pembrolizumab

Pembrolizumab (MK-3475) is a highly selective humanized monoclonal antibody that antagonizes PD-1. It can block the PD-1 protein on T cells and prevent their interaction with PD-L1 on cancer cells.

Quavonlimab (MK-1308) is a novel human monoclonal antibody designed to selectively target and block the immune checkpoint molecule cytotoxic T-lymphocyte-associated protein 4 (CTLA-4), investigation of quavonlimab in combination with the anti-PD-1 therapy KEYTRUDA (pembrolizumab) has shown encouraging anti-tumor activity along with an acceptable safety profile,making it an interesting compound for the reasearches into advanced non-small cell lung cancer (NSCLC).

Favezelimab (MK-4280), a humanized monoclonal antibody directed against LAG-3, inhibits the molecular interaction between LAG-3 and its ligand MHC class II, thereby restoring T-cell function. Favezelimab (MK-4280) has been evaluated as a candidate for colorectal cancer (CRC) research, particularly in studies that investigate synergistic effects in combination with the PD-L1 inhibitor Pembrolizumab .

Calderasib (MK-1084) is a selective KRAS G12C inhibitor with an IC50 value of 1.2 nM . Calderasib (MK-1084) exhibits significant anticancer activity, and it can be employed either as a monotherapy or in combination with the PD-1 inhibitor Pembrolizumab, providing a versatile approach for the investigation of KRAS-mutant driven cancers.

CD73-IN-3 (LY-3475070) is a potent and selective CD73 inhibitor with an IC50 of 28 nM, and its use alone or in combination with pembrolizumab is currently being tested in patients with advanced cancer.

ERG245 is a BCAT1 inhibitor that promotes oxidative phosphorylation (OXPHOS) in CD8+ T cells by selectively inhibiting the enzymatic activity of BCAT1, thereby increasing the cytotoxic capacity of CD8+ T cells. ERG245, when administered in combination with the anti-PD-1 antibody Pembrolizumab, induces tumor regression in preclinical settings, and it can be used as a research agent within the field of immuno-oncology.

Berahyaluronidase alfa is a recombinant human hyaluronidase that temporarily increases tissue permeability by degrading hyaluronan in the extracellular matrix, thereby facilitating the absorption and dispersion of co-administered subcutaneous drugs like pembrolizumab. Its application significantly enhances the bioavailability of large-molecule biologics via the subcutaneous route, enabling the transition from intravenous to more convenient subcutaneous delivery.