0000000001026240
AUTHOR
M. Meckel
177Lu-labelled macrocyclic bisphosphonates for targeting bone metastasis in cancer treatment
Background: Metastatic bone lesion is a common syndrome of many cancer diseases in an advanced state. The major symptom is severe pain, spinal cord compression, and pathological fracture, associated with an obvious morbidity. Common treatments including systemic application of bisphosphonate drugs aim on pain reduction and on improving the quality of life of the patient. Particularly, patients with multiple metastatic lesions benefit from bone-targeting therapeutic radiopharmaceuticals. Agents utilizing beta-emitting radionuclides in routine clinical praxis are, for example, [89Sr]SrCl2 and [153Sm]Sm-EDTMP. No-carrier-added (n.c.a.) 177Lu is remarkably suitable for an application in this sc…
Additional file 1: of Bone targeting compounds for radiotherapy and imaging: *Me(III)-DOTA conjugates of bisphosphonic acid, pamidronic acid and zoledronic acid
Figure S1. Quality control of [68Ga]DOTAZOL by means of cross checked radio-HPLC and radio-TLC, as a representative of 68Ga-labelled bisphosphonates. A: After 15 min reaction time. B: After SPE purification. A(HPLC): Rt([68Ga]DOTAZOL) = 0.6 min. (88 %), Rt([68Ga]DFO) = 4.1 min. (12 %). B(HPLC): Rt([68Ga]DOTAZOL) = 0.6 min. (98 %). A(TLC): Rf([68Ga]DOTAZOL) = 0.1 (85 %), Rf([68Ga]acetylacetonate) = 0.9 (15 %). B(TLC): Rf([68Ga]DOTAZOL) = 0.1 (99 %). Control(TLC): Rf([68Ga] acetylacetonate) = 0.9 (99 %). Figure S2. Radio-HPLC of [177Lu]DOTAZOL on a Zorbax 300SB-C18 9,4 × 250 mm 5 μ, A = 100 mM TEAP pH = 2,24, isocratic flow: 1 ml/min. Figure S3. Radio-HPLC of urine and blood samples after adm…