Enzelkitug

Enzelkitug is a humanized immunoglobulin monoclonal antibody specifically targeting human C-C motif chemokine receptor 8 (CCR8). Enzelkitug modulates immunosuppression in the tumor microenvironment by blocking CCR8-mediated signaling pathways and may play a role in research on various solid tumors and hematological malignancies.

CCR8 (human):32 pM (Kd), CCR8 (cynomolgus monkey):27 pM (Kd)

Method: Enzelkitug (the study used the development code RO7502175) was evaluated for binding to human and cynomolgus-monkey CCR8, ADCC against CCR8-positive cells and tumour-derived regulatory T cells, and cytokine release from human PBMCs.
Result: RO7502175 bound human and cynomolgus-monkey CCR8 with KD values of approximately 32 and 27 pM, respectively, selectively mediated ADCC against CCR8-positive regulatory T cells and caused minimal cytokine release from PBMCs.^[1]

Method: Enzelkitug (the study used the development code RO7502175) was evaluated after intravenous single- and repeated-dose administration to male and female cynomolgus monkeys. Pharmacokinetics, blood CCR8-positive regulatory T cells, cytokines and toxicity were assessed.
Result: RO7502175 showed a biphasic IgG1-like concentration-time profile, reduced circulating CCR8-positive regulatory T cells, produced minimal and transient cytokine secretion and was well tolerated, with a reported NOAEL of 100 mg/kg.^[1]

Human

Monoclonal

Unconjugated