Multiple Myeloma (MM) is malignant haematological disease characterized by uncontrolled proliferation of monoclonal plasma cells (PC) in bone marrow (BM). The receptor, CXCR4 is widely expressed on hematopoietic cells including MM cells and respond to CXCL12 gradients for mobilization through blood stream and bone marrow. CXCL12 plays an important role in recruitment of MM cells to bone marrow microenvironment and formation of neoangiogenic niches supporting tumor growth, survival and metastasis. The integral role of this chemokine-receptor axis in development of MM makes it a desirable target for therapeutics. In this review, we outline the background on MM and role of specific chemokine CXCL12 in the disease with an attempt to highlight the targeted therapeutics for its signaling receptor CXCR4 in MM.