Inclacumab (Anti-Human selectin P Recombinant Antibody) is a fully humanized IgG4 monoclonal antibody that selectively binds to P-selectin. Inclacumab inhibits platelet leukocyte aggregation induced by thrombin receptor-activating peptide (TRAP) or adenosine diphosphate (ADP). Inclacumab inhibits platelet leukocyte aggregation induced by thrombin receptor activating peptide (TRAP) or adenosine diphosphate (ADP).

PSGL-1 mimetic peptide binding to P-selectin:1.9 μg/mL, P-selectin:9.9 nM (Kd), PSGL-1-positive cell adhesion to P-selectin:430 ng/mL, TRAP-induced platelet-leukocyte aggregation:1.4 μg/mL

Inclacumab acted in the concentration range of 0.4-40 μg/mL for 5 min and significantly inhibited P-selectin-mediated adhesion to whole blood and isolated leukocytes, with a more pronounced inhibitory effect on the latter. [1]
Inclacumab had a high affinity for P-selectin with a dissociation constant (Kd) of 9.9 nM. it also effectively blocked PSGL-1 mimetic peptide binding to P-selectin with an IC50 of 1.9 μg/mL and inhibited PSGL-1-positive cell adhesion to P-selectin with an IC50 of 430 ng/mL. [2]
In addition, Inclacumab dose-dependently reduced TRAP-induced platelet-leukocyte aggregation in the concentration range of 0-100 μg/mL with an IC50 of 1.4 μg/mL. [3]

Inclacumab administered as a single subcutaneous dose of 4 mg/kg attenuated TRAP- and ADP-induced platelet activation (PLA) in cynomolgus monkeys. In addition, weekly intravenous doses ranging from 2 to 50 mg/kg for 13 weeks effectively inhibited TRAP-induced platelet activation in this species. [3]

Human

Immobilized Human P-Selectin Protein (His) (TMPY-02709) at 1 μg/mL (100 μL/well) can bind Crizanlizumab. The EC50 is 8.99 ng/mL.

Monoclonal

Unconjugated