radium-223 dichloride (Rx)

Brand and Other Names:Xofigo
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

IV solution

  • 1100 kBq/mL (30 microcurie/mL)
  • Available as 6mL/single-use vial
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Prostate Cancer

Indicated for treatment of men with castration-resistant prostate cancer with symptomatic bone metastases and no known visceral metastatic disease

55 kBq (1.49 microcurie) per kg IV infused over 1 minute; repeat q4weeks for 6 cycles total

Dosage calculation must be based on decay correction factor of radium-223

Dose calculation

  • Volume to be administered should be calculated using the:
  • -Patient’s body weight (kg)
  • -Dosage level 55 kBq/kg body weight or 1.49 microcurie/kg body weight
  • -Radioactivity concentration of the product (1,100 kBq/mL; 30 microcurie/mL) at the reference date
  • -Decay correction factor to correct for physical decay of radium-223
  • Example: (Body wt in kg x 55 kBq/kg body weight) ÷ (Decay factor x 1,100 kBq/mL) or (Body wt in kg x 1.49 microcurie body weight) ÷ (Decay factor x 30 microcurie/mL)
  • Decay correction factor table listed in prescribing information and is based on the vial’s reference date

Dosing Considerations

Safety beyond 6 treatment cycles not established

Safety and efficacy not established

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Adverse Effects

>10%

Percentages includes all toxicity grades (1-4)

Anemia (93%)

Lymphocytopenia (72%)

Leukopenia (35%)

Thrombocytopenia (31%)

Nausea (36%)

Diarrhea (25%)

Vomiting (19%)

Neutropenia (18%)

Peripheral edema (13%)

1-10%

Percentages includes all toxicity grades (1-4)

Renal failure and impairment (3%)

Dehydration (3%)

Pancytopenia (2%)

Erythema, pain, and edema at injection site (1%)

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Warnings

Contraindications

Pregnancy; radium-223 can cause fetal harm when administered to a pregnant woman based on its mechanism of action; not indicated for use in women and is contraindicated in women who are or may become pregnant

Cautions

May cause myelosuppression and bone marrow failure; perform hematologic evaluation at baseline and prior to every dose; discontinue if life-threatening complications occur despite supportive care for bone marrow failure

Safety and efficacy of concomitant chemotherapy have not been established; outside of a clinical trial, concomitant use with chemotherapy is not recommended due to the potential for additive myelosuppression

Because of potential effects on spermatogenesis associated with radiation, advise men who are sexually active to use condoms and their female partners of reproductive potential to use a highly effective contraceptive method during and for 6 months after completing treatment

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Pregnancy & Lactation

Pregnancy Category: X

Lactation: Not indicated for women; unknown if distributed in human breast milk

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.

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Pharmacology

Mechanism of Action

Alpha particle-emitting radiopharmaceutical; contains the heavy metal radium, which mimics calcium and forms complexes with the bone mineral hydroxyapatite at areas of increased bone turnover, such as bone metastases; this causes double-strand DNA breaks that are lethal to the prostate cancer cell at the site of increased bone turnover induced by the cancer

Absorption

Peak blood levels were linear in terms of dose proportionality and time independence in the dose range investigated

Distribution

After IV injection, rapidly cleared from the blood and distributed primarily into bone or is excreted into intestine

No significant uptake was seen in other organs such as heart, liver, kidneys, urinary bladder, and spleen at 4 hours post-injection

Detected in blood post-injection

  • 15 minutes: ~20% remains in blood
  • 4 hr: ~4% remains in blood
  • 24 hr: <1% remains in blood

Detected in bone/intestine post-injection

  • 10 minutes: Radioactivity was observed in bone and in intestine
  • 4 hr: Percentage of the radioactive dose present in bone and intestine was approximately 61% and 49%, respectively

Metabolism

Isotope that decays and is not metabolized

Elimination

~63% excreted from body within 7 days after injection (after correcting for decay)

Fecal excretion is the major elimination route; at 48 hr after injection, the cumulative fecal excretion was 13% (range 0 -34%), and the cumulative urine excretion was 2% (range 1 -5%)

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Administration

IV Administration

Follow procedures for proper handling and disposal of radioactive pharmaceuticals

Inspect visually for particulate matter and discoloration before administering

Ready-to-use IV solution; do not dilute or mix with any solutions

Slow IV injection over 1 minute

Flush IV line/cannula with 0.9% NaCl before and after injection

Storage

Store at room temperature, below 40°C (104°F)

Store in original container or equivalent radiation shielding

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Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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