Table 1 Activity and protease stability of 12G1 and V900.

From: Preclinical development of a bispecific TNFα/IL-23 neutralising domain antibody as a novel oral treatment for inflammatory bowel disease

Assay

12G1

V900

Human IL-23/IL-23R ELISA

0.2 nM

0.2 nM

Cynomolgus monkey IL-23/IL-23R ELISA

NT

0.7 nM

Cellular potency in mouse splenocytes

9.3 nM

10.7 nM

KD

NT

0.032 nM

Mouse small intestinal stability 1

51% (1 h)

51% (4 h)

Mouse small intestinal stability 2

22% (1 h)

40% (4 h)

Human faecal stability

5.6% (4 h)

29% (16 h)

  1. The activity of each SDA was measured in functional receptor/ligand inhibition ELISAs and a primary cell assay using mouse splenocytes. Potency (IC50) and affinity values shown are in nM. Protease stability was measured by incubating SDAs in pooled mouse small intestinal (2 biological replicates) or human faecal supernatants for relevant time periods and detecting residual activity in the human IL-23/23R functional ELISA. Stability values are %, brackets indicate incubation time in hours. NT = not tested.
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