Lu-177-DOTAZOL

¹⁷⁷Lu-DOTAZOL is a drug suitable for betatherapy of bone metastases of prostate cancer. The molecule corresponds to a new class of bisphosphonate.

¹⁷⁷Lu-DOTAZOL is a derivative of zoledronic acid, a (cold) drug that has already proven efficacy in several phase III studies in the treatment of bone metastases secondary to all solid tumor types (in particular prostate cancer) and bone lesions from multiple myeloma. The drug is expected to work as an efficient pain palliation agent in all cancers progressing in bone metastases, and could improve OS in these patients. This drug is associated with the diagnostic agent ⁶⁸Ga-DOTAZOL.

¹⁷⁷Lu-DOTAZOL is at an early stage of development and just in a first stage of trial in human. Binding studies and preclinical data have shown superiority of ¹⁷⁷Lu-DOTAZOL over ¹⁵³Sm-EDTMP and ¹⁶⁶Ho-DOTMP.

Clinical data reporting on Biodistribution and Dosimetry in patients with osteoblastic metastases were published in November 2019 , confirming as a potential new drug for Radionuclide therapy of bone Metastasis. Data in a patient with primary osseous metastatic bronchial carcinoma was published in June 2020.

The drug is still in Phase I clinical trials in Germany and the progression of the development remains quite slow, showing some lack of priority and funds.

Target/Mechanism: Bones

Leading Emitter: beta electrons (β^–)