HANK & LIN'S GROUP

¹⁷⁷Lu/⁶⁸Ga-P15-073

A novel bisphosphonate-based radioligand therapy (RLT) agent for bone metastases:

Introduction

1. Bone metastases are a common complication in advanced cancers, particularly in prostate, breast, and lung cancer, leading to severe pain, fractures, and impaired quality of life. Radioligand therapy (RLT) has emerged as a promising approach to selectively target metastatic bone lesions while minimizing off-target toxicity.
2. [¹⁷⁷Lu/⁶⁸Ga]P15-073 is a novel bisphosphonate-based theranostic agent designed for both imaging and targeted radionuclide therapy of bone metastases. This dual-labeled radiopharmaceutical consists of a bisphosphonate moiety for high-affinity binding to hydroxyapatite in bone lesions, a chelator for radiometal incorporation, and either 68Ga for PET imaging or 177Lu for therapeutic applications.
3. The therapeutic form ([¹⁷⁷Lu]Lu-P15-073) delivers beta radiation to osteoblastic and osteolytic metastases, effectively reducing tumor burden and alleviating symptoms. Meanwhile, the diagnostic counterpart ([⁶⁸Ga]Ga-P15-073) provides real-time PET imaging for precise lesion detection, dosimetry, and treatment planning.

Preclinical and early clinical studies suggest that P15-073 demonstrates:

• High and selective bone metastasis uptake
• Favorable pharmacokinetics for effective tumor retention
• Minimal off-target accumulation, ensuring a better safety profile compared to conventional bone-seeking radiopharmaceuticals

Given its unique properties, [¹⁷⁷Lu/⁶⁸Ga]P15-073 represents a next-generation theranostic solution for metastatic bone disease, offering improved patient outcomes through precision medicine.