Zimberelimab (GLS-010) is a fully human IgG4 anti-PD-1 monoclonal antibody with an EC50 of 210 pM for human PD-1. Zimberelimab effectively blocks the binding of PD-L1 and PD-L2 to cell-surface PD-1 in CHO-S cells, with IC50 values of 580 pM and 670 pM, respectively. Zimberelimab shows antitumor activities, and can be used for various cancers research, including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma.
Zimberelimab has an EC50 of 210 pM for human PD-1 but does not bind to related CD28 family receptors, such as ICOS, CD28 and CTLA-4[1].Zimberelimab binding to cell-expressed human PD-1 inhibits the interaction of the receptor with both human PD-L1 and PD-L2 with IC50s of 580 pM and 670 pM, respectively[1].Zimberelimab dose-dependently enhances IFN-γ production and proliferation by CD4+ T cells, saturating at concentrations below 100 pM[1].
Zimberelimab (10 and 20 mg/kg; i.v.; BIW*3) shows significant anti-tumor effects in mice[2].PK parameters of Zimberelimab after single vd administrations of 2, 6, and 18 mg/kg in cynomolgus macaques[2]
References:
[1]. Markham A. Zimberelimab: First Approval. Drugs. 2021 Nov;81(17):2063-2068.
[2]. Lou B, et al. Preclinical Characterization of GLS-010 (Zimberelimab), a Novel Fully Human Anti-PD-1 Therapeutic Monoclonal Antibody for Cancer. Front Oncol. 2021 Sep 15;11:736955.