Caspase-1, formerly known as Interleukin-1 converting enzyme (ICE), is a cysteine protease known for its role in mediating inflammation and its ability to induce programmed cell death via inflammasome activation (pyroptosis). Caspase-1 inhibitors are being studied for their possible therapeutic benefits in disorders involving chronic inflammation and for their ability to stop damage caused by pyroptosis in diseases such as Huntington’s and HIV. Solving of the crystal structure of caspase-1 has opened the door for more efficient strategies of CASP1 inhibitor design based on the structure of the binding site. Numerous caspase-1 inhibitors are currently available; some which are specific to caspase-1 while others work on multiple caspase subfamilies.