PD-1/PD-L1 Inhibitor

Safimestomig (6MW3211) is an CD47/PD-L1-targeting bispecific antibody. Safimestomig blocks CD47-mediated 'don't eat me' signaling and selectively binds to CD47 on tumor cells. Safimestomig blocks PD-L1-mediated immune checkpoint signaling. Safimestomig can be used for the research of cancer.

PD-1/PD-L1-IN-42 (Compound B8.4) is an inhibitor of the interaction between PD-1 and PD-L1, with an EC₅₀ of 0.1 μM. PD-1/PD-L1-IN-42 can be used for the research of cancer immunotherapy.

PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC₅₀ value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8⁺ T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model.

Garivulimab (BGB-A333) is a humanized IgG1-variant monoclonal antibody that specifically targets and binds to PD-L1. Garivulimab selectively blocks the interaction of PD-L1 and PD-1. Garivulimab has antitumor activity.

PD-1/PD-L1-IN-10 (compound B2) is an orally active PD-1/PD-L1 inhibitor (IC₅₀ of 2.7 nM) with potent anticancer efficacy.

Pimivalimab (JTX-4014) is a PD-1 inhibitor. Pimivalimab can be used for the research of solid tumor.

PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC₅₀ of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.

Sudubrilimab (HS636) is an Ig G1-kappa monoclonal antibody against PDL1. Sudubrilimab is fused at the C terminus of the heavy chain to a TGF-β1 receptor Ⅱ ectodomain (TGFBR2-ECD), and which can sequester the PD-1/PD-L1 pathway and TGF-β bioactivity in the immunosuppressive tumor microenvironment.

Human PD-L1 inhibitor V, a human PD-1 protein binding peptide with a K_d value of 3.32 μM. Human PD-L1 inhibitor V inhibit the interaction of hPD-1/hPD-L1.

Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a K_d value of 1.38 μM. Human PD-L1 inhibitor IV inhibits the interaction of hPD-1/hPD-L1.

Sabestomig (AZD7789) is a monovalent bispecific antibody targeting PD-1 and TIM-3. Sabestomig binds to PD-1 and an epitope in the TIM-3 IgV domain outside the phosphatidylserine-binding cleft, thereby precisely regulating immune responses. Sabestomig promotes IL-2 production, efferocytosis and cross-presentation of tumor antigens, and enhances the release of anti-tumor T cell cytokines, cytotoxicity, and secretion of IFN-γ. Sabestomig inhibits the growth of solid tumors, prolongs the duration of tumor suppression, and significantly enhances anti-tumor responses following anti-PD-1 therapy. Sabestomig has been used in studies related to non-small cell lung cancer and classical Hodgkin lymphoma.

LP23 is a non-arylmethylamine PD-1/PD-L1 inhibitor (IC₅₀: 16.7 nM) with anti-tumor activity. LP23 restores immune cell function in HepG2/Jurkat T cells and promotes HepG2 cell death. LP23 is active in vivo in the B16-F10 tumor model (TGI=88.6% at 30 mg/kg).

Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.

PL120131 acetate is a PD-1 antagonist, can specifically blocking the interaction between PD-1 and PD-L1, thereby effectively inhibiting the PD-1-mediated apoptosis signaling pathway. PL120131 acetate rescues lymphocytes from apoptosis, maintains the survival and activity of T cells, and induces cytotoxic T lymphocytes to exert killing effects and recognize macrophages and dendritic cells. PL120131 acetate can be used in research related to breast cancer and various malignant tumors.

Finotonlimab (SCT-I10A) is a recombinant humanised IgG PD-1 antibody. Finotonlimab has the potential for solid tumors or lymphomas research.

Iparomlimab is an anti-human PD-1/CD279/PDCD1 IgG4κ antibody. Iparomlimab also targets to human monoclonal PSB103 γ4-chain, disulfided with human monoclonal PSB103 κ-chain to form a dimer. Iparomlimab can be used for Oncology research.

Xirestomig (ATG-101) is a tetravalent "2+2″ PD-L1×4-1BB bispecific antibody. Xirestomig binds PD-L1 and 4-1BB concurrently, with a greater affinity for PD-L1, and potently activated 4-1BB+ T cells when cross-linked with PD-L1-positive cells. Xirestomig activates exhausted T cells upon PD-L1 binding. Xirestomig displays potent antitumor activity in numerous in vivo tumor models, including those resistant or refractory to immune checkpoint inhibitors (ICIs).

BMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor with an IC₅₀ towards the PD-L1/PD-1 complex in the range of 18 to 200 nM. BMS-37 shows unspecific toxicity against modified Jurkat T cells with an EC₅₀ between 3 and 6 µM. BMS-37 can be used for the study of the PD-L1-induced exhaustion of T-cells or as PD-L1 ligand to synthesize PROTAC molecules.

PD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC₅₀ of 9.1 nM. PD-1/PD-L1-IN-63 blocks the PD-1/PD-L1 interaction, induces cancer cell death and inhibits tumor growth. PD-1/PD-L1-IN-63 can be used in the research of melanoma.

Balstilimab (AGEN2034) is a fully human monoclonal IgG4 antibody against PD-1.