Radium-223 Dichloride

Radium-223 Dichloride Uses, Dosage, Side Effects, Food Interaction and all others data.

Radium Ra 223 Dichloride is a radiopharmaceutical containing the radioisotope radium-223 that emits short range but high linear energy alpha particles. As a cation, radium mimics calicum and binds to hydroxyapatite, which is a bone mineral found in areas of high bone turnover as seen in bone metastases. It was first approved by the FDA in May 2013 and is currently marketed under the brand name Xofigo, which was formerly called Alpharadin. Xofigo is indicated in patients who have metastatic bone cancer that is symptomatic with no visceral metastases and patients who have prostate cancer that is castration resistant. The FDA label includes a warning that Radium Ra 223 Dichloride should not be used in women who are pregnant or may become pregnant due to the high risk of fetal harm.

Physiologically, Radium Ra 223 Dichloride, prevents the spread of bone cancer by killing the associated bone cancer cells.

Radium-223 Dichloride
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Radium-223 Dichloride
Generic	Radium Ra 223 dichloride
Radium Ra 223 dichloride Other Names	Radium chloride Ra-223, Radium Ra 223 dichloride, Radium Ra-223 dichloride, Radium-223 chloride, Radium-223 dichloride
Type
Formula	Cl₂Ra
Weight	Average: 293.924 Monoisotopic: 292.956202554
Protein binding	There is negligible plasma protein binding.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Radium-223 Dichloride is a radiopharmaceutical agent used to treat patients with castration-resistant prostate cancer, symptomatic bone metastases and no known visceral metastatic disease.

Used in patients who have metastatic bone cancer that is symptomatic with no visceral metastases and patients who have prostate cancer that is castration resistant.

Radium-223 Dichloride is also used to associated treatment for these conditions: Castration resistant, metastatic Prostate cancer

How Radium-223 Dichloride works

Radium Ra 223 Dichloride is the radioisotope radium-223 that emits short range but high linear energy alpha particles. As a cation, radium mimics calicum and binds to hydroxyapatite, which is a bone mineral found in areas of high bone turnover as seen in bone metastases. The high energy damages bone cells by introducing double-stranded DNA breaks. This leads to cell death and prevention of the spread of the bone cancer cells. As well because of the alpha particle's short range of less than 10 cell diameters, its damaging effects would less likely affect the non-cancerous cells nearby.

Toxicity

Because of its cytotoxic actions that have a high potential to cause fetal harm, Radium Ra 223 Dichloride is contraindicated in women who are pregnant or are of child bearing age. Other side effects include several hematological lab abnormalities, peripheral edema, nausea, vomiting, and diarrhea.

Food Interaction

Drink plenty of fluids.

Volume of Distribution

The volume of distribution was not quantified, but after 24 hours, there is only 1% radium-223 remaining in the blood. The rest of the radium-223 is distributed to bone (61% of the radioactive dose after 4 hours) and intestine (49% of the radioactive dose after 4 hours). No other organs were found to have significant uptake.

Elimination Route

Since Radium Ra 223 Dichloride is administered I.V., the bioavailability should be 100%.

Half Life

The half-life is relatively long at 11.4 days for radium-223.

Clearance

The clearance rate of radium-223 was not quantified.

Elimination Route

Radium-223 is mainly eliminated through the feces (13%) and to a lesser extent in the urine (2%). It is also noted that the elimination rate of radium-223 from the intestines is variable due to the high variability of intestinal transit rates among patients. Therefore there could be more intestinal radiation exposure in patients with slower intestinal transit rates, but the significance of this in relation to toxicity is not known.