PD-1/PD-L1-IN-19 (Example 22) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-19 blocks PD-1/PD-L1 with the IC50 of 62.3 nM. PD-1/PD-L1-IN-19 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].
N2S2-CBMBC, an N2S2 bromo-benzyl ether derivative, acts as a ligand and use 99mTc-labelled complexes 99mTc-N2S2-CBMBC can be used as an imaging agent to be applied to the aspect of detecting PD-L1 expression, realize the real-time, comprehensive and convenient detection of the PD-L1 level of tumors, and overcome the defects of an immunohistochemical method[1].
Latikafusp (AMG 256) is a bifunctional fusion protein comprising a PD-1-targeting antibody and IL-21 mutein designed to deliver IL-21 pathway stimulation to PD-1+ cells. Latikafusp is designed to prime and extend the activity of cytotoxic and memory T cells and induce anti-tumor immunity. Latikafusp has the potential for solid tumors research[1][2].
PD-1-IN-17 is a programmed cell death- 1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM[1].
Eciskafusp alfa is a programmed cell death 1 (PDCD1, best known as PD-1) cis-targeted IL2v immunocytokine. Eciskafusp alfa preferentially targets antigen-specific stem-like PD-1+ TCF-1+ CD8+ T cells and differentiates them towards a novel population of better effectors. Eciskafusp alfa can be used for the research of cancer and chronic infections[1].
BMS-1 is an inhibitor of the PD-1/PD-L1 protein/protein interaction.
PD-1/PD-L1-IN-24 is a highly potent PD-1/PD-L1 inhibitor with IC50 value of 1.57 nM. PD-1/PD-L1-IN-24 can restore T-cell function at the cellular level by significantly elevating the IFN-γ level. PD-1/PD-L1-IN-24 has low toxicity on the PBMCs[1].
NP-12 is a peptide antagonist of the PD-1 signaling pathway, which acts as an immunomodulatory agent for cancer therapy[1].
PD-1/PD-L1-IN 5 is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM[1].
Toripalimab is the first domestic anti-tumor PD-1 antibody in China. Toripalimab is a selective, recombinant, humanized monoclonal antibody against PD-1. Toripalimab is able to bind to PD-1 and block the interaction with its ligands. Toripalimab has exhibited primary anti-tumor effects in tumors such as melanoma, lung cancer, digestive tract tumors, hepatobiliary and pancreatic tumors, neuroendocrine neoplasms, nasopharyngeal carcinoma and urothelial carcinoma[1].
Geptanolimab (CBT-501) is a humanized IgG4k monoclonal antibody against programmed death-1 (PD-1). Siplizumab inhibits the binding of PD-L1/L2 to PD-1 through a competitive action. Siplizumab can be used in research of cancer[1].
PD-1/PD-L1-IN 5 is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM[1].
Rosnilimab is a humanized IgG1-κ antibody targeting to PD-1[1][2].
PD1-PDL1-IN 1 is a potent programmed cell death 1 (PD-1) inhibitor. PD1-PDL1-IN 1 is useful as immune modulator[1].
Zeluvalimab (AMG-404) is a monoclonal antibody targeting the PD-1 receptor that can be used for the research of cancer[1].
Sotiburafusp alfa is a bispecific fusion protein, which is a humanized VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) fused via the peptide linker 101GGSGGSGGSGGSGGS115 to the N-terminus of the heavy chain (116-564) of a humanized IgG1-kappa anti-human PD-L1 heavy chain variant L352>A, L353>A. Sotiburafusp alfa is also an angiogenesis inhibitor[1].
Serplulimab is humanized monoclonal anti-PD-1 antibody[1].
Ezabenlimab (BI-754091) is an anti-PD-1 mAb with binding constant Kd value of 6 nM (CHO cells). Ezabenlimab blocks the interaction of PD-1 with PD-L1 and PD-L2. Ezabenlimab increases interferon-γ secretion in T cells, and inhibits tumor growth in vivo[1].
Nivolumab (anti-PD-1) is a programmed death receptor-1 (PD-1) blocking human IgG4 antibody to treat advanced (metastatic) non-small cell lung cancer[1].
Danburstotug (IMC-001) is an IgG1-lambda anti-CD274 (PDL1, B7 homologue 1, B7H1) humanized monoclonal antibody. Danburstotug also is immunostimulant and antineoplastic[1].
Tagitanlimab (HBM-9167) is a humanized anti-PD-L1 antibody (IgG1κ type). Tagitanlimab selectively blocks the interaction of PD-L1 and PD-1. Tagitanlimab has the potential to be studied in recurrent or metastatic nasopharyngeal carcinoma (NPC)[1][2].
Balstilimab (AGEN2034) is a fully human monoclonal IgG4 antibody against PD-1[1].
Pembrolizumab is a humanized antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.
Retifanlimab is an anti-programmed cell death protein 1 (anti-PD-1) monoclonal antibody (mAb). Retifanlimab can be used for the research of gastroesophageal adenocarcinoma (GEA)[1].
PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC50 of 132.8 nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model[1].
ASC-69 (APY69)is a potent and promising?PD-1/PD-L1 small-molecule inhibitor[1].
LSD1-IN-27 (Compound 5ac) is a LSD1 inhibitor (IC50: 13 nM). LSD1-IN-27 inhibits the stemness and migration of gastric cancer cells. LSD1-IN-27 also reduces the expression of PD-L1 in BGC-823 and MFC cells. LSD1-IN-27 can enhance T cell immune response in gastric cancer[1].
Manelimab is a monoclonal antibody that inhibits programmed death-ligand 1 (PD-L1)[1].
Izuralimab is a bispecific IgG1 antibody targeting inducible T-cell costimulator (ICOS/CD278) and PD-1[1].
Acrixolimab a humanized IgG4-κ antibody, targeting to PD-1[1][2].