PD-1/PD-L1 Inhibitor

Pumitamig (PM-8002, BNT-327) is a bispecific antibody targeting PD-L1 and VEGF-A, with immune activation and anti-angiogenic activities. By binding to PD-L1, Pumitamig restores the function of effector T cells, while neutralizing VEGF-A in the tumor microenvironment to reverse its inhibition on the infiltration and activation of immune cells and normalize tumor blood vessels. Pumitamig can also be combined with various ADCs targeting TROP2, B7H3, HER2, HER3 for the research of advanced/metastatic solid tumors, including non-small cell lung cancer, ovarian cancer, triple-negative breast cancer, cervical cancer, etc. Pumitamig also exhibits potential efficacy in "cold" tumors with low PD-L1 expression that are insensitive to immunotherapy.

Cilengitide TFA (EMD 121974 TFA) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC₅₀ values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide TFA inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide TFA inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide TFA can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.

Anti-Mouse PD-1 Antibody (S-5001) is a selective inhibitor targeting PD-1, blocking the PD-1/PD-L1 immune checkpoint axis through competitive binding to PD-1. Anti-Mouse PD-1 Antibody (S-5001) works by reversing the tumor immunosuppressive microenvironment and reactivating the anti-tumor activity of cytotoxic T lymphocytes. It can be used in research on tumors such as melanoma and HPV-positive oropharyngeal squamous cell carcinoma. Anti-Mouse PD-1 Antibody (S-5001) is often combined with photothermal therapy, chemotherapy, etc., to enhance efficacy.

Cadonilimab (AK104) is a humanized tetravalent IgG1 bispecific antibody targeting PD1/CTLA4. Cadonilimab blocks both PD-1 and CTLA-4 pathways, thereby relieving their corresponding immunosuppressive effects and reversing tumor specific T cell exhaustion. Cadonilimab significantly downregulates Fc-mediated effector functions, including antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), complement dependent cytotoxicity (CDC). Cadonilimab can be used for research of metastatic cervical cancer, as well as other malignancies such as gastric cancer, GEJ adenocarcinoma and non-small cell lung cancer (NSCLC).

Camrelizumab (SHR-1210) is a potent humanied high-affinity IgG4-κ monoclonal antibody (mAb) to PD-1. Camrelizumab binds PD-1 at a high affinity of 3 nM and inhibits the binding interaction of PD-1 and PD-L1 with an IC₅₀ of 0.70 nM. Camrelizumab acts as anti-PD-1/PD-L1 agent and can be used for cancer research, including NSCLC, ESCC, Hodgkin lymphoma, and advanced HCC et,al.

Avelumab (anti-PD-L1) a fully human IgG1 anti-PD-L1 monoclonal antibody (mAb) with potential antibody-dependent cell-mediated cytotoxicity (ADCC). Avelumab (anti-PD-L1) enhances ADCC on several cancer cell lines expressing PD-L1. Avelumab (anti-PD-L1) can be used for the study of chordoma.

Cemiplimab (Anti-Human PD-1) is a high-affinity programmed death receptor-1 (PD-1) monoclonal IgG4 antibody that blocks PD-1/PD-L1-mediated T-cell suppression. Cemiplimab is commonly used in squamous cell skin cancer research.

Acesulfame potassium is a synthetic sweetener. Long-term use of Acesulfame potassium can affect cognitive function, possibly by altering the neurometabolic functions in mice. Acesulfame potassium can suppress autophagic degradation of PD-L1 in RIL-175 and SK-Hep1 cells through the ERK1/2-mTORC1-ULK1 pathway, which may be related to immune evasion in cancer cells. Acesulfame potassium can be used in research on neurological diseases, metabolic disorders, cancer, and immune evasion.

Durvalumab (anti-PD-L1)(MEDI 4736) is a human anti-PD-L1 protein monoclonal antibody. Durvalumab (anti-PD-L1) completely blocks PD-L1 binding to PD-1 and CD80, IC ₅₀ are 0.1 and 0.04 nM respectively, has anti-tumor activity.

CD24/Siglec-10 blocking peptide, CSBP can not only block the interaction of CD24/Siglec-10 but also PD-1/PD-L1. CD24/Siglec-10 blocking peptide, CSBP can induce the phagocytosis of tumor cell.

BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC₅₀ of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.

PF-08046054 (SGN-PDL1V) is a PD-L1-directed Antibody-drug conjugate (ADC), which is comprised of an anti-PD-L1 antibody conjugated to VcMMAE (HY-15575). PF-08046054 is direct cytotoxicity to PD-L1-expressing tumor cells via the intracellular delivery of MMAE. PF-08046054 can be used for the study of solid tumors

IBI-363 is a PD-1/IL-2 bispecific antibody with functions of blocking the PD-1/PD-L1 pathway and activating the IL-2 pathway. The IL-2 arm of IBI-363 retains affinity for IL-2Rα but attenuates binding ability to IL-2Rβ and IL-2Rγ to reduce toxicity. The PD-1 binding arm of IBI-363 enables PD-1 blockade and selective delivery of IL-2. IBI-363 can be used in cancer research, such as non-small cell lung cancer.

SSGJ-707 (PF-08634404) is a bispecific antibody targeting VEGF and PD-1. SSGJ-707 exerts dual anti-tumor effects by neutralizing VEGF and blocking the PD-1 signaling pathway. SSGJ-707 can be combined with platinum-based chemotherapy to inhibit advanced non-small cell lung cancer (NSCLC), and its inhibitory effect is not limited by PD-L1 expression levels. In the HARMONi-2 trial, the objective response rate of SSGJ-707 correlates with the PD-L1 tumor proportion score, and the incidence of grade ≥3 adverse events is comparable to that of Inetetamab (HY-P99969). SSGJ-707 is being extensively investigated for a variety of malignancies including advanced NSCLC, colorectal cancer and small cell lung cancer.

CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of T cells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes.

INCB086550 is a potent, oral, small-molecule PD-L1 inhibitor with IC_50s value of 3.1, 4.9 and 1.9 nM for human, cynomolgus, and rat, respectively. INCB086550 promotes the dimerization of cell-surface PD-L1 and induces PD-L1 entry into Golgi vesicles then traffick to the nucleus. INCB086550 can be used for multiple cancers research.

Gilvetmab is a canine-derived anti-cPD-1 monoclonal antibody, as well as an immune activator/antitumor agent. Gilvetmab binds to canine PD-1, blocks the interaction of PD-1/PD-L1/L2, prevents immunosuppression, reactivates antitumor responses, induces tumor regression or disease stabilization, and may also trigger pseudoprogression. Gilvetmab can be used in research related to malignant melanoma and mast cell tumors.

PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC₅₀ of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model.

BMS-986189 is a macrocyclic peptide PD-1/PD-L1 interaction with an IC₅₀ of 1.03 nM inhibitor. BMS-986189 can be used for cancer research, such as human lung carcinoma cells L2987.

Serplulimab (HLX 10) is a humanized anti-PD-1 monoclonal antibody. Serplulimab can inhibit tumor growth, regulate the tumor microenvironment, and has anti-tumor activity. Serplulimab can be used in the research of cancer such as lung cancer and colon cancer.