Description

Simple

A medication used to treat prostate cancer in selected patients.

Clinical

A radiopharmaceutical agent used to treat patients with castration-resistant prostate cancer, symptomatic bone metastases and no known visceral metastatic disease.

Overview

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.

Pharmacology

Indication

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.

Pharmacodynamic

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

Mechanism of action

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... Read more

Absorption

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

Protein binding

There is negligible plasma protein binding.

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 t... Read more

Clearance

The clearance rate of radium-223 was not quantified.

Half life

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

Route of elimination

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... Read more

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.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Pregnancy
      • Drugbank Id: DBCOND0018394

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Darbepoetin alfa
The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Radium Ra 223 dichloride.
Erythropoietin
The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Radium Ra 223 dichloride.
Methoxy polyethylene glycol-epoetin beta
The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Radium Ra 223 dichloride.
Peginesatide
The risk or severity of Thrombosis can be increased when Peginesatide is combined with Radium Ra 223 dichloride.
3 References
  1. 1 . Suominen MI, Rissanen JP, Kakonen R, Fagerlund KM, Alhoniemi E, Mumberg D, Ziegelbauer K, Halleen JM, Kakonen SM, Scholz A: Survival benefit with radium-223 dichloride in a mouse model of breast cancer bone metastasis. J Natl Cancer Inst. 2013 Jun 19;105(12):908-16. doi: 10.1093/jnci/djt116. Epub 2013 May 16.PubMed: 23682134
  2. 2 . Nilsson S, Franzen L, Parker C, Tyrrell C, Blom R, Tennvall J, Lennernas B, Petersson U, Johannessen DC, Sokal M, Pigott K, Yachnin J, Garkavij M, Strang P, Harmenberg J, Bolstad B, Bruland OS: Bone-targeted radium-223 in symptomatic, hormone-refractory prostate cancer: a randomised, multicentre, placebo-controlled phase II study. Lancet Oncol. 2007 Jul;8(7):587-94.PubMed: 17544845
  3. 3 . Bruland OS, Nilsson S, Fisher DR, Larsen RH: High-linear energy transfer irradiation targeted to skeletal metastases by the alpha-emitter 223Ra: adjuvant or alternative to conventional modalities? Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6250s-6257s.PubMed: 17062709