Dosing & Uses
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
-
Hypersensitivity prophylaxis
- Previous Grade 1 or 2 reaction: Premedicate
- Previous Grade 3 or 4 reaction: Do not rechallenge patients; permanently discontinue
Dosage Modifications
Renal impairment
- Mild-to-moderate (CrCl 30-89 mL/min): No dose adjustment required; however, patients with baseline mild or moderate renal impairment may be at greater risk of toxicity, including renal toxicity, due to increased radiation exposure; perform more frequent assessments of renal function in patients with baseline mild to moderate impairment
- 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, first occurrence
- 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, first occurrence
- 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
- Recurrent renal toxicity: Permanently discontinue
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
- Recurrent hepatotoxicity: Permanently discontinue
Hypersensitivity reactions
- First occurrence of Grade 3 or 4: Permanently discontinue
Other adverse effects
-
Grade 3 or 4, first occurrence
- 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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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)
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%)
Warnings
Contraindications
None
Cautions
Drug contributes to a patient’s overall long-term cumulative 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; withhold dose, reduce dose, or permanently discontinue therapy based on severity of myelosuppression
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; monitor serum creatinine and calculated creatinine clearance; withhold dose, reduce dose, or permanently discontinue therapy based on severity of renal toxicity; patients with baseline renal impairment may be at increased risk of toxicity due to increased radiation exposure (see Adult Dosing and Dosage Modifications)
Rare reports of hepatotoxicity; monitor transaminases, bilirubin, serum albumin, and international normalized ratio (INR) during treatment; withhold dose, reduce dose, or permanently discontinue therapy based on severity of hepatotoxicity (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
Hepatic tumor hemorrhage, edema, or necrosis, reported with rare reports of intrahepatic congestion and cholestasis; patients with hepatic metastasis may be at increased risk of hepatotoxicity due to radiation exposure; monitor transaminases, bilirubin and serum albumin during treatment; withhold, reduce dose, or permanently discontinue therapy based on severity of hepatotoxicity
Can cause fetal harm and infertility in males and females based on mechanism of action (see Pregnancy)
Hypersensitivity reactions
- Hypersensitivity reactions, including angioedema, reported; monitor patients closely for signs and symptoms of hypersensitivity reactions, including anaphylaxis, during and following therapy administration for a minimum of 2 hr in a setting where cardiopulmonary resuscitation medication and equipment are available
- Discontinue infusion upon first observation of any signs or symptoms consistent with a severe hypersensitivity reaction, and initiate appropriate therapy
- Premedicate patients with history of Grade 1 or 2 hypersensitivity reactions to therapy before subsequent doses; permanently discontinue therapy in patients who experience Grade 3 or 4 hypersensitivity reactions
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)
Pregnancy & Lactation
Pregnancy
Based on its mechanism of action, can cause fetal harm and infertility
No data are available regarding use in pregnant women; however, all oncology#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.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
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 oncology#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 oncology#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
Monitor closely for signs and symptoms of hypersensitivity reactions during and following administration for at least 2 hr in a setting where CPR medication and equipment are available
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
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 |  |
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