Rituximab

Category: pharmacological

Aliases: Rituxan, MabThera, IDEC-C2B8

Pharmacological Mechanism

Chimeric mouse/human anti-CD20 IgG1 monoclonal antibody — depletes CD20+ B cells via ADCC + CDC + apoptosis. First approved oncology mAb (1997). Indications: non-Hodgkin lymphoma, CLL, rheumatoid arthritis, granulomatosis with polyangiitis / microscopic polyangiitis, pemphigus vulgaris, MS (off-label), various autoimmune diseases. Biologic PK — long IgG-class t½ ~22 days, IgG salvage / FcRn-mediated clearance, not metabolized by CYPs. PK (Rozman 2017 popPK PMID:28339136 + Rituxan label): IV-only mAb. Two-compartment model with time-varying clearance. V1 (central) 2.7-3.1 L, V/F apparent ~5 L. Two clearance routes: nonspecific CL1 0.14 L/day (Fc-receptor-mediated reticuloendothelial uptake — slow + constant) + specific CL2 0.59 L/day (B-cell/tumor-burden mediated — declines as B cells are depleted). Median terminal t½ 22 days (range 6-52). Steady state by ~16-24 weeks of weekly dosing in NHL protocol.

Half-Life (t½)

IV: 528h

Dosing Guidelines

Target Organ Systems