0000000000201540
AUTHOR
M. Miederer
Bone targeting compounds for radiotherapy and imaging: *Me(III)-DOTA conjugates of bisphosphonic acid, pamidronic acid and zoledronic acid
Background Bisphosphonates have a high adsorption on calcified tissues and are commonly used in the treatment of bone disorder diseases. Conjugates of bisphosphonates with macrocyclic chelators open new possibilities in bone targeted radionuclide imaging and therapy. Subsequent to positron emission tomography (PET) examinations utilizing 68Ga-labelled analogues, endoradiotheraphy with 177Lu-labelled macrocyclic bisphosphonates may have a great potential in the treatment of painful skeletal metastases. Methods Based on the established pharmaceuticals pamidronate and zoledronate two new DOTA-α-OH-bisphosphonates, DOTAPAM and DOTAZOL(MM1.MZ) were successfully synthesized. The ligands were labe…
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…