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DOTA-zoledronate
- Development stage
- Unknown
- Lead developer
- ITM Isotope Technologies
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
**DOTA-zoledronate** is a DOTA-conjugated derivative of the third-generation bisphosphonate zoledronic acid, designed as a radiopharmaceutical precursor for theranostic applications in bone metastases. The DOTA chelator enables radiolabeling with isotopes such as **68Ga** for PET/CT imaging or **177Lu** for targeted radionuclide therapy, leveraging zoledronic acid's high affinity for hydroxyapatite in bone and potent antiresorptive activity via inhibition of farnesyl pyrophosphate synthase (FPPS) in osteoclasts. It exhibits rapid uptake and prolonged retention in osteoblastic lesions with favorable biodistribution, showing promise in patients with metastatic castration-resistant prostate cancer (mCRPC) and other bone-metastatic cancers, with preclinical and early clinical data supporting its safety and dosimetry profile superior to some established bone-seeking agents.[1][2][3][4][7]
- Other names
- DOTA-ZOLDOTA-conjugated zoledronic acidZOL
02
Targets
FDPS (Farnesyl pyrophosphate synthase)
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