Osteosarcoma is the most common primary cancer of the bone that arises from progenitor cells with osteoblastic differentiation. It is defined as a rare disease, with an annual incidence of about 1–5 cases per million individuals, predominantly affecting adolescents and young adults aged 15-25.1
The standard of care is chemotherapy, surgery and external beam radiotherapy. Many patients with non-metastatic osteosarcoma can survive long-term, but a high proportion does not respond well to treatment or recurs, resulting in the need for alternative therapy options.
N.c.a. 177Lu-Zoledronate is an innovative Targeted Radionuclide Therapy agent under investigation for patients suffering from osteosarcoma or osteoblastic bone metastases.
N.c.a. 177Lu-Zoledronate consists of two molecular components – firstly, n.c.a. Lutetium-177 (EndolucinBeta®), a synthetic, low-energy beta-emitting isotope of Lutetium, and secondly, the novel bisphosphonate derivate Zoledronate. The targeting molecule Zoledronate binds with high affinity to the bone mineral hydroxyapatite and inhibits osteoclast activity, providing direct treatment options for degenerative bone disorders and cancer.2
N.c.a. 177Lu-Zoledronate has been shown to accumulate in bone with osteoblastic metastatic disease, with potential therapeutic benefit.3
Due to the versatile properties of Zoledronate for radiolabeling, it is a promising precursor for the development of other future-oriented radionuclide therapeutic concepts in the field of Precision Oncology, such as Targeted Alpha Therapy.
1 Savage & Mirabello, 2011, Sarcoma
2 Farrell et al., 2018, Bone Reports 9: 47–60
3 Berenson, 2005, The Oncologist 10(1): 52-62 and
Khawar et al., 2019, EJNMMI Research 9(102)