PD-1/PD-L1 Inhibitor

Acasunlimab (GEN1046) is a bispecific antibody (bsAb) targeting PD-L1 and 4-1BB. Acasunlimab enhances T-cell and NK-cell function through conditional 4-1BB stimulation while constitutively blocking the PD-1/PD-L1 inhibitory axis. Acasunlimab can be used in research of cancer.

Ertabresib (INCB-057643) is an orally active BET protein inhibitor. Ertabresib blocks gene transcription by targeting the BET protein family, induces cell cycle arrest and apoptosis by downregulating proto-oncogenes such as c-MYC, and additionally reduces the expression of FOXP3 and PD-L1 to improve the immune microenvironment. It also exerts synergistic effects and overcomes drug resistance when combined with chemotherapy and XPO1 inhibitors. Ertabresib can be used in research related to high-grade B-cell lymphoma with MYC and BCL2 rearrangements, pancreatic cancer, pancreatitis, and metastatic castration-resistant prostate cancer.

Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.

dBET57 is a potent and selective BRD4_BD1 PROTAC degrader with a DC₅₀ of approximately 500 nM. dBET57 forms a ternary complex with CRL4^CRBN and BRD4_BD1, induces the ubiquitination and degradation of BRD4, and indirectly inhibits the transcription of MYCN, c-Myc and PD-L1, ultimately leading to cell cycle arrest and apoptosis. dBET57 can be used in related research on neuroblastoma, non-small cell lung cancer and colorectal cancer.

Opucolimab (HLX20) is an engineered anti-PD-L1 humanised IgG1 antibody. Opucolimab, when conjugated with camptothecin toxoid, yields the PD-L1-targeting ADC, HLX43 (HY-177439). HLX43 can be used for non-small cell lung cancer (NSCLC), head and neck squamous cell carcinoma (HNSCC), esophageal squamous cell carcinoma (ESCC), melanoma (MEL), ovarian cancer (Ovc) research.

Adebrelimab (SHR-1316) is a humanized IgG4 monoclonal PD-L1 (PD-1/PD-L1) antibody. Adebrelimab has promising antitumor activity in solid tumors including extensive-stage small-cell lung cancer (SCLC).

Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities.

Atranorin is a secondary metabolite of lichens and AKT inhibitor. Atranorin possesses multiple activities such as antibacterial, anti-inflammatory, antioxidant, anti-glycation, analgesic, and anti-tumor effects. Atranorin has IC₅₀ values for scavenging DPPH and ABTS free radicals of 117 μM and less than 10 μM, respectively. Additionally, Atranorin also exhibits effects in promoting wound healing. Atranorin can be used in the research of various diseases, including myelodysplastic syndromes, tumors, and inflammatory conditions.

Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC₅₀s of 1.8 and 1.5 nM, respectively.

Cosibelimab (CK-301) is a high-affinity, fully human PD-L1-blocking monoclonal antibody that binds PD-L1 and blocks its interaction with PD-1. Cosibelimab exhibits antitumor efficacy.

Penpulimab is an IgG1 backbone anti-PD-1 monoclonal antibody with antitumor activities.

PD-L1-IN-1 (Compound 10) is a potent PD-L1 inhibitor with an IC₅₀ of 115 nM. PD-L1-IN-1 strongly binds with the PD-L1 protein and challenged it in a co-culture of PD-L1 expressing cancer cells and peripheral blood mononuclear cells enhanced antitumor immune activity of the latter. PD-L1-IN-1 significantly exhibits low cytotoxicity in healthy cells.

MAX-10181 (PD-1/PD-L1-IN-30) is a PD-1/PD-L1 binding inhibitor, with an IC₅₀ value of 0.018 μM. MAX-10181 can be used for research of cancers and other related diseases.

N-deacetylated BMS-202 is the deacetylated of BMS-202. BMS-202 is an inhibitor of the PD-1/PD-L1 interaction, mainly used for cancer treatment.

Evixapodlin (GS-4224) is a human PD-1/PD-L1 protein/protein interaction inhibitor with an IC₅₀ of 0.213 nM. Evixapodlin has anticancer and antiviral functions.

Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2-Mouse IgG1) is a recombinant chimeric version of the original 10F.9G2 antibody (HY-P99145). The variable domain sequences are identical to the original 10F.9G2 but the constant region sequences have been switched from rat IgG2b to mouse IgG1. Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2-Mouse IgG1) contains no Fc mutations just as the original rat IgG2b antibody does not. Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2-Mouse IgG1) blocks PD-1 signaling. Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2-Mouse IgG1) can be used for the research of cancer.

Anti-Mouse PD-1 Antibody (J43) is a kind of armenian hamster IgG antibody inhibitor, targeting to mouse PD-1. Anti-Mouse PD-1 Antibody (J43) inhibits the interaction of PD-1 with PD-L1. Anti-Mouse PD-1 Antibody (J43) can be used for the researches of cancer and immunology, such as breast cancer and colon cancer.

RC148 is a humanized IgG1 bispecific antibody targeting VEGF and PD-1. RC148 blocks PD-1-PD-L1 and VEGF-VEGFR interactions, triggers VEGF-dependent enhanced PD-1 binding, enables VEGF crosslinking, and inhibits PD-1-mediated immunosuppression. RC148 can be used for the research of metastatic gastric/gastroesophageal junction adenocarcinoma, non-small cell lung cancer, and metastatic breast cancer.

ARB-272572 is an oral effective small molecule PD-L1 inhibitor, with an IC₅₀ value of 400 pM. ARB-272572 has research significance in tumors and chronic viral infections.

Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation.