NP-12 is a branched peptide designed from analysis of the strands and loops of programmed cell death protein 1 (PD-1) at the interface of the PD-1/ programmed cell death ligand 1 (PD-L1) interaction. NP-12 binds to PD-L1 and is a functional equipotent antagonist of both PD-L1 and PD-L2 signaling. In preclinical models of melanoma, colon cancer, and kidney cancers, NP-12 showed significant efficacy in inhibiting primary tumour growth and metastasis. NP-12 shows antitumour activity in pre-established tumour models either as a single agent or when in combination with other immunologic cell death agents.