Table 1.
Examples of proteins and peptides administered subcutaneously[10]
| INN/BAN (description) | Trade name | MW (kDa) | Absolute bioavailability1 | SC animal models used in drug development |
| Buserelin acetate (LH-releasing hormone analog) | Suprefact | 1.30 | Human: 70% | Pharm: rat, hamster, guinea pig, rabbit, dog and monkey Tox: mouse, rat, rabbit and dog |
| Pramlintide acetate (amylin analog) | Symlin | 3.95 | Human: 30 to 40% | Pharm: rat and dog PK: mouse, rat, rabbit and dog Tox: mouse, rat, rabbit and dog |
| Insulin lispro (insulin analog) | Humalog | 5.81 | Human: 55 to 77% | Pharm: rat, rabbit, dog and pig PK: rat and dog Tox: rat, rabbit and dog |
| Insulin glulisine (insulin analog) | Apidra | 5.82 | Human: about 70% Dog: 42% Rat: 96%2 | Pharm: rat and dog PK: rat and dog Tox: mouse, rat, rabbit and dog |
| Insulin glargine (insulin analog) | Lantus | 6.06 | Precipitates in skin-slow uptake in human, dog and rat | Pharm: mouse, rat, guinea pig, rabbit and dog PK: rat and dog Tox: mouse, rat, guinea pig, rabbit and dog |
| Mecasermin (IGF-1) | Increlex | 7.65 | Human: about 100% Rabbit: 47% Rat: 38 to 57% | Pharm: mouse, rat, rabbit and monkey PK: rat, rabbit, dog and monkey Tox: rat, dog, rabbit and monkey |
| IFNβ-1b (cytokine) | Betaseron | 18.5 | Human: 50% Monkey: 31 to 44% | Pharm: monkey PK: monkey Tox: rabbit and monkey |
| Somatropin (GH) | Nutropin | 22 | Human: 81% | Pharm: rat PK: rat and monkey Tox: mouse, rat, dog and monkey |
| IFNβ-1a (cytokine) | Rebif | 22.5 | Human: 6 to 62% Monkey: 12 to 38% Rat: 16% | Pharm: mouse and monkey PK: rat and monkey Tox: monkey |
| PEG-IFNα-2b (cytokine variant) | PEG-Intron | 31 | Monkey: 57 to 89% Rat: 43 to 51% | Pharm: rat and monkey PK: rat and monkey Tox: mouse, rat, rabbit and monkey |
| Pegfilgrastim (PEG-G-CSF) | Neulasta | 39 | Monkey: 49 to 68% Rat: < 10% to 30% | Pharm: mouse, rat and dog PK: mouse, rat and monkey Tox: rat and monkey |
| Pegvisomant (PEG-GH) | Somavert | 42, 47 and 523 | Human: 49 to 65% Monkey: 70 to 81% Mouse: 45 to 73% | Pharm: mouse and monkey PK: mouse, rat, rabbit and monkey Tox: mouse, rat, rabbit and monkey |
| PEG-IFNα-2a (cytokine variant) | Pegasys | 60 | Human: 61 to 80% | Pharm: mouse PK: rat and monkey Tox: mouse, rat and monkey |
| Certolizumab pegol (PEG-anti-TNFα Fab' fragment) | Cimzia | 91 | Human: 76 to 88% Rat: 24 to 34% | PK: rat and monkey Tox: monkey |
| Canakinumab (anti-IL-1β mAb) | Ilaris | 145 | Human: 63 to 67% Monkey: 60% | Pharm: mouse, rat and monkey (marmoset) PK: mouse and monkey Tox: mouse and monkey |
| Adalimumab (anti-TNF mAb) | Humira | 148 | Human: 64% Monkey: 96% | PK: monkey Tox: rabbit and monkey |
| Omalizumab (anti-IgE mAb) | Xolair | 149 | Human: 53 to 71% Monkey: 64 to 104% Mouse: 90% | Pharm: monkey PK: mouse and monkey Tox: monkey |
| Golimumab (anti-TNF mAb) | Simponi | 150 | Human: 53% Monkey: 77% | PK: monkey Tox: mouse and monkey |
| Ustekinumab (anti-p40 mAb) | Stelara | 150 | Human: 24 to 95% Monkey: 97% | Pharm: monkey PK: monkey Tox: monkey |
| Etanercept (TNF receptor-Fc-IgG1 fusion protein) | Enbrel | 150 | Human: 76% Monkey: 73% Mouse: 58% | Pharm: mouse PK: mouse, rat and monkey Tox: mouse, rat, rabbit and monkey |
| Rilonacept (IL-1 inhibitor, fusion protein) | Arcalyst | 251 | Human: 43% Monkey: 70% Rat: 60% Mouse: 78% | Pharm: mouse and monkey PK: mouse, rat and monkey Tox: monkey |
1
Systemic dose following subcutaneous (SC) injection relative to systemic dose following intravenous injection;
2
Assumes linearity of AUC/dose;
3
Product is a mixture of three distinct protein variants. GH: Growth hormone; LH: Luteinizing hormone; MW: Molecular weight; Pharm: Pharmacology; PK: Pharmacokinetics; Tox: Toxicology (including safety pharmacology); INN: International nonproprietary name; BAN: British approved name; SC: Subcutaneous; PEG: Polyethylene glycol; IFN: Interferon; TNF: Tumor necrosis factor; IL: Interleukin.