An orally bioavailable gallium (Ga)-based small molecule agent with potential anti-bone resorption and antineoplastic activities. Upon oral administration, AP-002 selectively inhibits osteoclast differentiation and bone resorption, and may promote the growth of osteoblasts thereby improving the skeletal sequelae of bony metastases which include pain, spinal cord compression, fractures and hypercalcemia of malignancy. Additionally, AP-002 may, through an as of yet undescribed mechanism of action, directly target and kill bone tumor cells.