TABLE 1

Overview of marketed IgGs and IgG Fc-fusion proteins administered via the subcutaneous route

Data on time to maximum serum concentration and bioavailability collected from the European Medicines Agency (EMA) Summary of Product Characteristics (http://www.ema.europa.eu/ema/index.jsp?curl=pages/home/Home_Page.jsp&mid=), EMA assessment reports, or the Food and Drug Administration homepage (http://www.accessdata.fda.gov/scripts/cder/drugsatfda).

INN NameTrade NameAntibody TypeTargetTmax in HumansBioavailability in Humans and Animals
days%
AdalimumabHumiraIgG1TNF5.5Humans: 64
Cynomolgus monkey: 96
CanakinumabIlarisIgG1IL-1β7Humans: 70
Marmoset: 60
DenosumabProliaIgG2RANK-L10Humans: 78
Mice: 86
Cynomolgus monkey: 28–100a
GolimumabSimponiIgG1TNF2–6Humans: 53
Cynomolgus monkey: 77
OmalizumabXolairIgG1IgE7–8Humans: 62
Mice: 90
Cynomolgus monkey: 64–104
RituximabMabtheraIgG1CD203Humans: 71
Mice: 63
Minipig: 71
TocilizumabActemra / RoActemraIgG1IL-6RHumans: 80
Minipig: 84
Cynomolgus monkey: 72
TrastuzumabHerceptinIgG1HER23Humans: 82
Mice: 83
Minipigs: 82
Cynomolgus monkey: ca. 100
UstekinumabStelaraIgG1IL-12/23p408.5Humans: 57 (24–95)
Cynomolgus monkey: 97
AbataceptOrenciaFc-fusion proteinCD80/863–5Humans: 79
Mice: 78–110
Rat: 41-63
EtanerceptEnbrelFc-fusion proteinTNF3Humans: 76
Mice: 58
Cynomolgus monkey: 73
RilonaceptArcalystFc-fusion proteinIL-1α, IL-1β, IL-1raHumans: 43
Mice: 78
Rats: 54
Cynomolgus monkey: 70
RomiplostimNplateFc-fusion proteinThrombopoietin receptor0.6Humans: –
Rats: 21–28
Cynomolgus monkey: 19
Rhesus monkey: 45–74
  • CD, Cluster of Differentiation; HER2, human epidermal growth factor receptor 2; IL, interleukin; INN, international nonproprietary name; RANK-L, receptor activator of nuclear factor-κB ligand; TNF, tumor necrosis factor.

  • a Bioavailability increases with increasing dose.