checkpoint

Monalizumab is a novel immune checkpoint inhibitor targeting natural killer cell population 2A (NKG2A). Monalizumab is a humanized monoclonal antibody against NKG2A that induces IFN-γ production, thereby activating natural killer cell function. Monalizumab has antitumor activity and can be used to study neck squamous cell carcinoma (HNSCC).

Vudalimab, a fully humanized bispecific monoclonal antibody, effectively inhibits both PD-1 and CTLA-4 immune checkpoint receptors. This dual action facilitates the selective activation of T-cells targeting tumors.

Cemiplimab (Anti-Human PD-1) is a human monoclonal antibody that inhibits the PD-1 PD-L1 pathway, serving as a checkpoint inhibitor. It is applicable in research on metastatic cancer and squamous cell skin cancer.

Dostarlimab (TSR-042) is a programmed cell death protein 1 (PD-1) receptor immune checkpoint inhibitor that blocks interactions with PD-L1 and PD-L2, used in the study of endometrial cancer.

Neihulizumab (ALTB-168), an immune checkpoint agonistic antibody, targets and binds to human CD162 (PSGL-1), resulting in the downregulation of activated T-cells. It is utilized in research aimed at treating steroid-refractory acute graft-versus-host disease (SR-aGVHD), psoriasis, psoriatic arthritis, and ulcerative colitis [1].

Tuvonralimab (PSB-205; QL1706), comprising a combination of Iparomlimab and Tuvonralimab [1], functions as a dual immune checkpoint inhibitor through its formulation of anti-PD-1 IgG4 and anti-CTLA-4 IgG1 antibodies.

Pacmilimab (CX-072) is a Probody immune checkpoint inhibitor targeting programmed death ligand 1 (PD-L1) with anti-tumor activity for the study of solid tumors.

Cudarolimab (IBI-101) is a fully human anti-OX40 antibody with potential immune checkpoint inhibitory and anti-tumor activity for the study of cancer.

Rulonilimab, a human IgG1 monoclonal antibody, targets and binds to PD-1, inhibiting its downstream signaling pathways. This action potentially enables immune checkpoint inhibition and exhibits anti-tumor activity [1].

Simlukafusp alfa (FAP-IL2v) is a tumor-targeting immune cytokine, a human IgG1 antibody, with antitumor activity and immunostimulatory properties that potentiate in vitro and in vivo activity of therapeutic antibodies mediating antibody-dependent or T-cell-independent cytotoxicity (TDCC) and programmed death ligand 1 (PD-L1) checkpoint inhibition.

COM701 is a humanized monoclonal antibody targeting PVRIG, an immune checkpoint inhibitor with anti-tumor activity, used in liver cancer research.

Tinurilimab (Bay 1834942) is a monoclonal antibody that targets and inhibits CEACAM6, an immune checkpoint regulator. Tinurilimab can be used in studies about effector T-cells against tumors.

Lesabelimab (LDP) is an anti-CD274 monoclonal antibody of the immunoglobulin G1-kappa subclass. It targets CD274, an immune checkpoint ligand that suppresses antitumor immunity by engaging with the PDCD1 receptor [1] [2].

Firastotug, an IgG1κ antibody, targets CTLA4, a cytotoxic T lymphocyte-associated protein that serves as a crucial immune checkpoint in autoimmunity and cancer [1].

Tuparstobart (Incagn-02385) is an IgG1κ monoclonal antibody targeting the immune checkpoint receptor protein LAG-3, predominantly expressed on activated T cells, NK cells, B cells, and plasmacytoid dendritic cells [1].

Ontorpacept (TTI-621) is a soluble fusion protein comprising the N-terminal (1-118) of human SIRPα fused to the Fc region of human IgG1. This N-terminal (1-118) segment serves as the binding domain for CD47, an inhibitor of macrophage-mediated phagocytosis. As a checkpoint inhibitor that blocks CD47, ontorpacept exhibits antitumor activity [1].

Dargistotug (M-6223) is a fully human IgG1 monoclonal antibody that targets TIGIT (T cell immune receptor with Ig domain and ITIM), an inhibitory immune checkpoint that depletes NK cells and reduces cytokine secretion via interaction with CD155. It also modulates effector T cell activity and enhances regulatory T cell (Tregs) function, contributing to immunosuppression [1].

Volrustomig is a bi-engineered fragment crystallizable (Fc) domain, a monovalent bispecific IgG1 monoclonal antibody targeting the key immune checkpoint receptors PD-1 and CTLA-4. It boosts T-cell activation and antitumor immunity, making it a promising immunotherapy for various cancers. Molecular weight: 146.77 kDa.

INBRX-105 is a recombinant humanized bispecific antibody that targets programmed death-ligand 1 (PD-L1) and 4-1BB (CD137), exhibiting potential checkpoint inhibition, immune stimulation, and anti-tumor activity. By binding to 4-1BB on activated T-lymphocytes and PD-L1 on tumor cells, INBRX-105 enhances T-cell co-stimulation and inhibits PD-L1-mediated T-cell suppression, potentially reducing tumor growth. It demonstrates anti-tumor efficacy and increased T-cell frequency in patients with solid tumors and in vivo. Molecular weight: 101.9 kD.

Lomvastomig is a bispecific antibody that targets PD-1 and TIM-3 to inhibit immune checkpoint regulation and enhance immune response. It is designed for cancer treatment by promoting T cell activation and overcoming immune suppression. [Molecular weight: 145.34 kDa]

Rilvegostomig is a bispecific humanized IgG1 antibody targeting the immune-regulating receptor programmed cell death protein 1 (PD-1) and the co-inhibitory immune checkpoint molecule T cell immunoreceptor with immunoglobulin (Ig) and immunoreceptor tyrosine-based inhibitory motif (ITIM) domains (TIGIT). It enhances T cell activation, fostering a robust anti-tumor immune response, especially in cancers such as non-small cell lung cancer (NSCLC). Molecular weight: 146.06 KD.

Ngm707 is a humanized monoclonal antibody that acts as a dual antagonist against the key inhibitory immune checkpoint receptors ILT2 and ILT4. It shows potential for immunomodulatory and antitumor effects and can be used alone or in combination to treat advanced solid tumors. Molecular weight: 148.32 kDa.

Ipilimumab (anti-CTLA-4) is an immunomodulatory monoclonal antibody directed against the cell surface antigen CTLA-4 and also a type of immune checkpoint inhibitor.