By inhibiting the action of cathepsins, which are implicated in tumour invasion and metastasis, cathepsin inhibitors have showed potential as cancer treatments. Cathepsins K, B, and L are a few of the cathepsins that have been linked to the development of cancer. These enzymes might possibly be inhibited to reduce or stop cancer spread.

Odanacatib is a selective cathepsin K inhibitor that is currently in clinical development for the treatment of breast and prostate cancer. Talabostat, a dipeptidyl peptidase inhibitor that also inhibits cathepsin B, is another cathepsin inhibitor in clinical development for the treatment of cancer.

Cathepsin inhibitors have shown promising results in preclinical studies for the treatment of various types of cancer, including breast, prostate, lung, and pancreatic cancer. These compounds have the potential to improve the efficacy of chemotherapy and radiation therapy by reducing cancer metastasis.