Table 3.
Pharmacokinetics of TNFi in rheumatologic diseases.
| Infliximab | Etanerceptc | Adalimumab | Golimumab | Certolizumab | |
|---|---|---|---|---|---|
| Administration | IV | SC | SC | SC | SC |
| Loading dose | 3–5 mg/kg at 0, 2, and 6 wks | – | – | – | 400 mg at 0, 2, and 4 wks |
| Maintenance dosages | 3–10 mg/kg every 4–8 wks | 50 mg weekly | 40 mg eow | 50 mg once a month | 200 mg eow or 400 mg once a month |
| Half-life (t1/2) | 8–10 daysa | 3–5 days | 14 days | 14 daysd | 14 days |
| Clearance (L/d) | 0.26b | 1.67 | 0.269 | 0.40d | 0.408 |
| Bioavailability | – | 58% | 64% | 53% | 80% |
| Cmax (μg/ml) | 192 ± 51b | 2.4 ± 1.5 | 4.7 ± 1.6 | 2.5 | 43–49 (after loading dose) |
| References | [38,64,67–70] | [53,65,70–72] | [65,70,73] | [61,74] | [65,66] |
a
Population PK in PsA for infliximab: the t1/2 life was 15.7 days [75].
b
Based on 5 mg/kg IV in RA patients.
c
PK of etanercept 50 mg once weekly is comparable to 25 mg twice a week SC [76].
d
Population pharmacokinetics in PsA were characterized using a one-compartment model. Clearance: 0.68 L/d, t1/2 life of golimumab was 12.5 days [77]; eow: every other week; SC: subcutaneous; IV: intravenous; TNFi: tumor necrosis factor inhibitor; wk: week.