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).

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

Inclacumab 在0.4-40 μg/mL浓度范围内作用5分钟，显著抑制了P-选择素介导的全血和分离白细胞的黏附，对后者的抑制效果更为明显。[1]
Inclacumab 与P-选择素具有较高的亲和力，解离常数（Kd）为9.9 nM。它还有效地阻止了PSGL-1模拟肽与P-选择素的结合，IC50为1.9 μg/mL，并抑制了PSGL-1阳性细胞与P-选择素的黏附，IC50为430 ng/mL。[2]
另外，Inclacumab 在0-100 μg/mL的浓度范围内，剂量依赖性地减少了TRAP诱导的血小板-白细胞聚集，IC50为1.4 μg/mL。[3]

Inclacumab 以4 mg/kg的单次皮下给药，可以减轻TRAP和ADP诱导的食蟹猴血小板激活（PLA）。此外，每周静脉注射2至50 mg/kg的剂量，连续13周可有效抑制该物种中TRAP诱导的血小板激活。[3]