In this issue of Blood, Dairaghi and colleagues demonstrate the efficacy of a potent and orally bioavailable inhibitor of CCR1, one of the receptors for the chemokine CCL3/MIP-1, in a mouse model of multiple myeloma (MM) and MM bone disease. They show CCX721 to be a highly selective and efficient inhibitor of CCR1 and in turn a suppressor of osteoclastic activity, osteolytic lesions, and disease burden in a preclinical MM model.