Our lead compound, the orally bioavailable, LOX inhibitor, LXG6403 overcomes chemotherapy resistance in several chemoresistant in vitro, organoid, and in vivo models of highly aggressive triple negative breast cancer (TNBC). The optimization studies of the current lead are on-going to advance it towards an IND application. In addition, we have several other compounds with variable selectivity towards different lysyl oxidase family members. We execute an extensive and tedious optimization pipeline for each candidate to improve on-target potency, oral bioavailability, in vivo efficacy in combination with standard therapies, while addressing any metabolic or toxicity liabilities.