Adult: In patients with unresectable or metastatic, progressive, well-differentiated (G1 and G2), somatostatin receptor-positive cases, including foregut, midgut, and hindgut tumours: 7.4 GBq (200 mCi) via slow infusion over approx 30 minutes every 8 weeks for 4 doses. Dosage interval may be increased up to 16 weeks if severe toxicity occurs. For symptom control, concomitant use with somatostatin analogues is required; discontinue short- or long-acting somatostatin analogues at least 24 hours or 4 weeks, respectively, before each infusion. For renal protection, administer IV amino acid solution 30 minutes before infusion then continue during and for at least 3 hours after the infusion. Premedicate with antiemetics 30 minutes before IV amino acid infusion. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety and tolerability (refer to detailed product guideline).
Pregnancy and lactation.
Patient with previous chemotherapy or oncologic radiometabolic therapies with 131I-compounds or other therapy using unshielded radioactive sources; urinary incontinence, brain metastasis, bone metastasis, history of other malignant tumours (unless considered to be in remission for at least 5 years). Initiation of therapy is not recommended in patients with severe impairment of haematological function at baseline (e.g. Hb <4.9 mmol/L or 8 g/dL, platelet count <75 g/L or 75 x 103/mm3, leucocytes <2 g/L or 2,000/mm3) [except lymphopenia]. Renal (CrCl ≥30 mL/min) and hepatic impairment.
Significant: Myelosuppression (e.g. anaemia, neutropenia, thrombocytopenia), myelodysplastic syndrome, acute leukaemia, renal failure, neuroendocrine hormonal crisis, infertility, tumour lysis syndrome, vomiting, nausea. Very rarely, hepatic tumour haemorrhage, oedema, or necrosis; intrahepatic congestion, cholestasis. Endocrine disorders: Secondary hypothyroidism. Gastrointestinal disorders: Abdominal distention or pain, diarrhoea, constipation, upper abdominal pain, dyspepsia, gastritis, dysgeusia. General disorders and administration site conditions: Fatigue, inj site reactions, peripheral oedema, chills, flu-like illness, lethargy. Hepatobiliary disorders: Hyperbilirubinaemia. Investigations: Increased AST, ALT, alkaline phosphatase, gamma-glutamyltransferase, blood creatine; ECG QT prolonged. Metabolism and nutrition disorders: Decreased appetite, hyperglycaemia, dehydration, hypomagnesaemia, hyponatraemia, hypokalaemia, hyperuricaemia. Musculoskeletal and connective tissue disorders: Musculoskeletal pain, muscle spasms. Nervous system disorders: Dizziness, headache. Psychiatric disorders: Sleep disorders, anxiety. Renal and urinary disorders: Acute kidney injury, haematuria, proteinuria. Respiratory, thoracic and mediastinal disorders: Dyspnoea. Skin and subcutaneous tissue disorders: Alopecia. Surgical and medical procedures: Transfusion. Vascular disorders: Hypertension, flushing or hot flush, hypotension, syncope.
Verify pregnancy status before initiation of treatment in women of reproductive potential. Confirm the overexpression of somatostatin receptors in the tumour tissue with imaging (scintigraphy or positron emission tomography [PET]) before initiating treatment. Monitor CBC count, kidney function (CrCl, serum creatinine), LFTs at least once within 2-4 weeks prior to therapy and shortly before each administration, then every 4 weeks for at least 3 months after the last administration and every 6 months thereafter. Monitor for signs or symptoms of secondary malignancies and neuroendocrine hormonal crisis (e.g. hypotension, flushing, bronchospasm).
Somastostatin and its analogues (e.g. octreotide) may interfere with the efficacy of lutetium (177Lu) oxodotreotide. Corticosteroids may induce down-regulation of subtype 2 somatostatin receptors (SST2) which may lead to reduction of therapeutic effect of lutetium (177Lu) oxodotreotide.
Description: Lutetium (177Lu) oxodotreotide is a β- and γ-emitting radionuclide that has high affinity for subtype 2 somatostatin receptors (SST2). After its binding to malignant cells which overexpress SST2 receptors, the resultant complex is internalised by the cell. The β emission from lutetium (177Lu) oxodotreotide induces cellular damage by forming free radicals in the target and neighbouring cells.
Synonym: lutetium Lu-177 dotatate. Pharmacokinetics: Distribution: Distributed in the kidneys, tumour lesions, liver, spleen, and sometimes, the pituitary gland and thyroid within 4 hours following infusion. Volume of distribution: 460 L. Plasma protein binding: 43% (non-radioactive form). Metabolism: Poorly metabolised. Excretion: Via urine (as intact compound; approx 60% within 24 hours and approx 65% within 48 hours after infusion). Elimination half-life: 71 ± 28 hours (terminal).
Store below 25°C. Do not freeze. Stable for 72 hours. This is a radiopharmaceutical agent, follow applicable procedures for storing, receiving, handling, administration, and disposal in accordance with national guideline.
V10XX04 - lutetium (177Lu) oxodotreotide ; Belongs to the class of various therapeutic radiopharmaceuticals.
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