38270-90-5[89Sr+2].[Cl-].[Cl-]AHBGXTDRMVNFER-FCHARDOESA-LStrontium chloride (Sr-89), initially FDA-approved in 1993, is used as a paliative therapeutic option to help relieve the pain from bone metastases. Strontium chloride is mainly used in cases of metastatic castrate-resistant prostate cancer. Bone metastases is a common and severe complication presented in advanced stages of the disease. It is usually presented mainly in patients with prostatic and breast cancer, as well as in cancer of lung, bladder and thyroid. There has been some cases of apparent tumor regression which has given it a potential tumoricidal effect.
38270-90-5In some studies performed in polluted water, it was showed that strontium is able to bind to plasma proteins. In human plasma studies, it has been shown a possible recovery of 45-60% of administered strontium by ultrafiltration, while other studies confirm a protein binding of 30-40%.
Metastatic bone lesions are zones of high bone mineral turnover. Thus, there is a constant need of calcium supply for the development of the malignancy. Strontium chloride 89 is a divalent ion, similar to calcium, therefore it is taken up by sites of active osteogenesis. This relieves bone metastatic-driven pain withouth generating important side effects and it also presents a very little radioprotection concern. Once combined with external beam radiotherapy, strontium chloride 89 can emit β particules with a maximum range in tissue of 6-8mm. This radiation is capable to reduce new bone metastases and produces an analgesic role.
Strontium chloride 89, a similar to calcium divalent ion, concentrates in areas of increased osteogenesis, by being taken up into the inorganic matter of the bone. Strontium chloride 89 presents a 10-fold higher affinity for metastatic bone. Some reports indicate that after Strontium chloride 89 is incorporated into the osteoid matrix adjascently to the metastatic cells, it emits β-rays getting even to 1.3-64Gy. Thus, there is a possible tumoricidal effect driven by the radiation selectively emited by strontium chloride 89 into metastatic bones.
Strontium can interact with components than normally bind to calcium, including hydroxyapatite (main component of mineralized bone), calcium-binding or calcium-transport proteins. It can form complexes with different inorganic anions like carbonate, citrate, phosphate, carboxylic acid or lactate.
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Following intravenous injection, strontium chloride 89 behaves like its calcium analog. It clears rapidly from the blood stream and selectively gets localized on the bone mineral, preferentially in zones of osteogenesis, where it can stay retained for about 14 days.
The elimination is done mainly by urinary excretion greatly in the two first days after injection. The rest of the elimination route is found in faeces. The percentage of urinary excretion may vary depending on the presence of bone lesions. The presence of strontium chloride 89 in faeces suggests an absorption into the gastrointestinal tract either by the bile or from the plasma.
There have been several studies regarding the pharmacokinetics of different administration routes of strontium chloride 89. The values are different but it ranges between 40-67L.
Strontium chloride 89 is mainly cleared by urine on a 3:1 ratio compared with fecal excretion. The total drug clearance can be slow, giving it a long half-life.