While the evidence for an involvement of sphingolipids (SLs) in a variety of diseases is rapidly increasing, the development of sphingolipid-related drugs is still in its infancy. In fact, the recently FDA-approved fingolimod or FTY-720 (see chapter by J. Pfeilschifter for more information) is the first drug on the market to interfere with sphingolipid signaling. The reasons for this lagging are manifold and within this chapter we try to name some of them. Ceramide is in the center of sphingolipid metabolism. We describe the most important and most recent inhibitors for enzymes controlling cellular ceramide levels.