Lutathera
Somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), including foregut, midgut, and hindgut NETs, in adults.
7.4 GBq (200 mCi) IV every 8 weeks for a total of 4 doses
Amino acid infusion: Co-administer amino acid solution (lysine/arginine) for renal protection, starting 30 minutes before and continuing for 4 hours after each infusion
Pre-medication: Antiemetic (ondansetron 0.25 mg IV) 30 minutes before amino acid solution
Infusion time: Over approximately 30 minutes
Continue long-acting somatostatin analogue (withhold octreotide LAR ≥4 weeks before each dose)
Injection: 7.4 GBq (200 mCi) per single-dose vial at calibration date
Pregnancy.
- Myelosuppression: Grade 3-4 thrombocytopenia (2%), lymphopenia (9%), anemia (3%). Monitor CBC every 8 weeks for up to 60 months post-treatment.
- Myelodysplastic Syndrome/Acute Leukemia: In 2-3% of patients. Monitor CBC long-term.
- Nephrotoxicity: Renal radiation exposure. Amino acid co-infusion is mandatory for renal protection. Monitor renal function every 8 weeks.
- Hepatotoxicity: Grade 3-4 in <1%. Monitor LFTs.
- Neuroendocrine Hormonal Crises: Can occur within 24 hours. Particularly in carcinoid with hepatic tumor burden. Pre-treatment with octreotide may help.
- Radiation Safety: Patient is radioactive. Minimize close contact for 7 days.
Nausea (59%), vomiting (47%), fatigue (28%), decreased appetite (15%), abdominal pain (14%), lymphopenia (23%), diarrhea (11%), peripheral edema (11%), dizziness (9%)
Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.
Lutathera binds to somatostatin receptors (particularly SSTR2) overexpressed on NET cells. DOTA-TATE is a somatostatin analogue (octreotide derivative) that acts as a targeting ligand, delivering the beta-emitting radionuclide lutetium-177 directly to the tumor cell surface. Upon receptor binding and internalization, Lu-177 emits beta particles (max energy 497 keV, mean tissue range 0.67 mm) causing DNA damage and cell death in the tumor and immediate microenvironment.
Lu-177 physical half-life: 6.647 days. After IV infusion, rapidly accumulates in somatostatin receptor-expressing tissues. Approximately 65% excreted in urine within 24 hours. Effective half-life in tumor tissue: 3-5 days. Renal absorbed dose: 2.8-4.7 Gy per treatment cycle (mitigated by amino acid co-infusion).
Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.
- NETTER-1 — 177Lu-DOTATATE + octreotide LAR vs. octreotide LAR alone in midgut NETs. Phase III, n=229.