lutetium Lu 177-dota-tate (Rx)

Brand and Other Names:Lutathera
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injection, solution for IV use

  • 370 MBq/mL (10 mCi/mL) single-dose vial
  • Solution volume in each vial adjusted from 20.5-25 mL to provide a total of 7.4 GBq (200 mCi) of radioactivity per vial

Neuroendocrine Tumors

Indicated for somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), including foregut, midgut, and hindgut neuroendocrine tumors in adults

7.4 GBq (200 mCi) IV q8weeks for a total of 4 doses administered with premedication and concomitant medications

Premedication and concomitant medications

  • Somatostatin analogs
    • Before initiating lutetium Lu 177-dota-tate: Discontinue long-acting somatostatin analogs (eg, long-acting octreotide) for at least 4 weeks beforehand; administer short-acting octreotide as needed; discontinue at least 24 hr before initiating lutetium Lu 177-dota-tate
    • During treatment: Administer long-acting octreotide 30 mg IM between 4-24 hr after each lutetium Lu 177-dota-tate dose; do not administer long-acting octreotide within 4 weeks of each subsequent lutetium Lu 177-dota-tate dose; short-acting octreotide may be given for symptomatic management, but must be withheld for at least 24 hr before each lutetium Lu 177-dota-tate dose
    • Following lutetium Lu 177-dota-tate treatment: Continue long-acting octreotide 30 mg IM q4weeks after completing lutetium Lu 177-dota-tate until disease progression or for up to 18 months following treatment initiation
  • Antiemetic
    • Administer antiemetics 30 min before recommended amino acid solution
  • Amino acid solution
    • Initiate IV amino acid solution 30 min before administering lutetium Lu 177-dota-tate
    • IV amino acid solution contains: L-lysine (18-24 g) and L-arginine (18-24 g) per 1.5-2.2 L; osmolarity <1060 mOsmol
    • Use a 3-way valve to administer amino acids using the same venous access as lutetium Lu 177-dota-tate or administer amino acids through a separate venous access in the patient’s other arm
    • Continue the infusion during, and for at least 3 hr after, lutetium Lu 177-dota-tate infusion
    • Do not decrease amino acid solution dose if the dose of lutetium Lu 177-dota-tate is reduced

Dosage Modifications

Renal impairment

  • Mild-to-moderate (CrCl 30-70 mL/min): No dose adjustment required; however, patients may be at greater risk of toxicity; perform more frequent assessments of renal function
  • Severe (CrCl <30 mL/min) or end-stage renal disease: Not studied

Hepatic impairment

  • Mild-to-moderate: No dose adjustment required
  • Severe (TB >3x ULN and any AST): Not studied

Thrombocytopenia

  • Grade 2, 3, or 4
    • Withhold dose until complete or partial resolution (grade 0 to 1), then resume dose at 3.7 GBq (100 mCi) with complete or partial resolution
    • If reduced dose does not result in grade 2, 3, or 4 thrombocytopenia, administer at 7.4 GBq (200 mCi) for next dose
    • Permanently discontinue for grade ≥2 thrombocytopenia requiring a treatment delay ≥16 weeks
  • Grade 2, 3, or 4 recurrence
    • Permanently discontinue

Anemia and neutropenia

  • Grade 3 or 4
    • Withhold dose until complete or partial resolution (grade 0, 1, or 2), then resume dose at 3.7 GBq (100 mCi) with complete or partial resolution
    • If reduced dose does not result in grade 3 or 4 anemia or neutropenia, administer at 7.4 GBq (200 mCi) for next dose
    • Permanently discontinue for ≥grade 3 thrombocytopenia requiring a treatment delay ≥16 weeks
  • Grade 3 or 4 recurrence
    • Permanently discontinue

Renal toxicity

  • Renal toxicity definition
    • CrCl <40 mL/min OR
    • CrCl decreased 40% from baseline OR
    • Baseline serum creatinine increased 40%
  • Actions
    • Withhold dose until complete resolution
    • Resume dose at 3.7 GBq (100 mCi) in patients with complete resolution
    • If reduced dose does not result in renal toxicity, administer at 7.4 GBq (200 mCi) for next dose
    • Permanently discontinue for renal toxicity requiring a treatment delay ≥16weeks

Hepatotoxicity

  • Hepatotoxicity definition
    • Bilirubinemia >3x ULN (Grade 3 or 4) OR
    • Hypoalbuminemia <30 g/L with a decreased prothrombin ratio <70%
  • Actions
    • Withhold dose until complete resolution
    • Resume dose at 3.7 GBq (100 mCi) in patients with complete resolution
    • If reduced dose does not result in hepatotoxicity, administer at 7.4 GBq (200 mCi) for next dose
    • Permanently discontinue for hepatotoxicity requiring a treatment delay ≥16weeks

Other nonhematologic toxicity

  • Grade 3 or 4
    • Withhold dose until complete or partial resolution (grade 0-2), then resume dose at 3.7 GBq (100 mCi) with complete or partial resolution
    • If reduced dose does not result in grade 3 or 4 toxicity, administer at 7.4 GBq (200 mCi) for next dose
    • Permanently discontinue for grade ≥3 toxicity requiring a treatment delay ≥16 weeks
  • Grade 3 or 4 recurrence
    • Permanently discontinue

Dosing Considerations

Verify pregnancy status of females of reproductive potential prior to initiating

Safety and efficacy not established

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Interactions

Interaction Checker

and lutetium Lu 177-dota-tate

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (4)

                • lanreotide

                  lanreotide decreases effects of lutetium Lu 177-dota-tate by receptor binding competition. Modify Therapy/Monitor Closely. Somatostatin analogs competitively bind to the same somatostatin receptors as lutetium Lu 177-dota-tate and may affect its efficacy. Discontinue long-acting somatostatin analogs at least 4 weeks and short-acting octreotide at least 24 hr prior to each lutetium Lu 177-dota-tate dose. Administer short- and long-acting octreotide during treatment as recommended.

                • octreotide

                  octreotide decreases effects of lutetium Lu 177-dota-tate by receptor binding competition. Modify Therapy/Monitor Closely. Somatostatin analogs competitively bind to the same somatostatin receptors as lutetium Lu 177-dota-tate and may affect its efficacy. Discontinue long-acting somatostatin analogs at least 4 weeks and short-acting octreotide at least 24 hr prior to each lutetium Lu 177-dota-tate dose. Administer short- and long-acting octreotide during treatment as recommended.

                • pasireotide

                  pasireotide decreases effects of lutetium Lu 177-dota-tate by receptor binding competition. Modify Therapy/Monitor Closely. Somatostatin analogs competitively bind to the same somatostatin receptors as lutetium Lu 177-dota-tate and may affect its efficacy. Discontinue long-acting somatostatin analogs at least 4 weeks and short-acting octreotide at least 24 hr prior to each lutetium Lu 177-dota-tate dose. Administer short- and long-acting octreotide during treatment as recommended.

                • siponimod

                  siponimod and lutetium Lu 177-dota-tate 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.

                Minor (0)

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                  Adverse Effects

                  >10% All Grades

                  Lymphopenia (90%)

                  Creatinine increased (85%)

                  Hyperglycemia (82%)

                  Anemia (81%)

                  Increased GGT (66%)

                  Increased alkaline phosphatase (65%)

                  Nausea (65%)

                  Leukopenia (55%)

                  Vomiting (53%)

                  Thrombocytopenia (53%)

                  AST increased (50%)

                  ALT increased (43%)

                  Fatigue (38%)

                  Hyperuricemia (34%)

                  Hypocalcemia (32%)

                  Blood bilirubin increased (30%)

                  Hypokalemia (26%)

                  Abdominal pain (26%)

                  Diarrhea (26%)

                  Neutropenia (26%)

                  Decreased appetite (21%)

                  Hyperkalemia (19%)

                  Hypernatremia (17%)

                  Headache (17%)

                  Dizziness (17%)

                  Peripheral edema (16%)

                  Hypoglycemia (15%)

                  Flushing (14%)

                  Back pain (13%)

                  Anxiety (12%)

                  Renal failure (12%)

                  Alopecia (12%)

                  Hypertension (12%)

                  Pain in extremity (11%)

                  Cough (11%)

                  >10% Grades 3-4

                  Lymphopenia (44%)

                  Increased GGT (20%)

                  1-10% All Grades

                  Constipation (10%)

                  Pyrexia (8%)

                  Dysgeusia (8%)

                  Radiation-related toxicity to urinary tract (8%)

                  Atrial fibrillation (5%)

                  Myalgia (5%)

                  Neck pain (5%)

                  1-10% Grades 3-4

                  Vomiting (7%)

                  Hyperuricemia (6%)

                  Nausea (5%)

                  Alkaline phosphatase increased (5%)

                  AST increased (5%)

                  ALT increased (4%)

                  Hyperglycemia (4%)

                  Hypokalemia (4%)

                  Renal failure (3%)

                  Abdominal pain (3%)

                  Diarrhea (3%)

                  Neutropenia (3%)

                  Back pain (2%)

                  Hypertension (2%)

                  Leukopenia (2%)

                  Blood bilirubin increased (2%)

                  Anxiety (1%)

                  Atrial fibrillation (1%)

                  Fatigue (1%)

                  Cough (1%)

                  Thrombocytopenia (1%)

                  Creatinine increased (1%)

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                  Warnings

                  Contraindications

                  None

                  Cautions

                  Drug contributes to overall long-term radiation exposure; long-term cumulative radiation exposure is associated with an increased risk for cancer; radiation can be detected in the urine for up to 30 days; minimize radiation exposure to patients, medical personnel, and household contacts during and after treatment with institutional good radiation safety practices and patient management procedures

                  Myelosuppression may occur; monitor blood cell counts (see Dosage Modifications)

                  Secondary myelodysplastic syndrome and leukemia reported

                  Renal failure development may occur up to 36 mo after treatment; administer the recommended amino acid solution before, during, and after lutetium Lu 177-dota-tate to decrease reabsorption through the proximal tubules and decrease the radiation dose to the kidneys; patients with baseline renal impairment may be at greater risk (see Adult Dosing and Dosage Modifications)

                  Rare reports of hepatotoxicity; monitor transaminases, bilirubin, and serum albumin (see Dosage Modifications)

                  Neuroendocrine hormonal crises, manifesting with flushing, diarrhea, bronchospasm, and hypotension, reported; typically occurs during or within 24 hr after initial dose; monitor patients for flushing, diarrhea, hypotension, bronchoconstriction, or other signs and symptoms of tumor-related hormonal release; administer IV somatostatin analogs, fluids, corticosteroids, and electrolytes as indicated

                  Corticosteroids can induce down-regulation of subtype 2 somatostatin receptors (SST2). Avoid repeated administration of high-doses of glucocorticosteroids during treatment

                  Can cause fetal harm and infertility in males and females based on mechanism of action (see Pregnancy)

                  Drug interaction overview

                  • Somatostatin and its analogs competitively bind to somatostatin receptors and may interfere with lutetium Lu 177-dota-tate efficacy (see Adult Dosing)
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                  Pregnancy

                  Pregnancy

                  Based on its mechanism of action, can cause fetal harm and infertility

                  No data are available regarding use in pregnant women; however, all radiopharmaceuticals have the potential to cause fetal harm

                  Advise pregnant women of the risk to a fetus

                  Verify pregnancy status of females of reproductive potential prior to initiating

                  Infertility

                  • May cause infertility in males and females
                  • The recommended cumulative dose of 29.6 GBq results in a radiation absorbed dose to the testis and ovaries within the range in which temporary or permanent infertility can be expected following external beam radiotherapy

                  Contraception

                  • Females: Advise females of reproductive potential to use effective contraception during treatment and for 7 months after the final dose
                  • Males: Advise males with female partners of reproductive potential to use effective contraception during and for 4 months after the final dose

                  Lactation

                  There are no data on the presence of lutetium Lu 177 dotatate in human milk, or its effects on the breastfed infant or milk production

                  No lactation studies in animals were conducted

                  Because of the potential risk for serious adverse reactions in breastfed infants, advise women not to breastfeed during treatment and for 2.5 months 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

                  Radiolabeled somatostatin analog; binds to somatostatin receptors with highest affinity for subtype 2 receptors (SSRT2)

                  Upon binding to somatostatin receptor-expressing cells, including malignant somatostatin receptor-positive tumors, the compound is internalized

                  Beta emission from Lu 177 induces cellular damage by forming free radicals in somatostatin receptor-positive cells and in neighboring cells

                  Absorption

                  Peak plasma concentration: 10 ng/mL (mean) at end of IV infusion

                  AUC: 41 n·gh/mL (mean)

                  Distribution

                  Protein bound: 43%

                  Vd: 640 L; within 4 hr drug is distributed in kidneys, tumor lesions, liver, spleen, and in some patients, pituitary and thyroid glands

                  Coadministration of amino acids reduces median radiation dose to the kidneys by 47% (34-59%) and increases mean beta-phase blood clearance by 36%

                  Metabolism

                  Does not undergo hepatic metabolism

                  Elimination

                  Half-life, blood elimination: 3.5 hr

                  Half-life, terminal: 71 hr

                  Clearance: 4.5 L/hr

                  Excretion

                  • Primarily eliminated renally
                  • 44% within 5 hr after dose
                  • 58% within 24 hr after dose
                  • 65% within 48 hr after dose
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                  Administration

                  IV Preparation

                  Use aseptic technique and radiation shielding when administering solution

                  Use tongs when handling vial to minimize radiation exposure

                  Do not inject directly into any other IV solution

                  Confirm the amount of radioactivity in the radiopharmaceutical vial with an appropriate dose calibrator prior to and after administration

                  Inspect the product visually for particulate matter and discoloration under a shielded screen prior to administration; solution should appear clear and colorless to slightly yellow; discard vial if particulates or discoloration are present

                  Handling radiopharmaceuticals

                  • Radiopharmaceutical; handle with appropriate safety measures to minimize radiation exposure
                  • Use waterproof gloves and effective radiation shielding when handling
                  • Radiopharmaceuticals should be used by or under the control of physicians who are qualified by specific training and experience in the safe use and handling, and whose experience and training have been approved by the appropriate governmental agency authorized to license the use of radiopharmaceuticals
                  • Dispose of any unused medicinal product or waste material in accordance with local and federal laws

                  IV Administration

                  May infuse by either gravity method or infusion pump method; see precise instructions in prescribing information for each method in conjunction with 0.9% NaCl

                  Storage

                  Store in the original package (ie, lead-shielded container placed in a plastic sealed container)

                  Store at temperature below 25°C (77°F)

                  Shelf life is 72 hr; discard appropriately at 72 hr

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                  Images

                  BRAND FORM. UNIT PRICE PILL IMAGE
                  Lutathera intravenous
                  -
                  10 mCi/mL (370 mBq/mL) vial
                  Lutathera intravenous
                  -
                  10 mCi/mL (370 mBq/mL) 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

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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
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                  Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the 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.