Ceramide 1-phosphate (C1P) possesses emerging and diversified roles in the regulation of various physiological and pathological processes, including cell proliferation, apoptosis and inflammation. Data have established a proinflammatory role for C1P and have also produced information on the structure, function, substrate specificity and regulatory mechanisms of its synthesizing enzyme, ceramide kinase (CERK). This review focuses on the rationale for designing specific inhibitors of CERK and provides evidence for the potential of CERK inhibition as a promising anti-inflammatory therapy.