Chemical formula: Ra Molecular mass: 293.924 g/mol
Radium-223 dichloride is not indicated in women. Radium-223 dichloride is not to be used in women who are, or may be, pregnant.
Radium-223 dichloride is not indicated in women. Radium-223 dichloride is not to be used in women who are breast-feeding.
Animal reproduction studies have not been conducted with radium-223 dichloride.
Because of potential effects on spermatogenesis associated with radiation, men should be advised to use effective contraceptive methods during and up to 6 months after treatment with radium-223 dichloride.
There are no human data on the effect of radium-223 dichloride on fertility.
Based on studies in animals, there is a potential risk that radiation from radium-223 dichloride could cause adverse effects on fertility. Male patients should seek advice on conservation of sperm prior to treatment.
Radium-223 dichloride has no or negligible influence on the ability to drive and use machines.
The overall safety profile of radium-223 dichloride is based on data from 600 patients treated with radium-223 dichloride in the phase III study.
The most frequently observed adverse reactions (≥10%) in patients receiving radium-223 dichloride were diarrhoea, nausea, vomiting, thrombocytopenia and bone fracture.
The most serious adverse reactions were thrombocytopenia and neutropenia.
The adverse reactions observed with radium-223 dichloride are represented in below. They are classified according to System Organ Class. The most appropriate MedDRA term is used to describe a certain reaction and its synonyms and related conditions. Adverse reactions from clinical trials are classified according to their frequencies. Frequencies are defined as: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100).
Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.
Adverse reactions reported in clinical trials in patients treated with radium-223 dichloride:
Very common: Thrombocytopenia
Common: Neutropenia, Pancytopenia, Leukopenia
Uncommon: Lymphopenia
Very common: Diarrhoea, Vomiting, Nausea
Very common: Bone fracture
Uncommon: Osteoporosis
Common: Injection site reactions
Radium-223 dichloride increases the risk of bone fractures. In clinical studies, concurrent use of bisphosphonates or denosumab reduced the incidence of fractures in patients treated with radium-223 monotherapy. Fractures have occurred for up to 24 months after the first dose of radium-223.
Thrombocytopenia (all grades) occurred in 11.5% of patients treated with radium-223 dichloride and 5.6% of patients receiving placebo. Grade 3 and 4 thrombocytopenia was observed in 6.3% of patients treated with radium-223 dichloride and in 2% of patients receiving placebo. Overall, the frequency of grade 3 and 4 thrombocytopenia was lower in patients that did not previously receive docetaxel (2.8% in patients treated with radium-223 dichloride versus 0.8% in patients receiving placebo) compared to patients that previously received docetaxel (8.9% in patients treated with radium-223 dichloride versus 2.9% in patients receiving placebo). In EOD4 (“superscan”) patients, thrombocytopenia (all grades) was reported in 19.6% of patients treated with radium-223 dichloride and in 6.7% of patients receiving placebo. Grade 3 and 4 thrombocytopenia was observed in 5.9% of patients treated with radium-223 dichloride and in 6.7% of patients receiving placebo.
Neutropenia (all grades) was reported in 5% of patients treated with radium-223 dichloride and in 1% of patients receiving placebo. Grade 3 and 4 neutropenia was observed in 2.2% of patients treated with radium-223 dichloride and in 0.7% of patients receiving placebo. Overall, the frequency of grade 3 and 4 neutropenia was lower in patients that did not previously receive docetaxel (0.8% in patients treated with radium-223 dichloride versus 0.8% in patients receiving placebo) compared to patients that previously received docetaxel (3.2% in patients treated with radium-223 dichloride versus 0.6% in patients receiving placebo).
In a phase I study, neutrophil and platelet count nadirs occurred at 2 to 3 weeks after intravenous administration of a single dose of radium-223 dichloride.
Grade 1 and 2 injection site reactions, such as erythema, pain and swelling, were reported in 1.2% of patients treated with radium-223 dichloride and in 0% of patients receiving placebo.
Radium-223 dichloride contributes to a patient’s overall long-term cumulative radiation exposure. Long-term cumulative radiation exposure may be associated with an increased risk of cancer and hereditary defects. In particular, the risk for osteosarcoma, myelodysplastic syndrome and leukaemias may be increased. No cases of radium-223 dichloride-induced cancer have been reported in clinical trials in follow-up of up to three years.
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