Disease relevance of (1-hydroxy-1-phosphonooxy-ethoxy)phosphonic acid

• Phase 1 study of rhenium-186-HEDP in patients with bone metastases originating from breast cancer [1].
• Transient cranial neuropathy in prostatic cancer with bone metastases after rhenium-186-HEDP treatment [2].
• A Phase 1 dosage escalation study was performed using 186Re-HEDP in patients with metastatic breast cancer [1].
• Two patients who received 2960 MBq 186Re-HEDP showed Grades 3 (platelets 25-50 x 10(9)/l) and 4 (platelets < 25 x 10(9)/l) platelet toxicity, which was defined as unacceptable [1].
• Evaluation of thrombocytopenia in patients treated with rhenium-186-HEDP: guidelines for individual dosage recommendations [3].

High impact information on (1-hydroxy-1-phosphonooxy-ethoxy)phosphonic acid

• Furthermore, the EDrm50 (i.e., the bone marrow absorbed dose producing a 50% platelet decrease) to bone marrow for 186Re-HEDP was on the order of 2 Gy [4].
• CONCLUSION: Although the function of normal bone marrow is affected by metastases in patients with metastatic bone disease, the MIRD model can be used to relate toxicity to the bone marrow absorbed dose after a therapeutic dosage of 186Re-HEDP [4].
• Both patients developed transient cranial neuropathy shortly after treatment with 186Re-HEDP [2].
• Bone marrow absorbed dose of rhenium-186-HEDP and the relationship with decreased platelet counts [4].
• The pharmacokinetics of 186Re-HEDP, a radiopharmaceutical for palliative treatment of metastatic bone pain, was investigated in 11 patients (17 studies) who suffered from metastatic breast or prostate cancer [5].

Chemical compound and disease context of (1-hydroxy-1-phosphonooxy-ethoxy)phosphonic acid

• Rhenium-186 (tin) hydroxyethylidene diphosphonate (186Re-HEDP), a bone-seeking radiopharmaceutical, has been successfully used in the treatment of patients with painful bone metastases [2].
• Moreover, proposals made earlier to use 32P or 89Sr for palliation of pain in patients with disseminated skeletal metastases were picked up again and led also to other radiopharmaceuticals (186Re-HEDP, 153Sm-EDTMP, 117mSn-DTPA) which are applied today for the same purpose with very good success [6].
• Serum Hemoglobin Levels Predict Response to Strontium-89 and Rhenium-186-HEDP Radionuclide Treatment for Painful Osseous Metastases in Prostate Cancer [7].

Biological context of (1-hydroxy-1-phosphonooxy-ethoxy)phosphonic acid

• From this study we conclude that the maximally tolerated dose of 186Re-HEDP is 2960 MBq [8].
• Rhenium-186-HEDP was used to treat these osseous metastatic lesions due to its bone seeking kinetics attractive radiochemical properties [9].

Anatomical context of (1-hydroxy-1-phosphonooxy-ethoxy)phosphonic acid

• Two patients who received 3515 MBq 186Re-HEDP showed grade 3 toxicity (thrombocytes 25-50 x 10(9)/l), defined as unacceptable toxicity [8].
• The thorough clinical and laboratory investigation of both patients assessed that this extraosseous radio-rhenium accumulation was multifactorial with the main cause being a disturbance of body fluid acid-balance, favoring calcium and phosphate ion precipitation and leading to 186Re-HEDP extraosseous uptake [10].

Associations of (1-hydroxy-1-phosphonooxy-ethoxy)phosphonic acid with other chemical compounds

• Rhenium-186 hydroxyethylidene diphosphonate (186Re-HEDP) has been used for the palliative treatment of metastatic bone pain [8].

Analytical, diagnostic and therapeutic context of (1-hydroxy-1-phosphonooxy-ethoxy)phosphonic acid

• Scintigraphic images in rabbits after injecting 70-100 MBq of 186Re-CTMP and using a dual head gamma camera were observed to be superior to 186Re-HEDP, prepared by a procedure standardized by us [11].
• Patients described an improvement on Karnofsky performance status (KPS) from 73 +/- 7 percent to 85 +/- 8 percent 12 weeks after 188Re-HEDP (p < 0. 05), from 72 +/- 13 percent to 79 +/- 12 percent after 186Re-HEDP (p = 0.251), and from 62 +/- 14 percent to 69 +/- 16 percent after 89Sr (p = 0.415) [12].

References