Radium-223-dichloride

XOFIGO (Radium Ra-223 dichloride)

🔴 Red Flag (Important) Information

• ONLY for castration-resistant prostate cancer with bone metastases → no visceral metastases

• Causes bone marrow suppression → FBC required before every dose

• Do NOT combine with abiraterone + prednisone/prednisolone → ↑ fracture risk and mortality

• Stabilise spinal cord compression or fractures before treatment

• Alpha-emitting radiopharmaceutical → strict handling and radiation safety required

• May impair fertility → counsel patients prior to treatment

🔹 1. Basic Information

• Generic name: Radium Ra-223 dichloride

• Brand name: XOFIGO

• Drug class: Alpha-emitting radiopharmaceutical

• Formulation: Solution for injection

• Strength: 1100 kBq/mL

• Route: Intravenous injection

• Mechanism of action:
  Radium-223 mimics calcium and selectively targets areas of increased bone turnover. It emits short-range alpha particles, causing double-strand DNA breaks in tumour cells within bone metastases while limiting damage to surrounding tissue.

🔹 2. Indications (FULL – As per Approved PI)

XOFIGO is indicated for the treatment of:

• Advanced (castration-resistant) prostate cancer

• With symptomatic bone metastases

• And no known visceral metastatic disease

🔹 3. Dosing & Administration

• Dose: 55 kBq per kg body weight

• Schedule: Once every 4 weeks

• Total duration: 6 injections

• Route: Slow intravenous injection

Administration notes:

• Administered by trained personnel in controlled settings

• IV line must be flushed with saline before and after injection

• No dose adjustment required for:

  • Age ≥ 65 years

  • Renal impairment

  • Hepatic impairment

🔹 4. Contraindications

• Hypersensitivity to radium-223 or excipients

• Patients < 18 years

• Pregnancy and breastfeeding

• Concomitant use with abiraterone + prednisone/prednisolone

🔹 5. Monitoring Requirements

Before starting and before each dose:

• Full blood count (mandatory):

  • Platelets

  • Neutrophils

  • Haemoglobin

Clinical monitoring:

• Symptoms of bone marrow suppression

• Signs of infection or bleeding

• Fracture risk and skeletal stability

🔹 6. Special Warnings & Precautions

• Bone marrow suppression:
  Treatment may need to be delayed or stopped based on FBC results

• Spinal cord compression:
  Must be treated before starting XOFIGO

• Fractures:
  Stabilise prior to initiation

• Fertility risk:
  Radiation exposure may impair spermatogenesis

• Inflammatory bowel disease:
  No safety data in Crohn’s disease or ulcerative colitis

🔹 7. Drug Interactions

• Avoid combination with chemotherapy → additive myelosuppression

• Avoid abiraterone + prednisone/prednisolone

• No formal interaction studies performed

🔹 8. Use in Special Populations

• Women: Contraindicated

• Pregnancy/Breastfeeding: Contraindicated

• Paediatrics: Not indicated

• Elderly: No dose adjustment required

• Renal impairment: No adjustment needed

• Hepatic impairment: No adjustment needed

🔹 9. Adverse Effects

Very common / Common:

• Thrombocytopenia

• Neutropenia

• Anaemia

• Diarrhoea

• Nausea and vomiting

Less common:

• Pancytopenia

• Leukopenia

• Lymphopenia

• Injection site reactions

Serious:

• Severe myelosuppression

• Infection due to neutropenia

• Bleeding due to thrombocytopenia

🔹 10. Duration of Use / When to Stop the Drug

• Standard course: 6 injections only

• Discontinue if:

  • Severe or persistent bone marrow suppression

  • Inability to meet blood count thresholds

  • Serious adverse events

• No data to support treatment beyond 6 doses

🔹 11. Practical Clinical Notes

• XOFIGO is excreted mainly via faeces → hygiene precautions required

• Handle contaminated linen and bodily fluids with care

• Radiation safety regulations must be followed at all times

https://pi-pil-repository.sahpra.org.za/wp-content/uploads/2023/10/XOFIGO-EN-PIL-11092023-.pdf