In a first-in-man study, the safety, pharmacokinetics and pharmacodynamics of a daily oral administration of Debio 1143 (monotherapy) was investigated in cancer patients, and showed that the IAPa was well tolerated at doses up to 900 mg daily (QDx5 every 3 weeks), elicited BIRC2 target engagement in PBMCs and skin biopsies, and induced a moderate increase in cytokine and chemokine that are mechanistically related to NF-kB signaling modulation [50, 64]. Here, NFKB1 is linked to cancer.