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lutetium (177Lu) oxodotreotide

V10XX04

Forms & Strengths

Solution for intravenous infusion: 370 MBq/mL (10 mCi/mL) of lutetium Lu 177 at the time of injection

Adult Dosing

7.4 GBq (200 mCi) every 8 weeks for a total of 4 doses
Premedication with antiemetics recommended 30 minutes prior to administration
Administer concomitant amino acid solution during and after infusion for renal protection

Pediatric Dosing

Safety and efficacy in pediatric patients (< 18 years) have not been established

Indications

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

Mechanism of Action

Radioconjugate composed of a somatostatin analogue (oxodotreotide) linked to the beta-emitting radioisotope lutetium-177
Binds to somatostatin receptors (principally subtype 2)
Delivers beta radiation directly to tumor cells and neighboring cells expressing somatostatin receptors, inducing DNA damage and cell death

Contraindications

Hypersensitivity to lutetium Lu 177 oxodotreotide or any of its excipients
Pregnancy

Adverse Reactions

Myelosuppression (lymphopenia, anemia, thrombocytopenia, leukopenia)
Fatigue, nausea, vomiting, decreased appetite
Nephrotoxicity (elevated creatinine)
Hepatotoxicity (elevated GGT, AST, ALT)
Electrolyte abnormalities (hypomagnesemia, hypokalemia, hypocalcemia)

Drug Interactions

Somatostatin analogues: Competition for somatostatin receptor binding; discontinue long-acting octreotide at least 4 weeks prior to each dose, and short-acting octreotide at least 24 hours prior
Glucocorticoids: May induce downregulation of somatostatin receptors, potentially decreasing efficacy

Curated Content: Needs Vetting Before Put to Clinical Use