Table 1.

Clinical studies of therapeutic agents targeting the P-selectin/PSGL-1 pathway

Agent namePurposePhaseResultsClinicalTrials.gov identifier
Anti–P-selectin antibodies     
Crizanlizumab (SelG1, Adakveo)32,33,35  To assess efficacy in preventing or reducing VOC in SCD Phase 2 Reduced the rate of vaso-occlusive pain crisis NCT01895361 
 To assess efficacy in patients with brain metastases in combination with nivolumab Phase 1/2 recruiting Estimated completion in 2030 NCT05909618 
 To assess efficacy in treating retinal vasculopathy with cerebral leukoencephalopathy Phase 2 active, not recruiting Estimated completion in 2027 NCT04611880 
 To assess efficacy and safety in patients hospitalized with COVID-19 Phase 2 Reduced P-selectin levels by 89%, increased D-dimer levels by 77%, and decreased prothrombin fragment 1.2, but there were no significant differences between crizanlizumab and placebo in clinical end points NCT04435184
NCT04505774 
Inclaclumab (RO4905417)40-42  To evaluate the efficacy and safety in patients with non-STEMI undergoing coronary intervention Phase 2 Reduced myocardial injury in patients with non-STEMI undergoing coronary intervention NCT01327183 
 To evaluate the efficacy and safety in the prevention of saphenous vein graft disease in patients undergoing elective or urgent CABG surgery Phase 2 Did not prevent saphenous vein graft disease in patients undergoing elective or urgent CABG NCT01245634 
 To assess the safety and efficacy of a single dose in preventing VOC after an index VOC Phase 3 Completed in 2023, terminated due to slow enrollment NCT04927247 
 To assess the safety and efficacy in reducing the frequency of sickle cell VOC Phase 3 active, not recruiting Estimated completion in 2024 NCT04935879 
 To evaluate the safety of long-term administration in patients with SCD Phase 3 recruiting Estimated completion in 2028 NCT05348915 
Anti–PSGL-1 antibodies     
SelK243  To assess efficacy in preventing VTE in patients having a total knee replacement Phase 2 Failed to reduce the incidence of VTE compared with enoxaparin alone NCT03812328 
 To assess safety and efficacy in preserving airway function and reducing pulmonary inflammation after allergen challenge in patients with asthma and COPD Phase 2 Completed in 2022; results not published NCT04540042 
Recombinant PSGL-1-Ig     
YSPSL52,53  To evaluate the prevention of ischemic reperfusion injury in patients undergoing cadaveric orthotopic liver transplantation Phase 2 Measures of graft function trended toward improvement with normalized liver enzymes, but primary study endpoints were not achieved NCT00876902 
 To assess the safety and efficacy in preventing delayed graft function in patients undergoing cadaveric kidney transplantation Phase 1/2 Did not impact the rate of dialysis free delayed graft function NCT00298168 
Glycomimetics     
Cylexin (CY-1503)66  To assess the reduction of ischemia reperfusion injury in infant heart surgery Phase 2/3 Reduction of ischemia reperfusion injury was not demonstrated NCT00226369 
Rivipansel (GMI-1070)69,70  To evaluate the safety and the reduction in time for pain resolution in patients with VOC Phase 1/2 Reduced time to resolution of VOC, decreased the intake of opioids, and found to be safe NCT01119833 
 To evaluate efficacy and safety in treating patients with SCD, 6 years of age or older, experiencing a pain crisis necessitating hospitalization Phase 3 Efficacy was not observed NCT02187003 
Bimosiamose (TBC-1269)72-74  To assess the safety and efficacy in the treatment of plaque-type psoriasis when applied as a cream Phase 2 Reduction of epidermal thickness and lymphocyte infiltration, with no abnormal findings of safety parameters NCT00823693 
 To evaluate the safety and efficacy of inhaled bimosiamose for the treatment of patients with moderate to severe COPD Phase 2 Attenuation of airway inflammation, safe and well tolerated in patients with COPD NCT01108913 
 To evaluate the safety, tolerability and efficacy of repeated inhalation doses on ozone-induced sputum neutrophilia in healthy patients Phase 2 Favorable anti-inflammatory effects on ozone-induced airway inflammation in healthy volunteers NCT00962481 
Heparinoids     
PGX-10082  To determine whether PGX-100, when added to conventional treatment, is more effective in treating COPD exacerbations than conventional therapy alone Phase 2 Failed to achieve primary endpoints in the treatment of acute COPD NCT00457951 
Sevuparin83  To investigate efficacy and safety in the management of acute VOC in patients with SCD Phase 2 Failed to demonstrate efficacy in the management of VOC NCT02515838 
Small molecules     
PSI-697104,105  To assess the inhibition of platelet-leukocyte aggregates in patients who smoke Phase 1 The desired pharmacokinetic profile was not achieved and the formation of circulating platelet-leukocyte aggregates was not inhibited in people who smoke. NCT03860506 
 To evaluate the safety of an orally administered single dose in patients with scleritis Phase 1 Effective inhibition of leukocyte rolling in scleral blood vessels of individuals with autoimmune scleritis was not achieved NCT00367692 
P-selectin expression inhibitors     
Famotidine111  To assess efficacy in reducing endothelial expression of P-selectin in children with SCD Phase 2/3 recruiting Estimated completion in 2023, ongoing NCT05084521 
Agent namePurposePhaseResultsClinicalTrials.gov identifier
Anti–P-selectin antibodies     
Crizanlizumab (SelG1, Adakveo)32,33,35  To assess efficacy in preventing or reducing VOC in SCD Phase 2 Reduced the rate of vaso-occlusive pain crisis NCT01895361 
 To assess efficacy in patients with brain metastases in combination with nivolumab Phase 1/2 recruiting Estimated completion in 2030 NCT05909618 
 To assess efficacy in treating retinal vasculopathy with cerebral leukoencephalopathy Phase 2 active, not recruiting Estimated completion in 2027 NCT04611880 
 To assess efficacy and safety in patients hospitalized with COVID-19 Phase 2 Reduced P-selectin levels by 89%, increased D-dimer levels by 77%, and decreased prothrombin fragment 1.2, but there were no significant differences between crizanlizumab and placebo in clinical end points NCT04435184
NCT04505774 
Inclaclumab (RO4905417)40-42  To evaluate the efficacy and safety in patients with non-STEMI undergoing coronary intervention Phase 2 Reduced myocardial injury in patients with non-STEMI undergoing coronary intervention NCT01327183 
 To evaluate the efficacy and safety in the prevention of saphenous vein graft disease in patients undergoing elective or urgent CABG surgery Phase 2 Did not prevent saphenous vein graft disease in patients undergoing elective or urgent CABG NCT01245634 
 To assess the safety and efficacy of a single dose in preventing VOC after an index VOC Phase 3 Completed in 2023, terminated due to slow enrollment NCT04927247 
 To assess the safety and efficacy in reducing the frequency of sickle cell VOC Phase 3 active, not recruiting Estimated completion in 2024 NCT04935879 
 To evaluate the safety of long-term administration in patients with SCD Phase 3 recruiting Estimated completion in 2028 NCT05348915 
Anti–PSGL-1 antibodies     
SelK243  To assess efficacy in preventing VTE in patients having a total knee replacement Phase 2 Failed to reduce the incidence of VTE compared with enoxaparin alone NCT03812328 
 To assess safety and efficacy in preserving airway function and reducing pulmonary inflammation after allergen challenge in patients with asthma and COPD Phase 2 Completed in 2022; results not published NCT04540042 
Recombinant PSGL-1-Ig     
YSPSL52,53  To evaluate the prevention of ischemic reperfusion injury in patients undergoing cadaveric orthotopic liver transplantation Phase 2 Measures of graft function trended toward improvement with normalized liver enzymes, but primary study endpoints were not achieved NCT00876902 
 To assess the safety and efficacy in preventing delayed graft function in patients undergoing cadaveric kidney transplantation Phase 1/2 Did not impact the rate of dialysis free delayed graft function NCT00298168 
Glycomimetics     
Cylexin (CY-1503)66  To assess the reduction of ischemia reperfusion injury in infant heart surgery Phase 2/3 Reduction of ischemia reperfusion injury was not demonstrated NCT00226369 
Rivipansel (GMI-1070)69,70  To evaluate the safety and the reduction in time for pain resolution in patients with VOC Phase 1/2 Reduced time to resolution of VOC, decreased the intake of opioids, and found to be safe NCT01119833 
 To evaluate efficacy and safety in treating patients with SCD, 6 years of age or older, experiencing a pain crisis necessitating hospitalization Phase 3 Efficacy was not observed NCT02187003 
Bimosiamose (TBC-1269)72-74  To assess the safety and efficacy in the treatment of plaque-type psoriasis when applied as a cream Phase 2 Reduction of epidermal thickness and lymphocyte infiltration, with no abnormal findings of safety parameters NCT00823693 
 To evaluate the safety and efficacy of inhaled bimosiamose for the treatment of patients with moderate to severe COPD Phase 2 Attenuation of airway inflammation, safe and well tolerated in patients with COPD NCT01108913 
 To evaluate the safety, tolerability and efficacy of repeated inhalation doses on ozone-induced sputum neutrophilia in healthy patients Phase 2 Favorable anti-inflammatory effects on ozone-induced airway inflammation in healthy volunteers NCT00962481 
Heparinoids     
PGX-10082  To determine whether PGX-100, when added to conventional treatment, is more effective in treating COPD exacerbations than conventional therapy alone Phase 2 Failed to achieve primary endpoints in the treatment of acute COPD NCT00457951 
Sevuparin83  To investigate efficacy and safety in the management of acute VOC in patients with SCD Phase 2 Failed to demonstrate efficacy in the management of VOC NCT02515838 
Small molecules     
PSI-697104,105  To assess the inhibition of platelet-leukocyte aggregates in patients who smoke Phase 1 The desired pharmacokinetic profile was not achieved and the formation of circulating platelet-leukocyte aggregates was not inhibited in people who smoke. NCT03860506 
 To evaluate the safety of an orally administered single dose in patients with scleritis Phase 1 Effective inhibition of leukocyte rolling in scleral blood vessels of individuals with autoimmune scleritis was not achieved NCT00367692 
P-selectin expression inhibitors     
Famotidine111  To assess efficacy in reducing endothelial expression of P-selectin in children with SCD Phase 2/3 recruiting Estimated completion in 2023, ongoing NCT05084521 

CABG, coronary artery bypass; Ig, immunoglobulin; STEMI, ST elevation myocardial infarction; VOC, vaso-occlusive crisis; VTE, venous thromboembolism.

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