Radium Ra 223 Dichloride

Các tên gọi khác (3) :

Radium-223 chloride
Radium-223 dichloride
Xofigo

diagnostic agents

Thuốc Gốc

Small Molecule

CAS: 444811-40-9

CTHH: Cl₂Ra

PTK: 293.924

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.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

Cl₂Ra

Phân tử khối

293.924

Monoisotopic mass

292.956202554

InChI

InChI=1S/2ClH.Ra/h2*1H;/q;;+2/p-2/i;;1-3

InChI Key

InChIKey=RWRDJVNMSZYMDV-SIUYXFDKSA-L

IUPAC Name

dichloro(²²³Ra)radium

Traditional IUPAC Name

dichloro(²²³Ra)radium

SMILES

Cl[223Ra]Cl

Độ hòa tan

7.47e+01 g/l

logP

1.27

logS

-0.6

Refractivity

12.27 m³·mol^-1

Polarizability

7.26 Å³

Polar Surface Area (PSA)

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

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

Cơ Chế Tác Dụng : 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. 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.

Dược Động Học :

▧ Absorption :
Since Radium Ra 223 Dichloride is administered I.V., the bioavailability should be 100%.
▧ 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.
▧ Protein binding :
There is negligible plasma protein binding.
▧ Metabolism :
Radium-223 does not undergo metabolism because it is a radioisotope that decays.
▧ 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 radiation exposure in patients with slower intestinal transit rates, but the significance of this in relation to toxicity is not known.
▧ 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.

Độc Tính : 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.

Chỉ Định : 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.

Liều Lượng & Cách Dùng : Injection, solution - Intravenous - 162MCI/6ML (27MCI/ML)

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty :

Sản phẩm biệt dược : Alpharadin
Công ty : Bayer Healthcare

Sản phẩm biệt dược : Xofigo

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB08913

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/50419-208-01

Wikipedia

http://en.wikipedia.org/wiki/Radium-223_chloride

RxList

http://www.rxlist.com/xofigo-drug.htm

Drugs.com

http://www.drugs.com/xofigo.html

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