                mobocertinib and gemtuzumab both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.

              • palifermin

                palifermin increases toxicity of gemtuzumab by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hr before, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.

              • pitolisant

                gemtuzumab and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.

              Monitor Closely (104)

              • acalabrutinib

                acalabrutinib, gemtuzumab. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may increase risk of myelosuppressive effects.

              • albuterol

                albuterol and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • alfuzosin

                alfuzosin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • amiodarone

                amiodarone and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • anagrelide

                anagrelide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • apomorphine

                apomorphine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • arformoterol

                arformoterol and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • aripiprazole

                aripiprazole and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • arsenic trioxide

                arsenic trioxide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • artemether

                artemether and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • artemether/lumefantrine

                artemether/lumefantrine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • asenapine

                asenapine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • atomoxetine

                atomoxetine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • azithromycin

                azithromycin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • ceritinib

                ceritinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • chloroquine

                chloroquine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • chlorpromazine

                chlorpromazine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • chlorpropamide

                chlorpropamide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • ciprofloxacin

                ciprofloxacin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • citalopram

                citalopram and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • clarithromycin

                clarithromycin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • clofazimine

                clofazimine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • clozapine

                clozapine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • crizotinib

                crizotinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • dasatinib

                dasatinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • degarelix

                degarelix and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • dengue vaccine

                gemtuzumab decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine.

              • deutetrabenazine

                deutetrabenazine and gemtuzumab both increase QTc interval. Modify Therapy/Monitor Closely. For patients requiring deutetrabenazine doses >24 mg/day and are taking other drugs known to prolong QTc, assess the QTc interval before and after increasing the dose of deutetrabenazine or other medications known to prolong QTc.

              • disopyramide

                disopyramide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • dofetilide

                dofetilide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • dolasetron

                dolasetron and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • donepezil

                donepezil and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • doxepin

                doxepin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • droperidol

                droperidol and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • eribulin

                eribulin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • erythromycin base

                erythromycin base and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • erythromycin ethylsuccinate

                erythromycin ethylsuccinate and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • erythromycin lactobionate

                erythromycin lactobionate and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • erythromycin stearate

                erythromycin stearate and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • escitalopram

                escitalopram increases toxicity of gemtuzumab by QTc interval. Use Caution/Monitor.

              • ezogabine

                ezogabine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • fingolimod

                fingolimod and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • flecainide

                flecainide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • fluconazole

                fluconazole and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • fostemsavir

                gemtuzumab and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.

              • goserelin

                goserelin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • granisetron

                granisetron and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • haloperidol

                haloperidol and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • histrelin

                histrelin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • ibutilide

                ibutilide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • iloperidone

                iloperidone and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • indacaterol, inhaled

                indacaterol, inhaled and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • inotuzumab

                inotuzumab and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • lapatinib

                lapatinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • lenvatinib

                lenvatinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • leuprolide

                leuprolide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • levofloxacin

                levofloxacin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • lopinavir

                lopinavir and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • lumefantrine

                lumefantrine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • methadone

                methadone and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • mifepristone

                mifepristone and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • moxifloxacin

                moxifloxacin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • nilotinib

                nilotinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • ofatumumab SC

                ofatumumab SC, gemtuzumab. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.

              • ofloxacin

                ofloxacin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • olaparib

                gemtuzumab and olaparib both increase pharmacodynamic synergism. Use Caution/Monitor. Coadministration with other other myelosuppressive anticancer agents, including DNA damaging agents, may potentiate and prolongate the myelosuppressive toxicity.

              • ondansetron

                ondansetron and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • osilodrostat

                osilodrostat and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • osimertinib

                osimertinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • oxaliplatin

                oxaliplatin will increase the level or effect of gemtuzumab by Other (see comment). Use Caution/Monitor. Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT interval.

              • paliperidone

                paliperidone and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • panobinostat

                panobinostat and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • pasireotide

                pasireotide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • pazopanib

                pazopanib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • pentamidine

                pentamidine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • perflutren

                perflutren and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • pimavanserin

                pimavanserin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • pimozide

                pimozide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • ponesimod

                ponesimod and gemtuzumab both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

              • procainamide

                procainamide and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • propafenone

                propafenone and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • quetiapine

                quetiapine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • quinidine

                quinidine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • ranolazine

                ranolazine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • ribociclib

                ribociclib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • romidepsin

                romidepsin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • saquinavir

                saquinavir and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • selpercatinib

                selpercatinib increases toxicity of gemtuzumab by QTc interval. Use Caution/Monitor.

              • siponimod

                siponimod and gemtuzumab both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

              • sorafenib

                sorafenib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • sotalol

                sotalol and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • sunitinib

                sunitinib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • telavancin

                telavancin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • thioridazine

                thioridazine and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • toremifene

                toremifene and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • trastuzumab

                trastuzumab, gemtuzumab. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

              • trastuzumab deruxtecan

                trastuzumab deruxtecan, gemtuzumab. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

              • trazodone

                trazodone and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • triptorelin

                triptorelin and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • vandetanib

                vandetanib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • vemurafenib

                vemurafenib and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • voclosporin

                voclosporin, gemtuzumab. Either increases effects of the other by QTc interval. Use Caution/Monitor.

              • voriconazole

                voriconazole and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              • ziprasidone

                ziprasidone and gemtuzumab both increase QTc interval. Use Caution/Monitor.

              Minor (0)

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                Adverse Effects

                >10% (Newly diagnosed plus Daunorubicin and Cytarabine)

                Hypophosphatemia, grade 3 or higher (64%)

                Hypokalemia, grade 3 or higher (57%)

                Infection, grade 3 or higher (47-55%)

                Hyponatremia, grade 3 or higher (44%)

                Prolonged thrombocytopenia (19-35%)

                Hemorrhage, grade 3 or higher (5-18%)

                AST increased, grade 3 or higher (14%)

                Alkaline phosphatase increased, grade 3 or higher (13%)

                >10% (Monotherapy for Relapsed)

                Fever, all grades (79%)

                Infection, all grades (42%)

                Increased AST, all grades (40%)

                Bleeding, all grades (23%)

                Nausea and vomiting, all grades (21%)

                Constipation, all grades (21%)

                Mucositis, all grades (21%)

                Headache, all grades (19%)

                Increased ALT, all grades (16%)

                Rash, all grades (16%)

                Sepsis, grade 3 (32%)

                Fever, grade 3 (16%)

                Rash, grade 3 (11%)

                1-10% (Newly diagnosed plus Daunorubicin and Cytarabine)

                ALT increased, grade 3 or higher (10%)

                Blood bilirubin increased, grade 3 or higher (8%)

                Prolonged neutropenia (2-3%)

                Veno-occlusive disease, grade 3 or higher (2%)

                1-10% (Monotherapy for Relapsed)

                Hyperbilirubinemia (7%)

                Pneumonia, grade 3 (7%)

                Bleeding, grade 3 (7%)

                Mucositis, grade 3 (4%)

                Pain, grade 3 (4%)

                Diarrhea, grade 3 (2%)

                Headaches, grade 3 (2%)

                Tachycardia, grade 3 (2%)

                Lung edema, grade 3 (2%)

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                Warnings

                Black Box Warnings

                Hepatotoxicity, including severe or fatal veno-occlusive disease (VOD), also known as sinusoidal obstruction syndrome (SOS), has been reported in association with the use of gemtuzumab

                In clinical trials, the risk of VOD was higher in adults who received higher gemtuzumab doses as monotherapy, in patients with moderate/severe hepatic impairment prior to treatment, in patients treated with gemtuzumab after HSCT, and in patients who underwent hematopoietic stem cell transplantation (HSCT), after treatment with gemtuzumab

                Assess ALT, AST, total bilirubin, and alkaline phosphatase prior to each gemtuzumab dose

                Monitor frequently for signs/symptoms of VOD (eg, elevations in ALT, AST, total bilirubin, hepatomegaly, rapid weight gain, ascites) after treatment; monitoring only total bilirubin may not identify all patients at risk of VOD

                Patients who develop abnormal liver tests: More frequent monitoring of liver tests and clinical signs/symptoms of hepatotoxicity is recommended

                Patients who proceed to HSCT: Monitor liver tests frequently during the post-HSCT period, as appropriate

                Manage signs or symptoms of hepatic toxicity by dose interruption or discontinuation

                In patients who experience VOD, discontinue treatment and treat according to standard medical practice

                Contraindications

                Hypersensitivity to the active substance in gemtuzumab or any of its components or to any of the excipients

                Cautions

                Hepatotoxicity, including severe or fatal VOD also known as SOS, has been reported; see Black Box Warnings

                For patients being treated with gemtuzumab in combination with daunorubicin and cytarabine for newly diagnosed de novo AML, when cytogenetics testing results become available consider whether the potential benefit of continuing treatment outweighs the risks for the individual patient

                Animal data report gemtuzumab may cause embryo-fetal harm when administered to pregnant women; see Pregnancy

                Infusion-related reactions

                • Life-threatening or fatal infusion related-reactions can occur during or within 24 hr following gemtuzumab infusion
                • Premedicate prior to gemtuzumab infusion
                • Monitor vital signs frequently during infusion
                • Interrupt infusion immediately for patients who are suspected of infusion-related reaction, especially dyspnea, bronchospasm, or hypotension
                • Monitor patients during and for ≥1 hr after infusion completed or until signs/symptoms completely resolve
                • Discontinue gemtuzumab use in patients who develop signs or symptoms of anaphylaxis (eg, severe respiratory symptoms or clinically significant hypotension)

                Hemorrhage

                • Risk of fatal or life-threatening hemorrhage owing to prolonged thrombocytopenia
                • Proportion of patients with persistent thrombocytopenia increased with progressive treatment phases and was higher in patients treated with combination therapy plus gemtuzumab than with chemotherapy alone
                • Assess blood cell counts prior to each gemtuzumab dose; monitor frequently after treatment until resolution of cytopenias
                • Monitor patients for signs/symptoms of bleeding during treatment; manage severe bleeding, hemorrhage, or persistent thrombocytopenia by treatment interruption or discontinuation and provide appropriate medical care

                QT interval prolongation

                • QT interval prolongation has been observed in patients treated with other drugs containing calicheamicin
                • Obtain ECG and electrolytes before initiating drug and during treatment as needed in patients with history of or predisposition for QTc prolongation, who are taking drugs known to prolong QT interval, or with electrolyte disturbances
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                Pregnancy

                Pregnancy

                Based on animal data, gemtuzumab can cause embryo-fetal harm when administered to a pregnant woman

                No available data on gemtuzumab use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage

                In rat embryo-fetal development studies, gemtuzumab ozogamicin caused embryofetal toxicity at maternal systemic exposures that ≥0.4 times the exposure in patients at the maximum recommended dose, based on AUC

                For patients who are pregnant, or become pregnant during treatment, advise the patient of the potential risk to a fetus

                Verify the pregnancy status of females of reproductive potential prior to initiating treatment

                Gemtuzumab may impair fertility in male or females of reproductive potential

                Contraception

                • Advise females of reproductive potential to avoid becoming pregnant while receiving gemtuzumab
                • Advise females of reproductive potential to use effective contraception during treatment and for at least 6 months after last dose
                • Advise males with female partners of reproductive potential to use effective contraception during treatment and for at least 3 months after last dose

                Lactation

                No data on the presence of gemtuzumab ozogamicin or its metabolites in human milk, the effects on the breastfed infant, or the effects on milk production

                Owing to potential for adverse reactions in breastfed infants, women should not breastfeed during treatment and for at least 1 month after the final dose

                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

                CD33-directed antibody-drug conjugate (ADC); the antibody portion (hP67.6) recognizes human CD33 antigen and the small molecule, N-acetyl gamma calicheamicin, is a cytotoxic agent that is covalently attached to the antibody via a linker

                Nonclinical data suggest that the anticancer activity results from ADC binding to CD33-expressing tumor cells, followed by internalization of the ADC-CD33 complex, and intracellular release of N-acetyl gamma calicheamicin dimethyl hydrazide via hydrolytic cleavage of the linker

                Activation of N-acetyl gamma calicheamicin dimethyl hydrazide induces double-strand DNA breaks, subsequently inducing cell cycle arrest and apoptotic cell death

                Absorption

                Peak plasma concentration: 3 mg/mL (first dose); 3.6 mg/mL (second dose)

                Distribution

                Protein bound: 97% (N-acetyl gamma calicheamicin dimethyl hydrazide)

                Vd: ~21.4 L (hP67.6 antibody)

                Metabolism

                N-acetyl gamma calicheamicin dimethyl hydrazide is extensively metabolized, primarily via nonenzymatic reduction of the disulfide moiety

                Elimination

                Half-life (hP67.6 antibody): 62 hr (first dose); 90 hr (second dose)

                Clearance (hP67.6 antibody): 0.35 L/hr (first dose); 0.15 L/hr (second dose)

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                Administration

                IV Compatibilities

                0.9% NaCl

                IV Preparation

                Cytotoxic drug; follow applicable special handling and disposal procedures

                Reconstitution

                • Calculate dose in mg and determine number of vials required
                • Allow vials to reach ambient temperature for ~5 minutes
                • Reconstitute each vial with 5 mL sterile water for injection to obtain a concentration of 1 mg/mL
                • Do not shake; gently swirl vial to aid dissolution
                • Inspect reconstituted solution for particulates and discoloration
                • Reconstituted solution may contain small white to off-white, opaque-to-translucent, and amorphous to fiber like particles
                • Contains no bacteriostatic preservatives
                • Use solution immediately to further dilute or refrigerate (see Storage)

                Further dilution required

                • Calculate the required volume of the reconstituted solution needed to obtain the appropriate dose according to patient body surface area
                • Withdraw this amount from the vial(s) using a syringe; discard unused reconstituted solution
                • Remove a volume of 0.9% NaCl from the prefilled bag equal to the volume of product (mL) calculated above
                • Add reconstituted solution to infusion container with 0.9% NaCl to make a total volume of 50 mL or 100 mL, depending on dose
                • Do not shake; gently invert infusion container to mix diluted solution

                Premedication

                Children and adolescents

                • Premediate 1 hr before with acetaminophen and diphenhydramine, then 30 min before with methylprednisolone
                • Acetaminophen 15 mg/kg (not to exceed 650 mg/dose) PO AND
                • Diphenhydramine 1 mg/kg (not to exceed 50 mg/dose) PO/IV AND
                • Methylprednisolone 1 mg/kg PO/IV
                • Additional doses of acetaminophen and diphenhydramine may be administered q4hr after the initial pretreatment dose
                • Repeat with the same dose of methylprednisolone or an equivalent corticosteroid for any sign of an infusion reaction (eg, fever, chills, hypotension, or dyspnea) during the infusion or within 4 hr afterwards

                Adults

                • Premediate 1 hr before with acetaminophen and diphenhydramine, then 30 min before with methylprednisolone
                • Acetaminophen 650 mg PO AND
                • Diphenhydramine 50 mg PO/IV AND
                • Methylprednisolone 1 mg/kg IV or an equivalent dose of an alternative corticosteroid
                • Additional doses of acetaminophen and diphenhydramine may be administered q4hr after the initial pretreatment dose
                • Repeat with the same dose of methylprednisolone or an equivalent corticosteroid for any sign of an infusion reaction (eg, fever, chills, hypotension, or dyspnea) during the infusion or within 4 hr afterwards

                IV Administration

                • Must use an in-line 0.2 micron polyethersulfone (PES) filter for infusion
                • Protect IV bag from light using a light-blocking cover during infusion; the infusion line does not need to be protected from light
                • Infuse diluted solution IV over 2 hr
                • Do not mix or infuse gemtuzumab with other medicinal products
                • Cytotoxic drug; follow applicable special handling and disposal procedures

                Storage

                Protect from light

                Do not freeze

                Unopened vials

                • Refrigerate at 2-8°C (36-46°F) store in the original carton

                Reconstituted solution

                • Refrigerate at 2-8°C (36-46°F) for up to 1 hr

                Diluted solution

                • Store at room temperature 15-25°C (59-77°F) for up to 6 hr; the 6-hr timeframe includes the 2-hr infusion time and 1 hr, if needed, to allow the refrigerated diluted solution to equilibrate to room temperature
                • Refrigerate at 2-8°C (36-46°F) for up to 12 hr, which includes up to 1 hr in the vial following reconstitution
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                Images

                BRAND FORM. UNIT PRICE PILL IMAGE
                Mylotarg intravenous
                -
                4.5 mg (1 mg/mL initial conc) vial

                Copyright © 2010 First DataBank, Inc.

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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

                Adding plans allows you to compare formulary status to other drugs in the same class.

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                • View the formulary and any restrictions for each plan.
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                • Compare formulary status to other drugs in the same class.
                • Access your plan list on any device – mobile or desktop.

                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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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.