Cergutuzumab amunaleukin (CEA-IL2v) is a monomeric carcinoembryonic antigen (CEA)-targeted IL-2 variant-based immunocytokine. Cergutuzumab amunaleukin has immunostimulating and antineoplastic activities[1].
Cergutuzumab amunaleukin comprises a single IL-2 variant (IL2v) moiety with abolished CD25 binding, fused to the C-terminus of a high affinity, bivalent CEA-specific antibody devoid of Fc-mediated effector functions. Its molecular design aims to avoid preferential activation of regulatory T-cells vs. immune effector cells by removing CD25 binding[1].
The activation of NK cells by Cergutuzumab amunaleukin (CEA-IL2v; 0.001-1000 nM) translated into increased killing of the CEA-positive colon cancer cell line LS180 accompanied by increased release of Granzyme B, IFNγ and RANTES and upregulation of CD25 and CD69 on NK cells[1].
In tumor-free mice, a strong expansion of peripheral CD8+ T and NK cells after treatment with 0.5 and 2 mg/kg Cergutuzumab amunaleukin (CEA-IL2v; i.v.; once) is observed[1].
[1]. Christian Klein, et al. Cergutuzumab amunaleukin (CEA-IL2v), a CEA-targeted IL-2 variant-based immunocytokine for combination cancer immunotherapy: Overcoming limitations of aldesleukin and conventional IL-2-based immunocytokines. Oncoimmunology. 2017 Jan 11;6(3):e1277306.