Talabostat (Val-Boro-pro, PT-100, BXCL-701) is designed to inhibit the enzymatic activity of FAP, and several phase I and II clinical trials have shown promising results in multiple cancers, including pediatric solid tumors, metastatic colorectal cancer, melanoma and nonsmall-cell lung cancer, with improvements in response rates and prolonged states of stable disease. The gene discussed is FAP; the disease is lung cancer.