Table 1 V565 displays similar potency to approved anti-TNFα agents.

From: Preclinical Development of a Novel, Orally-Administered Anti-Tumour Necrosis Factor Domain Antibody for the Treatment of Inflammatory Bowel Disease

Assay Method

Antibody

TNFα

Functional Readout

Potency IC50 or KD (nM)

Biosensor

V565

sTNFα

TNFα association and dissociation kinetics

0.017b

Biosensor

adalimumaba

sTNFα

TNFα association and dissociation kinetics

0.005b

ELISA

V565

sTNFα

Inhibition of TNFα-TNFR2 interaction

0.41c

ELISA

adalimumab

sTNFα

Inhibition of TNFα-TNFR2 interaction

0.21c

ELISA

V565

sTNFα

Inhibition of TNFα-TNFR1 interaction

0.6c

ELISA

adalimumab

sTNFα

Inhibition of TNFα-TNFR1 interaction

0.2c

L929 cell viability

V565

sTNFα

Inhibition of TNFα-induced cell cytotoxicity

0.27d

L929 cell viability

adalimumab

sTNFα

Inhibition of TNFα-induced cell cytotoxicity

0.17d

HEK-NFkB-cells

V565

sTNFα

Inhibition of TNFα-induced NFkB-SEAP

0.3d

HEK-NFkB-cells

V565

tmTNFα

Inhibition of tmTNFα-CHO induced NFkB-SEAP

5.2d

HEK-NFkB-cells

adalimumab

tmTNFα

Inhibition of mTNFα-CHO induced NFkB-SEAP

3.1d

HEK-NFkB-cells

infliximab

tmTNFα

Inhibition of mTNFα-CHO induced NFkB-SEAP

3.8d

  1. aAdalimumab Fab fragment.
  2. bKD equilibrium dissociation constant.
  3. cIC50 concentration of V565 or adalimumab required to achieve 50% inhibition of maximal sTNFα-binding to TNFR1 or TNFR2 in a plate ELISA format.
  4. dIC50 concentration of V565 or adalimumab required to achieve 50% inhibition of maximal TNFα-induced response.